General Information of the Protein
Protein ID
PT01836
Protein Name
Gonadotropin-releasing hormone receptor
Gene Name
GNRHR
Secondarily
Gene Name
GRHR
Sequence
MANSASPEQNQNHCSAINNSIPLMQGNLPTLTLSGKIRVTVTFFLFLLSATFNASFLLKLQKWTQKKEKGKKLSRMKLLLKHLTLANLLETLIVMPLDGMWNITVQWYAGELLCKVLSYLKLFSMYAPAFMMVVISLDRSLAITRPLALKSNSKVGQSMVGLAWILSSVFAGPQLYIFRMIHLADSSGQTKVFSQCVTHCSFSQWWHQAFYNFFTFSCLFIIPLFIMLICNAKIIFTLTRVLHQDPHELQLNQSKNNIPRARLKTLKMTVAFATSFTVCWTPYYVLGIWYWFDPEMLNRLSDPVNHFFFLFAFLNPCFDPLIYGYFSL
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Short peptide receptor (family A GPCR)
>
GnRH receptor
Function
Receptor for gonadotropin releasing hormone (GnRH) that mediates the action of GnRH to stimulate the secretion of the gonadotropic hormones luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This receptor mediates its action by association with G-proteins that activate a phosphatidylinositol-calcium second messenger system. Isoform 2 may act as an inhibitor of GnRH-R signaling.
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Uniprot ID
Primary ID:
P30968

Secondarily ID:
O75793
Q14D13
Q92644
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Ensembl ID
ENSG00000109163
HGNC ID
HGNC:4421
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0495920
ethyl 3-[[benzyl(methyl)amino]methyl]-7-[(2,6-difluorophenyl)methyl]-2-[4-(methylcarbamoylamino)phenyl]-4-oxothieno[2,3-b]pyridine-5-carboxylate
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C34H32F2N4O4S
 1
1
IC50 = 0.06 nM
   TI
   LI
   LO
   TS
CP0039875
1-(4-(1-(2,6-difluorobenzyl)-5-((benzyl(methyl)amino)methyl)-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-methoxyurea
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C36H31F2N5O4S
 7
1
IC50 = 0.06 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.1 nM
   TI
   LI
   LO
   TS
3
IC50 = 0.6 nM
   TI
   LI
   LO
   TS
4
IC50 = 1.6 nM
   TI
   LI
   LO
   TS
5
IC50 = 1.9 nM
   TI
   LI
   LO
   TS
6
IC50 = 10 nM
   TI
   LI
   LO
   TS
7
IC50 = 270 nM
   TI
   LI
   LO
   TS
CP0359982
3-(N-benzyl-N-methylaminomethyl)-7-(2,6-difluorobenzyl)-4,7-dihydro-5-isobutyryl-2-[4-(3-methyluriedo)phenyl]-4-oxothieno[2,3-b]pyridine
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C35H34F2N4O3S
 3
1
IC50 = 0.07 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.1 nM
   TI
   LI
   LO
   TS
3
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
CP0464346
ethyl 3-[[benzyl(methyl)amino]methyl]-7-[(2-fluorophenyl)methyl]-2-[4-(methylcarbamoylamino)phenyl]-4-oxothieno[2,3-b]pyridine-5-carboxylate
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C34H33FN4O4S
 1
1
IC50 = 0.07 nM
   TI
   LI
   LO
   TS
CP0061893
1-(4-(1-(2,6-difluorobenzyl)-5-((benzyl(methyl)amino)methyl)-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-ethylurea
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C37H33F2N5O3S
 4
1
IC50 = 0.07 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.1 nM
   TI
   LI
   LO
   TS
3
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
4
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0199103
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[[2-methoxyethyl(methyl)amino]methyl]-3-(6-methoxypyridin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
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C32H32F2N6O6S
 4
1
IC50 = 0.07 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
3
IC50 = 0.49 nM
   TI
   LI
   LO
   TS
4
IC50 = 0.8 nM
   TI
   LI
   LO
   TS
CP0231917
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[[methyl(2-pyridin-2-ylethyl)amino]methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
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C36H32F2N6O4S
 1
1
IC50 = 0.07 nM
   TI
   LI
   LO
   TS
CP0050490
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[[2-methoxyethyl(methyl)amino]methyl]-3-(4-methoxyphenyl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
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C33H33F2N5O6S
 4
1
IC50 = 0.07 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.17 nM
   TI
   LI
   LO
   TS
3
IC50 = 0.29 nM
   TI
   LI
   LO
   TS
4
IC50 = 0.43 nM
   TI
   LI
   LO
   TS
CP0048798
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[[methyl(pyridin-2-ylmethyl)amino]methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
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C35H30F2N6O4S
 2
1
IC50 = 0.08 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.09 nM
   TI
   LI
   LO
   TS
CP0050481
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[[2-methoxyethyl(methyl)amino]methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
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C32H31F2N5O5S
 4
1
IC50 = 0.08 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.1 nM
   TI
   LI
   LO
   TS
3
IC50 = 0.5 nM
   TI
   LI
   LO
   TS
4
IC50 = 1.4 nM
   TI
   LI
   LO
   TS
CP0295225
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[[2-methoxyethyl(methyl)amino]methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
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C31H31F2N7O6S
 4
1
IC50 = 0.08 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.24 nM
   TI
   LI
   LO
   TS
3
IC50 = 0.26 nM
   TI
   LI
   LO
   TS
4
IC50 = 0.94 nM
   TI
   LI
   LO
   TS
CP0338284
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
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C29H27F2N7O5S
 4
1
IC50 = 0.08 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.33 nM
   TI
   LI
   LO
   TS
3
IC50 = 0.82 nM
   TI
   LI
   LO
   TS
4
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0351993
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[[methyl-[2-(2-oxopyrrolidin-1-yl)ethyl]amino]methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
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C35H34F2N6O5S
 2
1
IC50 = 0.09 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.21 nM
   TI
   LI
   LO
   TS
CP0497061
7-Chloro-2-oxo-4-[2-(4-oxo-azetidin-2-yl)-ethoxy]-3-((S)-3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid [1,2,5]thiadiazol-3-ylamide
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C26H24ClN5O4S
 2
1
IC50 = 0.1 nM
   TI
   LI
   LO
   TS
2
IC50 = 1.3 nM
   TI
   LI
   LO
   TS
CP0309511
3-(N-benzyl-N-methylaminomethyl)-7-(2,6-difluorobenzyl)-4,7-dihydro-2-[4-(1-hydroxy-1-cyclopropanecarboxamido)-phenyl]-5-isobutyryl-4-oxothieno[2,3-b]pyridine
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C37H37F2N3O4S
 3
1
IC50 = 0.1 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.9 nM
   TI
   LI
   LO
   TS
3
IC50 = 15 nM
   TI
   LI
   LO
   TS
CP0464280
ethyl 3-[[benzyl(methyl)amino]methyl]-7-[(2,6-difluorophenyl)methyl]-4-oxo-2-[4-(propanoylamino)phenyl]thieno[2,3-b]pyridine-5-carboxylate
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C35H33F2N3O4S
 1
1
IC50 = 0.1 nM
   TI
   LI
   LO
   TS
CP0464345
N-[4-[5-benzoyl-3-[[benzyl(methyl)amino]methyl]-7-[(2,6-difluorophenyl)methyl]-4-oxothieno[2,3-b]pyridin-2-yl]phenyl]-2-methylpropanamide
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C40H35F2N3O3S
 1
1
IC50 = 0.1 nM
   TI
   LI
   LO
   TS
CP0509912
1-[4-[5-[[benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methylurea
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C36H31F2N5O3S
 1
1
IC50 = 0.1 nM
   TI
   LI
   LO
   TS
CP0048796
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[[[6-(hydroxymethyl)pyridin-2-yl]methyl-methylamino]methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
   Show/Hide
C36H32F2N6O5S
 2
1
IC50 = 0.1 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.24 nM
   TI
   LI
   LO
   TS
CP0231905
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[[2-methoxyethyl(methyl)amino]methyl]-3-(5-methylpyridin-2-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
   Show/Hide
C32H32F2N6O5S
 4
1
IC50 = 0.1 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.18 nM
   TI
   LI
   LO
   TS
3
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
4
IC50 = 1.3 nM
   TI
   LI
   LO
   TS
CP0050489
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
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C30H28F2N6O5S
 4
1
IC50 = 0.12 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.26 nM
   TI
   LI
   LO
   TS
3
IC50 = 0.55 nM
   TI
   LI
   LO
   TS
4
IC50 = 0.95 nM
   TI
   LI
   LO
   TS
CP0039874
3-[(Benzyl-methyl-amino)-methyl]-7-(2,6-difluoro-benzyl)-2-(4-isobutyrylamino-phenyl)-4-oxo-4,7-dihydro-thieno[2,3-b]pyridine-5-carboxylic acid isopropyl ester; hydrochloride
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C37H37F2N3O4S
 4
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.6 nM
   TI
   LI
   LO
   TS
3
IC50 = 2 nM
   TI
   LI
   LO
   TS
4
Ki = 0.2 nM
   TI
   LI
   LO
   TS
CP0521653
3-(N-benzyl-N-methylaminomethyl)-7-(2,6-difluorobenzyl)-4,7-dihydro-2-(4-(2-hydroxy-2-methylpropionylamido)phenyl)-5-isobutyryl-4-oxothieno[2,3-b]pyridine
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C37H37F2N3O4S
 1
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
CP0536569
N-[4-[3-[[benzyl(methyl)amino]methyl]-7-[(2,6-difluorophenyl)methyl]-5-(2-methylpropanoyl)-4-oxothieno[2,3-b]pyridin-2-yl]phenyl]-2-methylpropanamide
   Show/Hide
C37H37F2N3O3S
 1
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
CP0538121
3-(N-benzyl-N-methylaminomethyl)-7-(2,6-difluorobenzyl)-4,7-dihydro-2-[4-(2-hydroxyacetamido)phenyl]-5-isobutyryl-4-oxothieno[2,3-b]pyridine
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C35H33F2N3O4S
 1
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
CP0897586
ethyl 3-(N-benzyl-N-methylaminomethyl)-7-(2,6-difluorobenzyl)-4,7-dihydro-2-(4-isobutyrylamidophenyl)-4-oxothieno[2,3-b]pyridine-5-carboxylate hydrochloride
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C36H36ClF2N3O4S
 1
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
CP0405458
1-{4-[5-[(Benzyl-methyl-amino)-methyl]-1-(2,6-difluoro-benzyl)-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydro-thieno[2,3-d]pyrimidin-6-yl]-phenyl}-3-isopropyl-urea; HCL.H2O
   Show/Hide
C38H35F2N5O3S
 1
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
CP0495465
N-[4-[5-[[benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-3-(3-methoxyphenyl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]propanamide
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C38H34F2N4O4S
 1
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
CP0508582
1-{4-[5-[(Benzyl-methyl-amino)-methyl]-1-(2,6-difluoro-benzyl)-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydro-thieno[2,3-d]pyrimidin-6-yl]-phenyl}-3-ethoxy-urea; HCL.2.H2O
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C37H33F2N5O4S
 1
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
CP0778924
3-[(Benzyl-methyl-amino)-methyl]-7-(2,6-difluoro-benzyl)-2-(4-isobutyrylamino-phenyl)-4-oxo-4,7-dihydro-thieno[2,3-b]pyridine-5-carboxylic acid isopropyl ester hydrochloride
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C37H38ClF2N3O4S
 3
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.6 nM
   TI
   LI
   LO
   TS
3
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0050491
1-[4-[1-[(2,6-difluorophenyl)methyl]-3-(5-fluoropyridin-2-yl)-5-[[2-methoxyethyl(methyl)amino]methyl]-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
   Show/Hide
C31H29F3N6O5S
 2
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
2
IC50 = 1 nM
   TI
   LI
   LO
   TS
CP0050492
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[[2-methoxyethyl(methyl)amino]methyl]-2,4-dioxo-3-pyridin-2-ylthieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
   Show/Hide
C31H30F2N6O5S
 4
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
3
IC50 = 0.83 nM
   TI
   LI
   LO
   TS
4
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0143092
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[[methyl-[2-[methyl(methylsulfonyl)amino]ethyl]amino]methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
   Show/Hide
C33H34F2N6O6S2
 2
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.27 nM
   TI
   LI
   LO
   TS
CP0338285
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[[methyl(pyridin-3-ylmethyl)amino]methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
   Show/Hide
C35H30F2N6O4S
 1
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
CP0342912
1-[4-[1-[(2,6-difluorophenyl)methyl]-3-(2-methoxyethyl)-5-[[2-methoxyethyl(methyl)amino]methyl]-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
   Show/Hide
C29H33F2N5O6S
 2
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.29 nM
   TI
   LI
   LO
   TS
CP0344569
1-[4-[1-[(2,6-difluorophenyl)methyl]-3-(2-ethoxyethyl)-5-[[2-methoxyethyl(methyl)amino]methyl]-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
   Show/Hide
C30H35F2N5O6S
 2
1
IC50 = 0.2 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.37 nM
   TI
   LI
   LO
   TS
CP0448182
3-[(Benzyl-methyl-amino)-methyl]-8-(2,6-difluoro-benzyl)-2-[4-(3-ethyl-ureido)-phenyl]-5-oxo-5,8-dihydro-imidazo[1,2-a]pyrimidine-6-carboxylic acid propyl ester
   Show/Hide
C35H36F2N6O4
 1
1
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
CP0095035
7-Chloro-2-oxo-4-((S)-2-piperidin-2-yl-ethoxy)-3-(3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid pyrimidin-4-ylamide
   Show/Hide
C30H32ClN5O3
 2
1
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
2
IC50 = 2.2 nM
   TI
   LI
   LO
   TS
CP0445881
7-Chloro-2-oxo-4-[2-(5-oxo-pyrrolidin-2-yl)-ethoxy]-3-((R)-3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid [1,2,5]thiadiazol-3-ylamide
   Show/Hide
C27H26ClN5O4S
 2
1
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.7 nM
   TI
   LI
   LO
   TS
CP0091820
ELIGARD
   Show/Hide
C59H84N16O12
 1
1
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
CP0272654
N-[4-[5-[[benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]propanamide
   Show/Hide
C37H32F2N4O3S
 4
1
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
2
IC50 = 4 nM
   TI
   LI
   LO
   TS
3
IC50 = 9 nM
   TI
   LI
   LO
   TS
4
IC50 = 300 nM
   TI
   LI
   LO
   TS
CP0481013
N-[4-[5-[[benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-3-(3-methoxyphenyl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-2-methylpropanamide
   Show/Hide
C39H36F2N4O4S
 1
1
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
CP0050493
1-[4-[1-[(2,6-difluorophenyl)methyl]-3-(2-hydroxy-2-methylpropyl)-5-[[2-methoxyethyl(methyl)amino]methyl]-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
   Show/Hide
C30H35F2N5O6S
 1
1
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
CP0292069
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[[methyl-[2-(triazol-1-yl)ethyl]amino]methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
   Show/Hide
C33H30F2N8O4S
 1
1
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
CP0351991
1-[4-[1-[(2,6-difluorophenyl)methyl]-3-(2-hydroxyethyl)-5-[[2-methoxyethyl(methyl)amino]methyl]-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
   Show/Hide
C28H31F2N5O6S
 1
1
IC50 = 0.3 nM
   TI
   LI
   LO
   TS
CP0445780
4-(2-Azetidin-2-yl-ethoxy)-7-chloro-2-oxo-3-((S)-3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid [1,2,5]thiadiazol-3-ylamide
   Show/Hide
C26H26ClN5O3S
 2
1
IC50 = 0.32 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.8 nM
   TI
   LI
   LO
   TS
CP0457343
3-[(Benzyl-methyl-amino)-methyl]-8-(2,6-difluoro-benzyl)-2-[4-(3-methoxy-ureido)-phenyl]-5-oxo-5,8-dihydro-imidazo[1,2-a]pyrimidine-6-carboxylic acid propyl ester
   Show/Hide
C34H34F2N6O5
 1
1
IC50 = 0.4 nM
   TI
   LI
   LO
   TS
CP0449419
ethyl 7-benzyl-3-[[benzyl(methyl)amino]methyl]-4-oxo-2-[4-(propanoylamino)phenyl]thieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C35H35N3O4S
 1
1
IC50 = 0.4 nM
   TI
   LI
   LO
   TS
CP0495919
3-(N-benzyl-N-methylaminomethyl)-7-(2,6-difluorobenzyl)-4,7-dihydro-5-(1-hydroxy-2-methylpropyl)-2-(4-isobutyrylamidophenyl)-4-oxothieno[2,3-b]pyridine
   Show/Hide
C37H39F2N3O3S
 1
1
IC50 = 0.4 nM
   TI
   LI
   LO
   TS
CP0511042
3-(N-benzyl-N-methylaminomethyl)-7-(2,6-difluorobenzyl)-4,7-dihydro-2-(4-isobutyrylamidophenyl)-4-oxo-5-propionyl-thieno[2,3-b]pyridine
   Show/Hide
C36H35F2N3O3S
 1
1
IC50 = 0.4 nM
   TI
   LI
   LO
   TS
CP0193577
N-[4-[5-[[benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-2-methylpropanamide
   Show/Hide
C38H34F2N4O3S
 1
1
IC50 = 0.4 nM
   TI
   LI
   LO
   TS
CP0504133
1-{4-[5-[(Benzyl-methyl-amino)-methyl]-1-(2,6-difluoro-benzyl)-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydro-thieno[2,3-d]pyrimidin-6-yl]-phenyl}-3-hydroxy-urea; HCL.H2O
   Show/Hide
C35H29F2N5O4S
 1
1
IC50 = 0.4 nM
   TI
   LI
   LO
   TS
CP0037858
(S)-4-(2-(azetidin-2-yl)ethoxy)-7-chloro-2-oxo-N-(pyrimidin-4-yl)-3-(3,4,5-trimethylphenyl)-1,2-dihydroquinoline-6-carboxamide
   Show/Hide
C28H28ClN5O3
 2
1
IC50 = 0.44 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.9 nM
   TI
   LI
   LO
   TS
CP0405359
3-[(Benzyl-methyl-amino)-methyl]-8-(2,6-difluoro-benzyl)-2-[4-(3-ethyl-ureido)-phenyl]-5-oxo-5,8-dihydro-imidazo[1,2-a]pyrimidine-6-carboxylic acid ethyl ester
   Show/Hide
C34H34F2N6O4
 3
1
IC50 = 0.5 nM
   TI
   LI
   LO
   TS
2
IC50 = 70.79 nM
   TI
   LI
   LO
   TS
3
Ki = 4.786 nM
   TI
   LI
   LO
   TS
CP0433534
7-Chloro-2-oxo-4-(2-piperidin-2-yl-ethoxy)-3-((S)-3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid [1,2,5]thiadiazol-3-ylamide
   Show/Hide
C28H30ClN5O3S
 2
1
IC50 = 0.55 nM
   TI
   LI
   LO
   TS
2
IC50 = 1.6 nM
   TI
   LI
   LO
   TS
CP0391243
7-Chloro-2-oxo-4-[2-(tetrahydro-furan-2-yl)-ethoxy]-3-(3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid pyrimidin-4-ylamide
   Show/Hide
C29H29ClN4O4
 2
1
IC50 = 0.6 nM
   TI
   LI
   LO
   TS
2
IC50 = 3.3 nM
   TI
   LI
   LO
   TS
CP0403266
4-[2-(1-Aza-bicyclo[2.2.2]oct-2-yl)-ethoxy]-7-chloro-2-oxo-3-(3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid [1,2,5]thiadiazol-3-ylamide
   Show/Hide
C30H32ClN5O3S
 2
1
IC50 = 0.6 nM
   TI
   LI
   LO
   TS
2
IC50 = 5.8 nM
   TI
   LI
   LO
   TS
CP0500775
7-Chloro-4-(2-[1,3]dioxolan-2-yl-ethoxy)-2-oxo-3-(3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid [1,2,5]thiadiazol-3-ylamide
   Show/Hide
C26H25ClN4O5S
 2
1
IC50 = 0.6 nM
   TI
   LI
   LO
   TS
2
IC50 = 67 nM
   TI
   LI
   LO
   TS
CP0461249
ethyl 7-benzyl-3-[[benzyl(methyl)amino]methyl]-2-[4-(2-methylpropanoylamino)phenyl]-4-oxothieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C36H37N3O4S
 1
1
IC50 = 0.6 nM
   TI
   LI
   LO
   TS
CP0497860
1-{4-[5-[(Benzyl-methyl-amino)-methyl]-1-(2,6-difluoro-benzyl)-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydro-thieno[2,3-d]pyrimidin-6-yl]-phenyl}-3-isopropoxy-urea; HCL.0.5 H2O
   Show/Hide
C38H35F2N5O4S
 1
1
IC50 = 0.6 nM
   TI
   LI
   LO
   TS
CP0397324
3-[(Benzyl-methyl-amino)-methyl]-8-(2,6-difluoro-benzyl)-2-[4-(3-methoxy-ureido)-phenyl]-5-oxo-5,8-dihydro-imidazo[1,2-a]pyrimidine-6-carboxylic acid ethyl ester
   Show/Hide
C33H32F2N6O5
 1
1
IC50 = 0.7 nM
   TI
   LI
   LO
   TS
CP0439544
7-Chloro-4-(2-morpholin-3-yl-ethoxy)-2-oxo-3-(3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid [1,2,5]thiadiazol-3-ylamide
   Show/Hide
C27H28ClN5O4S
 2
1
IC50 = 0.7 nM
   TI
   LI
   LO
   TS
2
IC50 = 32 nM
   TI
   LI
   LO
   TS
CP0854506
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-2-oxo-6-([1,2,5]thiadiazol-3-ylcarbamoyl)-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C29H29ClF3N5O5S
 2
1
IC50 = 0.8 nM
   TI
   LI
   LO
   TS
2
IC50 = 5.9 nM
   TI
   LI
   LO
   TS
CP0455638
7-Chloro-2-oxo-4-(2-pyrrolidin-2-yl-ethoxy)-3-((S)-3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid pyrimidin-4-ylamide
   Show/Hide
C29H30ClN5O3
 2
1
IC50 = 0.8 nM
   TI
   LI
   LO
   TS
2
IC50 = 2.2 nM
   TI
   LI
   LO
   TS
CP0874937
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-2-oxo-6-(pyrimidin-4-ylcarbamoyl)-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C31H31ClF3N5O5
 2
1
IC50 = 0.9 nM
   TI
   LI
   LO
   TS
2
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0509637
7-Chloro-4-(2-oxetan-2-yl-ethoxy)-2-oxo-3-((R)-3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid [1,2,5]thiadiazol-3-ylamide
   Show/Hide
C26H25ClN4O4S
 2
1
IC50 = 0.9 nM
   TI
   LI
   LO
   TS
2
IC50 = 49 nM
   TI
   LI
   LO
   TS
CP0213550
5-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-1H-pyridin-2-one
   Show/Hide
C37H46N4O2
 1
1
IC50 = 1 nM
   TI
   LI
   LO
   TS
CP0496785
ethyl 2-(4-benzamidophenyl)-7-benzyl-3-[[benzyl(methyl)amino]methyl]-4-oxothieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C39H35N3O4S
 1
1
IC50 = 1 nM
   TI
   LI
   LO
   TS
CP0061895
N-[4-[5-[[benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]benzamide
   Show/Hide
C41H32F2N4O3S
 1
1
IC50 = 1 nM
   TI
   LI
   LO
   TS
CP0510377
6-(4-Amino-phenyl)-5-[(benzyl-methyl-amino)-methyl]-1-(2,6-difluoro-benzyl)-3-(3-methoxy-phenyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione; HCL.H2O
   Show/Hide
C35H30F2N4O3S
 1
1
IC50 = 1 nM
   TI
   LI
   LO
   TS
CP0853701
Trifluoro-acetate2-{2-[7-chloro-6-(6-chloro-pyrimidin-4-ylcarbamoyl)-3-(3,5-dimethyl-phenyl)-2-oxo-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C31H30Cl2F3N5O5
 2
1
IC50 = 1.4 nM
   TI
   LI
   LO
   TS
2
IC50 = 14.5 nM
   TI
   LI
   LO
   TS
CP0227902
5-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-1-methyl-1H-pyridin-2-one
   Show/Hide
C38H48N4O2
 1
1
IC50 = 1.4 nM
   TI
   LI
   LO
   TS
CP0432859
7-Chloro-4-[2-(1-methyl-5-oxo-pyrrolidin-2-yl)-ethoxy]-2-oxo-3-((R)-3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid [1,2,5]thiadiazol-3-ylamide
   Show/Hide
C28H28ClN5O4S
 2
1
IC50 = 1.4 nM
   TI
   LI
   LO
   TS
2
IC50 = 11 nM
   TI
   LI
   LO
   TS
CP0880181
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-6-(2-methyl-pyrimidin-4-ylcarbamoyl)-2-oxo-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C32H33ClF3N5O5
 2
1
IC50 = 1.8 nM
   TI
   LI
   LO
   TS
2
IC50 = 33.3 nM
   TI
   LI
   LO
   TS
CP0299019
1-(1R,4S)-2-Aza-bicyclo[2.2.1]hept-2-yl-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(2-pyridin-4-yl-ethylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
   Show/Hide
C36H44N4O
 1
1
IC50 = 1.9 nM
   TI
   LI
   LO
   TS
CP0889555
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-2-oxo-6-([1,2,5]thiadiazol-3-ylcarbamoyl)-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C29H29ClF3N5O5S
 2
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
2
IC50 = 6.4 nM
   TI
   LI
   LO
   TS
CP0392522
7-Chloro-4-[2-((R)-1-methyl-6-trifluoromethyl-piperidin-2-yl)-ethoxy]-2-oxo-3-((S)-3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid pyrimidin-4-ylamide
   Show/Hide
C32H33ClF3N5O3
 2
1
IC50 = 2 nM
   TI
   LI
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   TS
2
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0497965
7-Chloro-2-oxo-4-[2-((R)-6-trifluoromethyl-piperidin-2-yl)-ethoxy]-3-((S)-3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid pyrimidin-4-ylamide
   Show/Hide
C31H31ClF3N5O3
 2
1
IC50 = 2 nM
   TI
   LI
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   TS
2
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0486698
ethyl 2-(4-acetamidophenyl)-7-benzyl-3-[[benzyl(methyl)amino]methyl]-4-oxothieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C34H33N3O4S
 1
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0551303
ethyl 7-benzyl-3-[[benzyl(methyl)amino]methyl]-2-[4-[methyl(methylcarbamoyl)amino]phenyl]-4-oxothieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C35H36N4O4S
 1
1
IC50 = 2 nM
   TI
   LI
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   TS
CP0869693
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-6-(5-methyl-isoxazol-3-ylcarbamoyl)-2-oxo-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C31H32ClF3N4O6
 2
1
IC50 = 2.3 nM
   TI
   LI
   LO
   TS
2
IC50 = 77.5 nM
   TI
   LI
   LO
   TS
CP0135587
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(2-pyridin-3-yl-ethylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
   Show/Hide
C37H46N4O
 1
1
IC50 = 2.6 nM
   TI
   LI
   LO
   TS
CP0880585
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-6-(6-methyl-pyrimidin-4-ylcarbamoyl)-2-oxo-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C32H33ClF3N5O5
 2
1
IC50 = 2.8 nM
   TI
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   TS
2
IC50 = 44 nM
   TI
   LI
   LO
   TS
CP0216361
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
   Show/Hide
C39H50N4O
 1
1
IC50 = 2.8 nM
   TI
   LI
   LO
   TS
CP0866906
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-6-(3-methyl-isothiazol-5-ylcarbamoyl)-2-oxo-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C31H32ClF3N4O5S
 2
1
IC50 = 2.9 nM
   TI
   LI
   LO
   TS
2
IC50 = 21.5 nM
   TI
   LI
   LO
   TS
CP0397655
2-(4-Acryloylamino-phenyl)-3-[(benzyl-methyl-amino)-methyl]-8-(2,6-difluoro-benzyl)-5-oxo-5,8-dihydro-imidazo[1,2-a]pyrimidine-6-carboxylic acid ethyl ester
   Show/Hide
C34H31F2N5O4
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0458966
3-[(Benzyl-methyl-amino)-methyl]-8-(2,6-difluoro-benzyl)-2-{4-[(furan-3-carbonyl)-amino]-phenyl}-5-oxo-5,8-dihydro-imidazo[1,2-a]pyrimidine-6-carboxylic acid ethyl ester
   Show/Hide
C36H31F2N5O5
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0847468
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-2-oxo-6-(pyrimidin-4-ylcarbamoyl)-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C31H31ClF3N5O5
 2
1
IC50 = 3.2 nM
   TI
   LI
   LO
   TS
2
IC50 = 8.3 nM
   TI
   LI
   LO
   TS
CP0847471
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-2-oxo-6-(pyridin-2-ylcarbamoyl)-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C32H32ClF3N4O5
 2
1
IC50 = 3.6 nM
   TI
   LI
   LO
   TS
2
IC50 = 19 nM
   TI
   LI
   LO
   TS
CP0850053
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-2-oxo-6-(pyridin-4-ylcarbamoyl)-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C32H32ClF3N4O5
 2
1
IC50 = 3.8 nM
   TI
   LI
   LO
   TS
2
IC50 = 10.6 nM
   TI
   LI
   LO
   TS
CP0522236
5-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-1-methoxymethyl-1H-pyridin-2-one
   Show/Hide
C39H50N4O3
 1
1
IC50 = 3.9 nM
   TI
   LI
   LO
   TS
CP0327922
1-(1R,4S)-2-Aza-bicyclo[2.2.1]hept-2-yl-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
   Show/Hide
C38H48N4O
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0371321
5-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-1,3-dimethyl-1H-pyridin-2-one
   Show/Hide
C39H50N4O2
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0409867
3-[(Benzyl-methyl-amino)-methyl]-2-[4-(cyclopropanecarbonyl-amino)-phenyl]-8-(2,6-difluoro-benzyl)-5-oxo-5,8-dihydro-imidazo[1,2-a]pyrimidine-6-carboxylic acid ethyl ester
   Show/Hide
C35H33F2N5O4
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0063211
1-(7-Aza-bicyclo[2.2.1]hept-7-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
   Show/Hide
C38H48N4O
 1
1
IC50 = 5.7 nM
   TI
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CP0361002
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-1-methyl-2-[2-(2-methyl-1-oxy-pyridin-4-yl)-ethylamino]-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
   Show/Hide
C38H48N4O2
 1
1
IC50 = 5.9 nM
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CP0112281
3-[(Benzyl-methyl-amino)-methyl]-7-(2,6-difluoro-benzyl)-2-(4-methoxy-phenyl)-4-oxo-4,7-dihydro-thieno[2,3-b]pyridine-5-carboxylic acid ethyl ester
   Show/Hide
C33H30F2N2O4S
 1
1
IC50 = 6 nM
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CP0364803
2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-1-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-propan-1-one
   Show/Hide
C42H56N4O
 1
1
IC50 = 6.4 nM
   TI
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CP0122740
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-1-methyl-2-[2-(1-oxy-pyridin-4-yl)-ethylamino]-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
   Show/Hide
C37H46N4O2
 1
1
IC50 = 6.4 nM
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CP0336314
1-(6-Aza-bicyclo[3.2.1]oct-6-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
   Show/Hide
C39H50N4O
 1
1
IC50 = 6.8 nM
   TI
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   TS
CP0896758
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-2-oxo-6-(pyrazin-2-ylcarbamoyl)-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C31H31ClF3N5O5
 2
1
IC50 = 7 nM
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2
IC50 = 16 nM
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CP0196863
1-(7-Aza-bicyclo[2.2.1]hept-7-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(2-pyridin-4-yl-ethylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
   Show/Hide
C36H44N4O
 1
1
IC50 = 7 nM
   TI
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   TS
CP0535305
3-[(Benzyl-methyl-amino)-methyl]-8-(2,6-difluoro-benzyl)-5-oxo-2-{4-[(thiophene-3-carbonyl)-amino]-phenyl}-5,8-dihydro-imidazo[1,2-a]pyrimidine-6-carboxylic acid ethyl ester
   Show/Hide
C36H31F2N5O4S
 1
1
IC50 = 7 nM
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CP0213240
(S)-1-(2-aza-bicyclo[2.2.2]octan-2-yl)-2-(2-(3,5-dimethylphenyl)-3-(1-(2-(pyridin-4-yl)ethylamino)propan-2-yl)-1H-indol-5-yl)-2-methylpropan-1-one
   Show/Hide
C37H46N4O
 1
1
IC50 = 7.2 nM
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CP0464146
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-2-[2-(2-hydroxymethyl-pyridin-4-yl)-ethylamino]-1-methyl-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
   Show/Hide
C38H48N4O2
 1
1
IC50 = 7.5 nM
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CP0464278
3-(N-benzyl-N-methylaminomethyl)-7-(2,6-difluorobenzyl)-4,7-dihydro-N-isopropyl-4-oxo-2-(4-propionylamidophenyl)-thieno[2,3-b]pyridine-5-carboxamide
   Show/Hide
C36H36F2N4O3S
 1
1
IC50 = 8 nM
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   TS
CP0272840
5-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-1-methyl-piperidin-2-one
   Show/Hide
C38H52N4O2
 1
1
IC50 = 8.2 nM
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   TS
CP0256294
2-{2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-N,N-diisobutyl-isobutyramide
   Show/Hide
C39H54N4O
 1
1
IC50 = 8.3 nM
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CP0076599
1-(1S,4R)-2-Aza-bicyclo[2.2.1]hept-2-yl-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
   Show/Hide
C38H48N4O
 1
1
IC50 = 8.7 nM
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CP0208585
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-1-methyl-2-[2-(2-methyl-pyridin-4-yl)-ethylamino]-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
   Show/Hide
C38H48N4O
 1
1
IC50 = 8.7 nM
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CP0334675
1-(8-Aza-bicyclo[3.2.1]oct-8-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
   Show/Hide
C39H50N4O
 1
1
IC50 = 8.8 nM
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CP0845332
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-6-(2-methoxy-pyrimidin-4-ylcarbamoyl)-2-oxo-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C32H33ClF3N5O6
 2
1
IC50 = 9 nM
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2
IC50 = 133 nM
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CP0524417
2-[4-(2-aminoacetamido)phenyl]-3-(N-benzyl-N-methylaminomethyl)-7-(2,6-difluorobenzyl)-4,7-dihydro-5-isobutyryl-4-oxothieno[2,3-b]pyridine
   Show/Hide
C35H34F2N4O3S
 1
1
IC50 = 9 nM
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CP0510586
3-[(Benzyl-methyl-amino)-methyl]-8-(2,6-difluoro-benzyl)-5-oxo-2-(4-propionylamino-phenyl)-5,8-dihydro-imidazo[1,2-a]pyrimidine-6-carboxylic acid ethyl ester
   Show/Hide
C34H33F2N5O4
 1
1
IC50 = 10 nM
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CP0257614
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-[3-{(S)-2-[2-(2,6-dimethyl-1-oxy-pyridin-4-yl)-ethylamino]-1-methyl-ethyl}-2-(3,5-dimethyl-phenyl)-1H-indol-5-yl]-2-methyl-propan-1-one
   Show/Hide
C39H50N4O2
 1
1
IC50 = 10 nM
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CP0110348
(S)-1-((S)-2-((S)-2-(2-((S)-2-((S)-2-((S)-2-((S)-3-(1H-imidazol-5-yl)-2-((S)-2-oxopyrrolidine-5-carboxamido)propanamido)-3-(1H-indol-2-yl)propanamido)-3-hydroxypropanamido)-3-(4-hydroxyphenyl)propanamido)acetamido)-4-methylpentanamido)-5-(diaminomethylene
   Show/Hide
C53H72N16O12
 1
1
IC50 = 10 nM
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CP0921767
Trifluoro-acetate2-{2-[7-chloro-6-(4-dimethylamino-phenylcarbamoyl)-3-(3,5-dimethyl-phenyl)-2-oxo-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C35H38ClF3N4O5
 2
1
IC50 = 10.9 nM
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2
IC50 = 360 nM
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CP0219557
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-2-[2-(6-methoxy-pyridin-3-yl)-ethylamino]-1-methyl-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
   Show/Hide
C38H48N4O2
 1
1
IC50 = 11 nM
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CP0221205
4-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-pyridine-2-carbonitrile
   Show/Hide
C38H45N5O
 1
1
IC50 = 11 nM
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CP0043368
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid diethylamide
   Show/Hide
C32H40N4O
 1
1
IC50 = 12 nM
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CP0463978
2-[3-{(S)-2-[2-(2-Acetyl-pyridin-4-yl)-ethylamino]-1-methyl-ethyl}-2-(3,5-dimethyl-phenyl)-1H-indol-5-yl]-1-(2-aza-bicyclo[2.2.2]oct-2-yl)-2-methyl-propan-1-one
   Show/Hide
C39H48N4O2
 1
1
IC50 = 12 nM
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CP0196182
1-(3-Aza-bicyclo[3.2.2]non-3-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
   Show/Hide
C40H52N4O
 1
1
IC50 = 13 nM
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CP0219252
2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-N,N-diisobutyl-isobutyramide
   Show/Hide
C40H56N4O
 1
1
IC50 = 14 nM
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CP0291132
1-(7-Aza-bicyclo[2.2.1]hept-7-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
   Show/Hide
C37H46N4O
 1
1
IC50 = 14 nM
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CP0847905
Trifluoro-acetate2-{2-[7-chloro-6-(2-cyclopropyl-pyrimidin-4-ylcarbamoyl)-3-(3,5-dimethyl-phenyl)-2-oxo-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C34H35ClF3N5O5
 2
1
IC50 = 15 nM
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2
IC50 = 250 nM
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CP0299802
2-{2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-1-(2,5-dimethyl-pyrrolidin-1-yl)-2-methyl-propan-1-one
   Show/Hide
C37H48N4O
 1
1
IC50 = 15 nM
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CP0332602
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid cyclooctyl-ethyl-amide
   Show/Hide
C38H50N4O
 1
1
IC50 = 15 nM
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CP0309400
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid cyclohexyl-ethyl-amide
   Show/Hide
C36H46N4O
 1
1
IC50 = 16 nM
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CP0236982
1-(7-Aza-bicyclo[2.2.1]hept-7-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
   Show/Hide
C37H46N4O
 1
1
IC50 = 18 nM
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CP0255311
1-(7-Aza-bicyclo[2.2.1]hept-7-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{2-[methyl-(4-pyridin-4-yl-butyl)-amino]-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
   Show/Hide
C38H48N4O
 1
1
IC50 = 18 nM
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CP0055695
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-2-[2-(2-ethyl-pyridin-4-yl)-ethylamino]-1-methyl-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
   Show/Hide
C39H50N4O
 1
1
IC50 = 19 nM
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CP0460098
2-(4-Benzoylamino-phenyl)-3-[(benzyl-methyl-amino)-methyl]-8-(2,6-difluoro-benzyl)-5-oxo-5,8-dihydro-imidazo[1,2-a]pyrimidine-6-carboxylic acid ethyl ester
   Show/Hide
C38H33F2N5O4
 1
1
IC50 = 20 nM
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CP0215042
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-[2-(3,5-dimethyl-phenyl)-3-((S)-2-{2-[2-(1-hydroxy-ethyl)-pyridin-4-yl]-ethylamino}-1-methyl-ethyl)-1H-indol-5-yl]-2-methyl-propan-1-one
   Show/Hide
C39H50N4O2
 1
1
IC50 = 20 nM
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CP0401406
N-[4-[5-[[benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-3-(3-methoxyphenyl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-N-methylpropanamide
   Show/Hide
C39H36F2N4O4S
 1
1
IC50 = 20 nM
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CP0508595
5-[(Benzyl-methyl-amino)-methyl]-1-(2,6-difluoro-benzyl)-3-(3-methoxy-phenyl)-6-(4-methoxy-phenyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione; HCL.0.8H2O
   Show/Hide
C36H31F2N3O4S
 1
1
IC50 = 20 nM
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CP0534533
5-[(Benzyl-methyl-amino)-methyl]-1-(2,6-difluoro-benzyl)-3-(3-methoxy-phenyl)-6-(4-nitro-phenyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione; HCL8.H2O
   Show/Hide
C35H28F2N4O5S
 1
1
IC50 = 20 nM
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CP0136681
1-(3,3-Dimethyl-azetidin-1-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
   Show/Hide
C37H48N4O
 1
1
IC50 = 21 nM
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CP0868282
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-2-oxo-6-([1,3,4]thiadiazol-2-ylcarbamoyl)-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C29H29ClF3N5O5S
 2
1
IC50 = 22 nM
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2
IC50 = 32 nM
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CP0190899
2-{2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indol-5-yl}-N,N-diisobutyl-isobutyramide
   Show/Hide
C39H54N4O
 1
1
IC50 = 22 nM
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CP0288623
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid cyclohexyl-ethyl-amide
   Show/Hide
C36H46N4O
 1
1
IC50 = 22 nM
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CP0299579
Acetic acid 4-(2-{(S)-2-[5-[2-(2-aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-pyridin-2-ylmethyl ester
   Show/Hide
C40H50N4O3
 1
1
IC50 = 22 nM
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CP0874971
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-6-(3-methyl-isoxazol-5-ylcarbamoyl)-2-oxo-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C31H32ClF3N4O6
 1
1
IC50 = 23 nM
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CP0115024
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-2-[2-(2,6-dimethyl-pyridin-4-yl)-ethylamino]-1-methyl-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
   Show/Hide
C39H50N4O
 1
1
IC50 = 24 nM
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CP0082419
4-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-pyridine-2-carboxylic acid methyl ester
   Show/Hide
C39H48N4O3
 1
1
IC50 = 25 nM
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CP0215181
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-1-methyl-2-[2-(3-methyl-1-oxy-pyridin-4-yl)-ethylamino]-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
   Show/Hide
C38H48N4O2
 1
1
IC50 = 26 nM
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CP0917751
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-6-(5-methyl-[1,3,4]thiadiazol-2-ylcarbamoyl)-2-oxo-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C30H31ClF3N5O5S
 1
1
IC50 = 28 nM
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CP0535333
3-[(Benzyl-methyl-amino)-methyl]-2-(4-butyrylamino-phenyl)-8-(2,6-difluoro-benzyl)-5-oxo-5,8-dihydro-imidazo[1,2-a]pyrimidine-6-carboxylic acid ethyl ester
   Show/Hide
C35H35F2N5O4
 1
1
IC50 = 30 nM
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CP0464281
ethyl 7-benzyl-3-[[benzyl(methyl)amino]methyl]-4-oxo-2-[4-(phenylcarbamoylamino)phenyl]thieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C39H36N4O4S
 1
1
IC50 = 30 nM
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CP0501953
ethyl 3-[[benzyl(methyl)amino]methyl]-7-[(2-fluorophenyl)methyl]-2-(4-methoxyphenyl)-4-oxothieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C33H31FN2O4S
 1
1
IC50 = 30 nM
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CP0531940
5-[(Benzyl-methyl-amino)-methyl]-1-(2,6-difluoro-benzyl)-3,6-bis-(4-methoxy-phenyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione; HCL.0.0.5H2O
   Show/Hide
C36H31F2N3O4S
 1
1
IC50 = 30 nM
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CP0149717
2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-1-(dodecahydro-carbazol-9-yl)-2-methyl-propan-1-one
   Show/Hide
C44H58N4O
 1
1
IC50 = 31 nM
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CP0850063
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-2-oxo-6-(pyridin-3-ylcarbamoyl)-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C32H32ClF3N4O5
 2
1
IC50 = 32 nM
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2
IC50 = 130 nM
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CP0150494
1-(7-Aza-bicyclo[2.2.1]hept-7-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-butan-1-one
   Show/Hide
C38H48N4O
 1
1
IC50 = 38 nM
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   TS
CP0331985
2-{2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-1-piperidin-1-yl-propan-1-one
   Show/Hide
C36H46N4O
 1
1
IC50 = 38 nM
   TI
   LI
   LO
   TS
CP0223103
2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-1-(4,4-dimethyl-piperidin-1-yl)-2-methyl-propan-1-one
   Show/Hide
C39H52N4O
 1
1
IC50 = 39 nM
   TI
   LI
   LO
   TS
CP0880605
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-6-(2,6-dimethyl-pyrimidin-4-ylcarbamoyl)-2-oxo-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C33H35ClF3N5O5
 2
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
2
IC50 = 486 nM
   TI
   LI
   LO
   TS
CP0310600
1-(7-Aza-bicyclo[2.2.1]hept-7-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-ethyl-butan-1-one
   Show/Hide
C39H50N4O
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0439642
ethyl 2-(4-aminophenyl)-7-benzyl-3-[[benzyl(methyl)amino]methyl]-4-oxothieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C32H31N3O3S
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0853700
Trifluoro-acetate2-{2-[7-chloro-6-(di-sec-butyl-carbamoyl)-3-(3,5-dimethyl-phenyl)-2-oxo-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C35H45ClF3N3O5
 1
1
IC50 = 45 nM
   TI
   LI
   LO
   TS
CP0172193
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-1-methyl-2-[2-(3-methyl-pyridin-4-yl)-ethylamino]-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
   Show/Hide
C38H48N4O
 1
1
IC50 = 48 nM
   TI
   LI
   LO
   TS
CP0384674
5-[(Benzyl-methyl-amino)-methyl]-1-(2,6-difluoro-benzyl)-6-(4-methoxy-phenyl)-3-phenyl-1H-thieno[2,3-d]pyrimidine-2,4-dione; HCL.0.5H2O
   Show/Hide
C35H29F2N3O3S
 1
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0290421
N-cyclohexyl-2-[2-(3,5-dimethylphenyl)-3-[2-(4-pyridin-4-ylbutylamino)ethyl]-1H-indol-5-yl]-N-ethyl-2-methylpropanamide
   Show/Hide
C39H52N4O
 1
1
IC50 = 54 nM
   TI
   LI
   LO
   TS
CP0155115
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-2-[2-(2-methoxymethyl-pyridin-4-yl)-ethylamino]-1-methyl-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
   Show/Hide
C39H50N4O2
 1
1
IC50 = 55 nM
   TI
   LI
   LO
   TS
CP0214051
2-{2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-N,N-diethyl-isobutyramide
   Show/Hide
C35H46N4O
 1
1
IC50 = 58 nM
   TI
   LI
   LO
   TS
CP0352069
2-(3,5-Dimethyl-phenyl)-3-{2-[methyl-(4-pyridin-4-yl-butyl)-amino]-ethyl}-1H-indole-5-carboxylic acid diethylamide
   Show/Hide
C33H42N4O
 1
1
IC50 = 58 nM
   TI
   LI
   LO
   TS
CP0138177
2-{2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-1-morpholin-4-yl-propan-1-one
   Show/Hide
C35H44N4O2
 1
1
IC50 = 59 nM
   TI
   LI
   LO
   TS
CP0369348
2-{2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-1-pyrrolidin-1-yl-propan-1-one
   Show/Hide
C35H44N4O
 1
1
IC50 = 61 nM
   TI
   LI
   LO
   TS
CP0207774
1-(3,3-Dimethyl-azetidin-1-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
   Show/Hide
C36H46N4O
 1
1
IC50 = 62 nM
   TI
   LI
   LO
   TS
CP0286926
[2-(3,5-dimethylphenyl)-3-[2-(4-pyridin-3-ylbutylamino)ethyl]-1H-indol-5-yl]-(2,5-dimethylpyrrolidin-1-yl)methanone
   Show/Hide
C34H42N4O
 1
1
IC50 = 62 nM
   TI
   LI
   LO
   TS
CP0193348
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-1-methyl-2-[2-(2-propyl-pyridin-4-yl)-ethylamino]-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
   Show/Hide
C40H52N4O
 1
1
IC50 = 62 nM
   TI
   LI
   LO
   TS
CP0225806
2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-1-(3aR,7aS)-octahydro-isoindol-2-yl-propan-1-one
   Show/Hide
C40H52N4O
 1
1
IC50 = 66 nM
   TI
   LI
   LO
   TS
CP0246348
2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-1-(1,4-dioxa-8-aza-spiro[4.5]dec-8-yl)-2-methyl-propan-1-one
   Show/Hide
C39H50N4O3
 1
1
IC50 = 66 nM
   TI
   LI
   LO
   TS
CP0182886
3-[(Benzyl-methyl-amino)-methyl]-7-(2-methoxy-benzyl)-2-(4-methoxy-phenyl)-4-oxo-4,7-dihydro-thieno[2,3-b]pyridine-5-carboxylic acid ethyl ester
   Show/Hide
C34H34N2O5S
 1
1
IC50 = 70 nM
   TI
   LI
   LO
   TS
CP0054992
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid diisobutylamide
   Show/Hide
C36H48N4O
 1
1
IC50 = 80 nM
   TI
   LI
   LO
   TS
CP0453601
5-[(Benzyl-methyl-amino)-methyl]-3-(2-chloro-phenyl)-1-(2,6-difluoro-benzyl)-6-(4-methoxy-phenyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione; HCL.0.5H2O
   Show/Hide
C35H28ClF2N3O3S
 1
1
IC50 = 80 nM
   TI
   LI
   LO
   TS
CP0299531
3-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-1-methyl-1H-pyridin-2-one
   Show/Hide
C38H48N4O2
 1
1
IC50 = 82 nM
   TI
   LI
   LO
   TS
CP0252860
1-(7-Aza-bicyclo[2.2.1]hept-7-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{2-[ethyl-(4-pyridin-4-yl-butyl)-amino]-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
   Show/Hide
C39H50N4O
 1
1
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0297942
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid bis-(2,2,2-trifluoro-ethyl)-amide
   Show/Hide
C32H34F6N4O
 1
1
IC50 = 91 nM
   TI
   LI
   LO
   TS
CP0524086
1-(8-Aza-spiro[4.5]dec-8-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
   Show/Hide
C41H54N4O
 1
1
IC50 = 93 nM
   TI
   LI
   LO
   TS
CP0184382
2-{2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indol-5-yl}-N,N-diethyl-isobutyramide
   Show/Hide
C35H46N4O
 1
1
IC50 = 94 nM
   TI
   LI
   LO
   TS
CP0386028
ethyl 3-[[benzyl(methyl)amino]methyl]-7-[(2-cyanophenyl)methyl]-2-(4-methoxyphenyl)-4-oxothieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C34H31N3O4S
 1
1
IC50 = 100 nM
   TI
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   TS
CP0551304
ethyl 3-[[benzyl(methyl)amino]methyl]-2-(4-methoxyphenyl)-7-[(2-nitrophenyl)methyl]-4-oxothieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C33H31N3O6S
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0194543
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-[2-(3,5-dimethyl-phenyl)-3-((S)-2-{2-[2-(1-hydroxy-1-methyl-ethyl)-pyridin-4-yl]-ethylamino}-1-methyl-ethyl)-1H-indol-5-yl]-2-methyl-propan-1-one
   Show/Hide
C40H52N4O2
 1
1
IC50 = 106 nM
   TI
   LI
   LO
   TS
CP0849296
Trifluoro-acetate2-{2-[6-[(benzo[1,3]dioxol-5-ylmethyl)-carbamoyl]-7-chloro-3-(3,5-dimethyl-phenyl)-2-oxo-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C35H35ClF3N3O7
 2
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
2
IC50 = 591 nM
   TI
   LI
   LO
   TS
CP0368048
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid ethyl-isopropyl-amide
   Show/Hide
C33H42N4O
 1
1
IC50 = 110 nM
   TI
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   LO
   TS
CP0045709
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid diisobutylamide
   Show/Hide
C36H48N4O
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0223421
2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-1-(4-ethanesulfonyl-piperazin-1-yl)-2-methyl-propan-1-one
   Show/Hide
C38H51N5O3S
 1
1
IC50 = 124 nM
   TI
   LI
   LO
   TS
CP0163117
(7-Aza-bicyclo[2.2.1]hept-7-yl)-(1-{2-(3,5-dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-cyclobutyl)-methanone
   Show/Hide
C38H46N4O
 1
1
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0916409
Trifluoro-acetate2-{2-[7-chloro-6-diethylcarbamoyl-3-(3,5-dimethyl-phenyl)-2-oxo-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C31H37ClF3N3O5
 1
1
IC50 = 190 nM
   TI
   LI
   LO
   TS
CP0105024
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid diethylamide
   Show/Hide
C32H40N4O
 1
1
IC50 = 190 nM
   TI
   LI
   LO
   TS
CP0244439
1-(7-Aza-bicyclo[2.2.1]hept-7-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{2-[isopropyl-(4-pyridin-4-yl-butyl)-amino]-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
   Show/Hide
C40H52N4O
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0436282
ethyl 3-[[benzyl(methyl)amino]methyl]-7-[(2-methoxyphenyl)methyl]-4-oxo-2-phenylthieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C33H32N2O4S
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0500544
ethyl 7-benzyl-3-[[benzyl(methyl)amino]methyl]-2-(4-methoxyphenyl)-4-oxothieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C33H32N2O4S
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0384670
5-[(Benzyl-methyl-amino)-methyl]-3-(3-chloro-phenyl)-1-(2,6-difluoro-benzyl)-6-(4-methoxy-phenyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione; HCL.H2O
   Show/Hide
C35H28ClF2N3O3S
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0405427
5-[(Benzyl-methyl-amino)-methyl]-1-(2,6-difluoro-benzyl)-3-(2-methoxy-phenyl)-6-(4-methoxy-phenyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione; HCL.1.5H2O
   Show/Hide
C36H31F2N3O4S
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0531947
5-[(Benzyl-methyl-amino)-methyl]-3-(4-chloro-phenyl)-1-(2,6-difluoro-benzyl)-6-(4-methoxy-phenyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione; HCL.H2O
   Show/Hide
C35H28ClF2N3O3S
 1
1
IC50 = 200 nM
   TI
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   LO
   TS
CP0196914
4-(2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propionyl)-piperazine-1-carboxylic acid tert-butyl ester
   Show/Hide
C41H55N5O3
 1
1
IC50 = 220 nM
   TI
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   TS
CP0445880
7-Chloro-4-(2-cyclopentyl-ethoxy)-2-oxo-3-(3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid [1,2,5]thiadiazol-3-ylamide
   Show/Hide
C28H29ClN4O3S
 2
1
IC50 = 243 nM
   TI
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   TS
2
IC50 = 1150 nM
   TI
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   TS
CP0041665
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid ethyl-(2-hydroxy-ethyl)-amide
   Show/Hide
C32H40N4O2
 1
1
IC50 = 260 nM
   TI
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   TS
CP0214050
(7-Aza-bicyclo[2.2.1]hept-7-yl)-{2-(3,5-dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-methanone
   Show/Hide
C34H40N4O
 1
1
IC50 = 260 nM
   TI
   LI
   LO
   TS
CP0847491
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-2-oxo-6-(pyrimidin-2-ylcarbamoyl)-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C31H31ClF3N5O5
 2
1
IC50 = 290 nM
   TI
   LI
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   TS
2
IC50 > 3200 nM
   TI
   LI
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   TS
CP0300561
1-(7-Aza-bicyclo[2.2.1]hept-7-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{2-[isobutyl-(4-pyridin-4-yl-butyl)-amino]-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
   Show/Hide
C41H54N4O
 1
1
IC50 = 300 nM
   TI
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   LO
   TS
CP0449533
ethyl 3-[[benzyl(methyl)amino]methyl]-2-(4-methoxyphenyl)-7-[(4-methoxyphenyl)methyl]-4-oxothieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C34H34N2O5S
 1
1
IC50 = 300 nM
   TI
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   TS
CP0485573
ethyl 3-[[benzyl(methyl)amino]methyl]-7-[(3-fluorophenyl)methyl]-2-(4-methoxyphenyl)-4-oxothieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C33H31FN2O4S
 1
1
IC50 = 300 nM
   TI
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   TS
CP0551305
ethyl 3-[[benzyl(ethyl)amino]methyl]-2-(4-methoxyphenyl)-7-[(2-methoxyphenyl)methyl]-4-oxothieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C35H36N2O5S
 1
1
IC50 = 300 nM
   TI
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   TS
CP0373317
ethyl 3-[[benzyl-[2-[[1-[2-[2-[2-[2-[2-[4-[[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]methyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]methylamino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
   Show/Hide
C86H94F4N20O14
 2
1
IC50 = 309.03 nM
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2
Ki = 194.98 nM
   TI
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CP0847053
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-2-oxo-6-(4H-[1,2,4]triazol-3-ylcarbamoyl)-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C29H30ClF3N6O5
 2
1
IC50 = 320 nM
   TI
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2
IC50 = 775 nM
   TI
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   TS
CP0376521
2-{2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indol-5-yl}-isobutyramide
   Show/Hide
C31H38N4O
 1
1
IC50 = 350 nM
   TI
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   TS
CP0535910
ethyl 3-[[benzyl(methyl)amino]methyl]-2-[4-[[1-[2-[2-[2-[2-[4-[[[4-[3-[[benzyl(methyl)amino]methyl]-8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-5-oxoimidazo[1,2-a]pyrimidin-2-yl]phenyl]carbamoylamino]methyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]methylcarbamoylamino]phenyl]-8-[(2,6-difluorophenyl)methyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
   Show/Hide
C78H80F4N18O11
 2
1
IC50 = 354.81 nM
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   TS
2
Ki = 29.51 nM
   TI
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   TS
CP0363826
4-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-pyridine-2-carboxylic acid
   Show/Hide
C38H46N4O3
 1
1
IC50 = 371 nM
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   TS
CP0464282
ethyl 3-[[benzyl(methyl)amino]methyl]-7-[(4-fluorophenyl)methyl]-2-(4-methoxyphenyl)-4-oxothieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C33H31FN2O4S
 1
1
IC50 = 400 nM
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CP0529753
ethyl 3-[[benzyl(methyl)amino]methyl]-2-(4-methoxyphenyl)-7-[(3-methoxyphenyl)methyl]-4-oxothieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C34H34N2O5S
 1
1
IC50 = 400 nM
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CP0461051
3-Benzyl-5-[(benzyl-methyl-amino)-methyl]-1-(2,6-difluoro-benzyl)-6-(4-methoxy-phenyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione; HCL.0.5H2O
   Show/Hide
C36H31F2N3O3S
 1
1
IC50 = 400 nM
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CP0522471
5-[(Benzyl-methyl-amino)-methyl]-1-(2,6-difluoro-benzyl)-3-isobutyl-6-(4-methoxy-phenyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione; HCL
   Show/Hide
C33H33F2N3O3S
 1
1
IC50 = 400 nM
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CP0373316
ethyl 3-[[[2-[[1-[2-[2-(2-azidoethoxy)ethoxy]ethyl]triazol-4-yl]methylamino]-2-oxoethyl]-benzylamino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C44H49F2N13O7
 1
1
IC50 = 467.74 nM
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CP0464285
ethyl 3-[(dimethylamino)methyl]-2-(4-methoxyphenyl)-7-[(2-methoxyphenyl)methyl]-4-oxothieno[2,3-b]pyridine-5-carboxylate
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C28H30N2O5S
 1
1
IC50 = 500 nM
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CP0486699
ethyl 7-benzyl-3-[[benzyl(methyl)amino]methyl]-2-(3-methoxyphenyl)-4-oxothieno[2,3-b]pyridine-5-carboxylate
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C33H32N2O4S
 1
1
IC50 = 500 nM
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CP0374809
ethyl 3-[[[2-[[1-[2-(2-azidoethoxy)ethyl]triazol-4-yl]methylamino]-2-oxoethyl]-benzylamino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
   Show/Hide
C42H45F2N13O6
 1
1
IC50 = 524.81 nM
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CP0258027
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid bis-(2-methoxy-ethyl)-amide
   Show/Hide
C34H44N4O3
 1
1
IC50 = 610 nM
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CP0435797
ethyl 3-[[benzyl(methyl)amino]methyl]-8-[(2,6-difluorophenyl)methyl]-5-oxo-2-[4-(prop-2-ynylcarbamoylamino)phenyl]imidazo[1,2-a]pyrimidine-6-carboxylate
   Show/Hide
C35H32F2N6O4
 2
1
IC50 = 676.08 nM
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2
Ki = 1.349 nM
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CP0436605
ethyl 2-[4-[[1-[2-[2-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]methylcarbamoylamino]phenyl]-3-[[benzyl(methyl)amino]methyl]-8-[(2,6-difluorophenyl)methyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
   Show/Hide
C45H52F2N12O8
 1
1
IC50 = 676.08 nM
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CP0538123
ethyl 7-benzyl-3-[[benzyl(methyl)amino]methyl]-2-(2-methoxyphenyl)-4-oxothieno[2,3-b]pyridine-5-carboxylate
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C33H32N2O4S
 1
1
IC50 = 700 nM
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CP0439698
5-[(Benzyl-methyl-amino)-methyl]-3-cyclohexyl-1-(2,6-difluoro-benzyl)-6-(4-methoxy-phenyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione; HCL.0.5H2O
   Show/Hide
C35H35F2N3O3S
 1
1
IC50 = 700 nM
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CP0373318
ethyl 3-[[[2-[[1-[2-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]ethyl]triazol-4-yl]methylamino]-2-oxoethyl]-benzylamino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
   Show/Hide
C46H53F2N13O8
 1
1
IC50 = 724.44 nM
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CP0445447
ethyl 3-[[[2-[[1-(2-azidoethyl)triazol-4-yl]methylamino]-2-oxoethyl]-benzylamino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
   Show/Hide
C40H41F2N13O5
 1
1
IC50 = 724.44 nM
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CP0373315
ethyl 3-[[benzyl-[2-[[1-[2-[2-[2-[4-[[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]methyl]triazol-1-yl]ethoxy]ethoxy]ethyl]triazol-4-yl]methylamino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
   Show/Hide
C82H86F4N20O12
 2
1
IC50 = 831.76 nM
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2
Ki = 58.88 nM
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CP0509408
ethyl 3-[[[2-[[1-[2-[2-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]methylamino]-2-oxoethyl]-benzylamino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
   Show/Hide
C48H57F2N13O9
 1
1
IC50 = 831.76 nM
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CP0874996
Trifluoro-acetate2-{2-[7-chloro-3-(3,5-dimethyl-phenyl)-6-(2-ethyl-2H-pyrazol-3-ylcarbamoyl)-2-oxo-1,2-dihydro-quinolin-4-yloxy]-ethyl}-piperidinium
   Show/Hide
C32H35ClF3N5O5
 2
1
IC50 = 860 nM
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2
IC50 = 977 nM
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CP0530448
ethyl 3-[[benzyl(methyl)amino]methyl]-2-[4-[[1-[2-[2-[2-[4-[[[4-[3-[[benzyl(methyl)amino]methyl]-8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-5-oxoimidazo[1,2-a]pyrimidin-2-yl]phenyl]carbamoylamino]methyl]triazol-1-yl]ethoxy]ethoxy]ethyl]triazol-4-yl]methylcarbamoylamino]phenyl]-8-[(2,6-difluorophenyl)methyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
   Show/Hide
C76H76F4N18O10
 2
1
IC50 = 954.99 nM
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2
Ki = 23.44 nM
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CP0541694
ethyl 3-[[benzyl-[2-oxo-2-(prop-2-ynylamino)ethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C38H37F2N7O5
 2
1
IC50 = 1000 nM
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2
Ki = 5.248 nM
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CP0256086
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid isopropylamide
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C31H38N4O
 1
1
IC50 = 1200 nM
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CP0405362
ethyl 3-[[benzyl-[2-[[1-[2-[2-[2-[2-[4-[[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]methyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]methylamino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
   Show/Hide
C84H90F4N20O13
 2
1
IC50 = 1318.26 nM
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2
Ki = 69.18 nM
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CP0435279
ethyl 3-[[benzyl(methyl)amino]methyl]-2-[4-[[1-[2-[2-[2-[2-[2-[4-[[[4-[3-[[benzyl(methyl)amino]methyl]-8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-5-oxoimidazo[1,2-a]pyrimidin-2-yl]phenyl]carbamoylamino]methyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]methylcarbamoylamino]phenyl]-8-[(2,6-difluorophenyl)methyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C80H84F4N18O12
 1
1
IC50 = 1348.96 nM
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CP0442969
ethyl 3-[[benzyl-[2-[[1-[2-[2-[4-[[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]methyl]triazol-1-yl]ethoxy]ethyl]triazol-4-yl]methylamino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C80H82F4N20O11
 1
1
IC50 = 1548.82 nM
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CP0435798
ethyl 3-[[benzyl-[2-[[1-[2-[4-[[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]methyl]triazol-1-yl]ethyl]triazol-4-yl]methylamino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
   Show/Hide
C78H78F4N20O10
 1
1
IC50 = 1905.46 nM
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CP0500896
ethyl 3-[[benzyl(methyl)amino]methyl]-2-[4-[[1-[2-[4-[[[4-[3-[[benzyl(methyl)amino]methyl]-8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-5-oxoimidazo[1,2-a]pyrimidin-2-yl]phenyl]carbamoylamino]methyl]triazol-1-yl]ethyl]triazol-4-yl]methylcarbamoylamino]phenyl]-8-[(2,6-difluorophenyl)methyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C72H68F4N18O8
 1
1
IC50 = 1905.46 nM
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CP0076365
7-(2-Methoxy-benzyl)-2-(4-methoxy-phenyl)-3-methylaminomethyl-4-oxo-4,7-dihydro-thieno[2,3-b]pyridine-5-carboxylic acid ethyl ester
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C27H28N2O5S
 1
1
IC50 = 2000 nM
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CP0523763
ethyl 3-[(benzylamino)methyl]-2-(4-methoxyphenyl)-7-[(2-methoxyphenyl)methyl]-4-oxothieno[2,3-b]pyridine-5-carboxylate
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C33H32N2O5S
 1
1
IC50 = 2000 nM
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CP0504053
ethyl 2-[4-[[1-[2-[2-(2-azidoethoxy)ethoxy]ethyl]triazol-4-yl]methylcarbamoylamino]phenyl]-3-[[benzyl(methyl)amino]methyl]-8-[(2,6-difluorophenyl)methyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C41H44F2N12O6
 1
1
IC50 = 2398.83 nM
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CP0464694
ethyl 2-[4-[[1-(2-azidoethyl)triazol-4-yl]methylcarbamoylamino]phenyl]-3-[[benzyl(methyl)amino]methyl]-8-[(2,6-difluorophenyl)methyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C37H36F2N12O4
 1
1
IC50 = 2570.4 nM
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CP0480378
ethyl 2-[4-[[1-[2-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]ethyl]triazol-4-yl]methylcarbamoylamino]phenyl]-3-[[benzyl(methyl)amino]methyl]-8-[(2,6-difluorophenyl)methyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C43H48F2N12O7
 1
1
IC50 = 3019.95 nM
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CP0437227
ethyl 3-[[benzyl(methyl)amino]methyl]-2-[4-[[1-[2-[2-[4-[[[4-[3-[[benzyl(methyl)amino]methyl]-8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-5-oxoimidazo[1,2-a]pyrimidin-2-yl]phenyl]carbamoylamino]methyl]triazol-1-yl]ethoxy]ethyl]triazol-4-yl]methylcarbamoylamino]phenyl]-8-[(2,6-difluorophenyl)methyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
   Show/Hide
C74H72F4N18O9
 1
1
IC50 = 3162.28 nM
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CP0437872
ethyl 2-[4-[[1-[2-(2-azidoethoxy)ethyl]triazol-4-yl]methylcarbamoylamino]phenyl]-3-[[benzyl(methyl)amino]methyl]-8-[(2,6-difluorophenyl)methyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C39H40F2N12O5
 1
1
IC50 = 3630.78 nM
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CP0501954
ethyl 3-[[benzyl(methyl)amino]methyl]-2-(4-methoxyphenyl)-7-methyl-4-oxothieno[2,3-b]pyridine-5-carboxylate
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C27H28N2O4S
 1
1
IC50 = 5000 nM
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CP0542982
ethyl 3-[[acetyl(benzyl)amino]methyl]-2-(4-methoxyphenyl)-7-[(2-methoxyphenyl)methyl]-4-oxothieno[2,3-b]pyridine-5-carboxylate
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C35H34N2O6S
 1
1
IC50 = 7000 nM
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CP0435772
3-[[benzyl(methyl)amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxo-N-prop-2-ynylimidazo[1,2-a]pyrimidine-6-carboxamide
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C35H33F2N7O3
 2
1
IC50 = 7079.46 nM
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2
Ki = 162.18 nM
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CP0515771
ethyl 2-(4-methoxyphenyl)-7-[(2-methoxyphenyl)methyl]-3-methyl-4-oxothieno[2,3-b]pyridine-5-carboxylate
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C26H25NO5S
 1
1
IC50 = 10000 nM
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CP0501955
ethyl 3-[[benzyl(methyl)amino]methyl]-2-(4-methoxyphenyl)-4-oxo-7H-thieno[2,3-b]pyridine-5-carboxylate
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C26H26N2O4S
 1
1
IC50 > 20000 nM
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CP0871618
3-{[benzyl(methyl)amino]methyl}-N-{[1-(2-{2-[2-(4-{[(3-{[benzyl(methyl)amino]methyl}-8-[(2,6-difluorophenyl)methyl]-2-{4-[(ethylcarbamoyl)amino]phenyl}-5-oxo-5H,8H-imidazo[1,2-a]pyrimidin-6-yl)formamido]methyl}-1H-1,2,3-triazol-1-yl)ethoxy]ethoxy}ethyl)-1H-1,2,3-triazol-4-yl]methyl}-8-[(2,6-difluorophenyl)methyl]-2-{4-[(methylcarbamoyl)amino]phenyl}-5-oxo-5H,8H-imidazo[1,2-a]pyrimidine-6-carboxamide
   Show/Hide
C75H76F4N20O8
 1
1
IC50 < 10000 nM
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CP0877635
3-{[benzyl(methyl)amino]methyl}-N-({1-[2-(2-{2-[2-(4-{[(3-{[benzyl(methyl)amino]methyl}-8-[(2,6-difluorophenyl)methyl]-2-{4-[(ethylcarbamoyl)amino]phenyl}-5-oxo-5H,8H-imidazo[1,2-a]pyrimidin-6-yl)formamido]methyl}-1H-1,2,3-triazol-1-yl)ethoxy]ethoxy}ethoxy)ethyl]-1H-1,2,3-triazol-4-yl}methyl)-8-[(2,6-difluorophenyl)methyl]-2-{4-[(ethylcarbamoyl)amino]phenyl}-5-oxo-5H,8H-imidazo[1,2-a]pyrimidine-6-carboxamide
   Show/Hide
C78H82F4N20O9
 1
1
IC50 < 10000 nM
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CP0877638
1-(4-(8-(2,6-difluorobenzyl)-6-(((1-(2-(2-azidoethoxy)ethyl)-1H-1,2,3-triazol-4-yl)methyl)carbamoyl)-3-((benzyl(methyl)amino)methyl)-5-oxo-5,8-dihydroimidazo[1,2-a]pyrimidin-2-yl)phenyl)-3-ethylurea
   Show/Hide
C39H41F2N13O4
 1
1
IC50 < 10000 nM
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CP0878009
1-(4-(8-(2,6-difluorobenzyl)-6-(((1-(2-(2-(2-(2-azidoethoxy)ethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)methyl)carbamoyl)-3-((benzyl(methyl)amino)methyl)-5-oxo-5,8-dihydroimidazo[1,2-a]pyrimidin-2-yl)phenyl)-3-ethylurea
   Show/Hide
C43H49F2N13O6
 1
1
IC50 < 10000 nM
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CP0878010
3-{[benzyl(methyl)amino]methyl}-N-({1-[2-(4-{[(3-{[benzyl(methyl)amino]methyl}-8-[(2,6-difluorophenyl)methyl]-2-{4-[(ethylcarbamoyl)amino]phenyl}-5-oxo-5H,8H-imidazo[1,2-a]pyrimidin-6-yl)formamido]methyl}-1H-1,2,3-triazol-1-yl)ethyl]-1H-1,2,3-triazol-4-yl}methyl)-8-[(2,6-difluorophenyl)methyl]-2-{4-[(ethylcarbamoyl)amino]phenyl}-5-oxo-5H,8H-imidazo[1,2-a]pyrimidine-6-carboxamide
   Show/Hide
C72H70F4N20O6
 1
1
IC50 < 10000 nM
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CP0878011
1-(4-(8-(2,6-difluorobenzyl)-6-(((1-(2-(2-(2-(2-(2-azidoethoxy)ethoxy)ethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)methyl)carbamoyl)-3-((benzyl(methyl)amino)methyl)-5-oxo-5,8-dihydroimidazo[1,2-a]pyrimidin-2-yl)phenyl)-3-ethylurea
   Show/Hide
C45H53F2N13O7
 1
1
IC50 < 10000 nM
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CP0883044
1-(4-(8-(2,6-difluorobenzyl)-6-(((1-(2-azidoethyl)-1H-1,2,3-triazol-4-yl)methyl)carbamoyl)-3-((benzyl(methyl)amino)methyl)-5-oxo-5,8-dihydroimidazo[1,2-a]pyrimidin-2-yl)phenyl)-3-ethylurea
   Show/Hide
C37H37F2N13O3
 1
1
IC50 < 10000 nM
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CP0886316
3-{[benzyl(methyl)amino]methyl}-N-[(1-{2-[2-(4-{[(3-{[benzyl(methyl)amino]methyl}-8-[(2,6-difluorophenyl)methyl]-2-{4-[(ethylcarbamoyl)amino]phenyl}-5-oxo-5H,8H-imidazo[1,2-a]pyrimidin-6-yl)formamido]methyl}-1H-1,2,3-triazol-1-yl)ethoxy]ethyl}-1H-1,2,3-triazol-4-yl)methyl]-8-[(2,6-difluorophenyl)methyl]-2-{4-[(ethylcarbamoyl)amino]phenyl}-5-oxo-5H,8H-imidazo[1,2-a]pyrimidine-6-carboxamide
   Show/Hide
C74H74F4N20O7
 1
1
IC50 < 10000 nM
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CP0886560
3-{[benzyl(methyl)amino]methyl}-N-({1-[14-(4-{[(3-{[benzyl(methyl)amino]methyl}-8-[(2,6-difluorophenyl)methyl]-2-{4-[(ethylcarbamoyl)amino]phenyl}-5-oxo-5H,8H-imidazo[1,2-a]pyrimidin-6-yl)formamido]methyl}-1H-1,2,3-triazol-1-yl)-3,6,9,12-tetraoxatetradecan-1-yl]-1H-1,2,3-triazol-4-yl}methyl)-8-[(2,6-difluorophenyl)methyl]-2-{4-[(ethylcarbamoyl)amino]phenyl}-5-oxo-5H,8H-imidazo[1,2-a]pyrimidine-6-carboxamide
   Show/Hide
C80H86F4N20O10
 1
1
IC50 < 10000 nM
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CP0941391
1-(4-(8-(2,6-difluorobenzyl)-6-(((1-(2-(2-(2-azidoethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)methyl)carbamoyl)-3-((benzyl(methyl)amino)methyl)-5-oxo-5,8-dihydroimidazo[1,2-a]pyrimidin-2-yl)phenyl)-3-ethylurea
   Show/Hide
C41H45F2N13O5
 1
1
IC50 < 10000 nM
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CP0403789
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(3-chloro-4-fluorophenyl)ethyl]-8-[(3R,4S,6R)-4-[cyclopropylmethyl(methyl)amino]-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] (4S)-4-methyl-2-oxo-1,3-oxazolidine-3-carboxylate
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C47H69ClFN3O13
 1
1
Ki = 0.3311 nM
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CP0480685
(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-8-[(3R,4S,6R)-4-[bis(cyclopropylmethyl)amino]-3-hydroxy-6-methyloxan-2-yl]oxy-15-[2-(3-chloro-4-fluorophenyl)ethyl]-2-ethyl-6-[(4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,12,16-trione
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C53H82ClFN2O13
 1
1
Ki = 0.8511 nM
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CP0533022
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-8-[(3R,4S,6R)-4-[bis(cyclopropylmethyl)amino]-3-hydroxy-6-methyloxan-2-yl]oxy-15-[2-(3,4-dichlorophenyl)ethyl]-2-ethyl-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] (4S)-4-methyl-2-oxo-1,3-oxazolidine-3-carboxylate
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C50H73Cl2N3O13
 1
1
Ki = 1.288 nM
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CP0522002
(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-8-[(3R,4S,6R)-4-[cyclopentyl(methyl)amino]-3-hydroxy-6-methyloxan-2-yl]oxy-15-[2-(3,4-dichlorophenyl)ethyl]-2-ethyl-6-[(4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,12,16-trione
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C51H80Cl2N2O13
 1
1
Ki = 1.514 nM
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CP0211775
A-198401
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C47H69Cl2N3O13
 1
1
Ki = 1.862 nM
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CP0403723
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-8-[(3R,4S,6R)-4-[cyclopentyl(methyl)amino]-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] (4S)-4-methyl-2-oxo-1,3-oxazolidine-3-carboxylate
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C48H72ClN3O13
 2
1
Ki = 3.89 nM
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2
Ki = 38.02 nM
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CP0453836
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-8-[(3R,4S,6R)-4-[cyclopentyl(methyl)amino]-3-hydroxy-6-methyloxan-2-yl]oxy-15-[2-(3,4-dichlorophenyl)ethyl]-2-ethyl-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] (4S)-4-methyl-2-oxo-1,3-oxazolidine-3-carboxylate
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C48H71Cl2N3O13
 1
1
Ki = 5.623 nM
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CP0375492
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-8-[(3R,4S,6R)-4-[cyclohexyl(methyl)amino]-3-hydroxy-6-methyloxan-2-yl]oxy-15-[2-(3,4-dichlorophenyl)ethyl]-2-ethyl-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] (4S)-4-methyl-2-oxo-1,3-oxazolidine-3-carboxylate
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C49H73Cl2N3O13
 1
1
Ki = 7.244 nM
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CP0514478
(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-8-[(3R,4S,6R)-4-[cyclopentyl(methyl)amino]-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-6-[(4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,12,16-trione
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C51H81ClN2O13
 1
1
Ki = 7.586 nM
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CP0520257
(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-8-[(3R,4S,6R)-4-[cyclopropylmethyl(methyl)amino]-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-6-[(4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,12,16-trione
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C50H79ClN2O13
 1
1
Ki = 13.18 nM
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CP0374667
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(3,4-dichlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] (4S)-4-methyl-2-oxo-1,3-oxazolidine-3-carboxylate
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C46H69Cl2N3O13
 1
1
Ki = 15.14 nM
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CP0430480
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-8-[(3R,4S,6R)-4-[cyclopropylmethyl(methyl)amino]-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] (4S)-4-methyl-2-oxo-1,3-oxazolidine-3-carboxylate
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C47H70ClN3O13
 1
1
Ki = 18.62 nM
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CP0448714
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] (4S)-4-methyl-2-oxo-1,3-oxazolidine-3-carboxylate
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C46H70ClN3O13
 1
1
Ki = 18.62 nM
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CP0394212
(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-6-[(4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,12,16-trione
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C49H79ClN2O13
 1
1
Ki = 22.39 nM
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CP0410101
(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-8-[(3R,4S,6R)-4-[butan-2-yl(cyclopropylmethyl)amino]-3-hydroxy-6-methyloxan-2-yl]oxy-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-6-[(4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,12,16-trione
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C53H85ClN2O13
 1
1
Ki = 27.54 nM
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CP0445667
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] 5-methyl-2-oxo-1,3-oxazolidine-3-carboxylate
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C46H70ClN3O13
 1
1
Ki = 36.31 nM
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CP0430277
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] (4R)-4-methyl-2-oxo-1,3-oxazolidine-3-carboxylate
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C46H70ClN3O13
 1
1
Ki = 48.98 nM
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CP0511367
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] (4S)-4-ethyl-2-oxo-1,3-oxazolidine-3-carboxylate
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C47H72ClN3O13
 1
1
Ki = 66.07 nM
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CP0381079
(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-6-[(4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-(methylamino)oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,12,16-trione
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C46H73ClN2O13
 1
1
Ki = 79.43 nM
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CP0381021
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] 4,4-dimethyl-2-oxo-1,3-oxazolidine-3-carboxylate
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C47H72ClN3O13
 1
1
Ki = 79.43 nM
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CP0502052
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] (4S,5R)-4,5-dimethyl-2-oxo-1,3-oxazolidine-3-carboxylate
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C47H72ClN3O13
 1
1
Ki < 100 nM
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CP0504856
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] 2-oxo-1,3-oxazolidine-3-carboxylate
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C45H68ClN3O13
 1
1
Ki = 114.82 nM
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CP0436307
ethyl 3-[[benzyl-[2-oxo-2-[4-(3-phenylprop-2-ynylcarbamoyl)piperidin-1-yl]ethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C50H50F2N8O6
 1
1
Ki = 140 nM
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CP0427984
ethyl 3-[[benzyl-[2-oxo-2-[[2-oxo-2-(3-phenylprop-2-ynylamino)ethyl]amino]ethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C46H44F2N8O6
 1
1
Ki = 170 nM
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CP0438999
(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-8-[(3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-6-[(4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,12,16-trione
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C47H75ClN2O13
 1
1
Ki = 190.55 nM
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CP0507096
(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-8-[(3R,4S,6R)-4-[cyclohexyl(methyl)amino]-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-6-[(4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,12,16-trione
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C52H83ClN2O13
 1
1
Ki = 204.17 nM
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CP0448712
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] oxolane-3-carboxylate
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C46H71ClN2O12
 1
1
Ki = 213.8 nM
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CP0436306
ethyl 3-[[benzyl-[2-oxo-2-[(2S)-2-(3-phenylprop-2-ynylcarbamoyl)pyrrolidin-1-yl]ethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C49H48F2N8O6
 1
1
Ki = 260 nM
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CP0403913
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] (4R)-4-(2-methylpropyl)-2-oxo-1,3-oxazolidine-3-carboxylate
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C49H76ClN3O13
 1
1
Ki = 275.42 nM
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CP0436308
ethyl 3-[[benzyl-[2-oxo-2-[[6-oxo-6-(3-phenylprop-2-ynylamino)hexyl]amino]ethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C50H52F2N8O6
 1
1
Ki = 380 nM
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CP0507827
ethyl 3-[[benzyl-[2-[4-[3-[3-[3-[[1-[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]piperidine-4-carbonyl]amino]prop-1-ynyl]phenyl]prop-2-ynylcarbamoyl]piperidin-1-yl]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C94H94F4N16O12
 1
1
Ki = 400 nM
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CP0436303
ethyl 3-[[benzyl-[2-[[(2S)-1-[3-[4-[3-[[(2S)-2-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]propanoyl]amino]prop-1-ynyl]phenyl]prop-2-ynylamino]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C88H86F4N16O12
 1
1
Ki = 480 nM
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CP0507828
ethyl 3-[[benzyl-[2-[4-[3-[2-[3-[[1-[2-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]acetyl]piperidine-4-carbonyl]amino]prop-1-ynyl]phenyl]prop-2-ynylcarbamoyl]piperidin-1-yl]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C93H93F4N17O11
 1
1
Ki = 500 nM
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CP0449200
ethyl 3-[[benzyl-[2-[4-[3-[4-[3-[[1-[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]piperidine-4-carbonyl]amino]prop-1-ynyl]phenyl]prop-2-ynylcarbamoyl]piperidin-1-yl]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C94H94F4N16O12
 1
1
Ki = 510 nM
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CP0433399
ethyl 3-[[benzyl-[2-[[2-[3-[4-[3-[[2-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]acetyl]amino]prop-1-ynyl]phenyl]prop-2-ynylamino]-2-oxoethyl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C86H82F4N16O12
 1
1
Ki = 530 nM
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CP0508616
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] 5-ethyl-2-oxo-1,3-oxazolidine-3-carboxylate
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C47H72ClN3O13
 1
1
Ki = 562.34 nM
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CP0436309
ethyl 3-[[benzyl-[2-oxo-2-[[4-oxo-4-(3-phenylprop-2-ynylamino)butyl]amino]ethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C48H48F2N8O6
 1
1
Ki = 580 nM
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CP0444487
ethyl 3-[[benzyl-[2-[[4-[3-[4-[3-[4-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]butanoylamino]prop-1-ynyl]phenyl]prop-2-ynylamino]-4-oxobutyl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C90H90F4N16O12
 1
1
Ki = 600 nM
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CP0436310
ethyl 3-[[benzyl-[2-[[6-[3-[4-[3-[6-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]hexanoylamino]prop-1-ynyl]phenyl]prop-2-ynylamino]-6-oxohexyl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C94H98F4N16O12
 1
1
Ki = 620 nM
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CP0391374
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] cyclopentanecarboxylate
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C47H73ClN2O11
 1
1
Ki = 630.96 nM
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CP0507830
ethyl 3-[[benzyl-[2-[[6-[3-[2-[3-[6-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]hexanoylamino]prop-1-ynyl]phenyl]prop-2-ynylamino]-6-oxohexyl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C91H94F4N16O10
 1
1
Ki = 700 nM
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CP0386687
ethyl 3-[[benzyl-[2-[[(2S)-1-[3-[4-[3-[[(2S)-2-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]-3-methylbutanoyl]amino]prop-1-ynyl]phenyl]prop-2-ynylamino]-3-methyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C92H94F4N16O12
 1
1
Ki = 720 nM
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CP0427978
ethyl 3-[[benzyl-[2-[(2S)-2-[3-[4-[3-[[(2S)-1-[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]prop-1-ynyl]phenyl]prop-2-ynylcarbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C92H90F4N16O12
 1
1
Ki = 740 nM
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CP0490573
ethyl 3-[[benzyl-[2-[[(2S)-3-methyl-1-oxo-1-(3-phenylprop-2-ynylamino)butan-2-yl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C49H50F2N8O6
 1
1
Ki = 770 nM
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CP0375305
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] 2-methyl-1,3-oxazolidine-3-carboxylate
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C46H72ClN3O12
 1
1
Ki = 794.33 nM
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CP0427979
ethyl 3-[[benzyl-[2-[[4-[3-[3-[3-[4-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]butanoylamino]prop-1-ynyl]phenyl]prop-2-ynylamino]-4-oxobutyl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C90H90F4N16O12
 1
1
Ki = 820 nM
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CP0449135
ethyl 3-[[benzyl-[2-[[4-[3-[2-[3-[4-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]butanoylamino]prop-1-ynyl]phenyl]prop-2-ynylamino]-4-oxobutyl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C87H86F4N16O10
 1
1
Ki = 840 nM
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CP0436304
ethyl 3-[[benzyl-[2-[[2-[(2S)-2-[3-[2-[3-[[(2S)-1-[2-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]prop-1-ynyl]phenyl]prop-2-ynylcarbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C93H92F4N18O12
 1
1
Ki = 850 nM
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CP0427987
ethyl 3-[[benzyl-[2-[[6-[3-[3-[3-[6-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]hexanoylamino]prop-1-ynyl]phenyl]prop-2-ynylamino]-6-oxohexyl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C94H98F4N16O12
 1
1
Ki = 930 nM
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CP0436311
ethyl 3-[[benzyl-[2-[(2S)-2-[3-[3-[3-[[(2S)-1-[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]prop-1-ynyl]phenyl]prop-2-ynylcarbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C92H90F4N16O12
 1
1
Ki = 930 nM
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CP0427988
ethyl 3-[[benzyl-[2-[[2-[3-[2-[3-[[2-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]acetyl]amino]prop-1-ynyl]phenyl]prop-2-ynylamino]-2-oxoethyl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C83H78F4N16O10
 1
1
Ki = 1000 nM
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CP0433400
ethyl 3-[[benzyl-[2-[[2-[3-[3-[3-[[2-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]acetyl]amino]prop-1-ynyl]phenyl]prop-2-ynylamino]-2-oxoethyl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C86H82F4N16O12
 1
1
Ki = 1100 nM
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CP0427983
ethyl 3-[[benzyl-[2-oxo-2-[[(2S)-1-oxo-1-(3-phenylprop-2-ynylamino)propan-2-yl]amino]ethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C47H46F2N8O6
 1
1
Ki = 1600 nM
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CP0375096
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] pyrrolidine-1-carboxylate
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C46H72ClN3O11
 1
1
Ki = 1621.81 nM
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CP0455132
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] 3-methylbutanoate
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C46H73ClN2O11
 1
1
Ki = 2041.74 nM
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CP0494596
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] 2-oxoimidazolidine-1-carboxylate
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C45H69ClN4O12
 1
1
Ki = 2041.74 nM
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CP0436312
ethyl 3-[[benzyl-[2-[[(2S)-1-[3-[3-[3-[[(2S)-2-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]-3-methylbutanoyl]amino]prop-1-ynyl]phenyl]prop-2-ynylamino]-3-methyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C92H94F4N16O12
 1
1
Ki = 2200 nM
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CP0449136
ethyl 3-[[benzyl-[2-[[2-[[(2S)-1-[3-[2-[3-[[(2S)-2-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]propanoyl]amino]prop-1-ynyl]phenyl]prop-2-ynylamino]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C87H85F4N17O11
 1
1
Ki = 3000 nM
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CP0436305
ethyl 3-[[benzyl-[2-[[2-[[(2S)-1-[3-[2-[3-[[(2S)-2-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]-3-methylbutanoyl]amino]prop-1-ynyl]phenyl]prop-2-ynylamino]-3-methyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C91H93F4N17O11
 1
1
Ki = 3300 nM
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CP0381020
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] 3-methyl-2-oxoimidazolidine-1-carboxylate
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C46H71ClN4O12
 1
1
Ki = 4677.35 nM
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CP0490571
ethyl 3-[[benzyl-[2-[[(2S)-1-[3-[3-[3-[[(2S)-2-[[2-[benzyl-[[8-[(2,6-difluorophenyl)methyl]-6-ethoxycarbonyl-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidin-3-yl]methyl]amino]acetyl]amino]propanoyl]amino]prop-1-ynyl]phenyl]prop-2-ynylamino]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate
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C88H86F4N16O12
 1
1
Ki = 5300 nM
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CP0415934
[(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] morpholine-4-carboxylate
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C46H72ClN3O12
 1
1
Ki = 5623.41 nM
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CP0430671
(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-15-[2-(4-chlorophenyl)ethyl]-2-ethyl-6-hydroxy-8-[(3R,4S,6R)-3-hydroxy-6-methyl-4-[methyl(propan-2-yl)amino]oxan-2-yl]oxy-9-methoxy-1,5,7,9,11,13-hexamethyl-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,12,16-trione
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C41H65ClN2O10
 1
1
Ki = 10000 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0037858
(S)-4-(2-(azetidin-2-yl)ethoxy)-7-chloro-2-oxo-N-(pyrimidin-4-yl)-3-(3,4,5-trimethylphenyl)-1,2-dihydroquinoline-6-carboxamide
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C28H28ClN5O3
 6
1 Activity = 0.4 nM
2 IC50 = 0.44 nM
3 IC50 = 0.5 nM
4 IC50 = 1 nM
5 IC50 = 60 nM
6 Ki = 0.4 nM
CP0039875
1-(4-(1-(2,6-difluorobenzyl)-5-((benzyl(methyl)amino)methyl)-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-methoxyurea
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C36H31F2N5O4S
 38
1 IC50 = 0.1 nM
2 IC50 = 0.3 nM
3 IC50 = 0.4 nM
4 IC50 = 0.5 nM
5 IC50 = 0.6 nM
6 IC50 = 0.7 nM
7 IC50 = 0.8 nM
8 IC50 = 0.9 nM
9 IC50 = 1.1 nM
10 IC50 = 1.2 nM
11 IC50 = 1.3 nM
12 IC50 = 1.4 nM
13 IC50 = 1.8 nM
14 IC50 = 1.9 nM
15 IC50 = 2 nM
16 IC50 = 2.3 nM
17 IC50 = 2.5 nM
18 IC50 = 3 nM
19 IC50 = 4.3 nM
20 IC50 = 5.2 nM
21 IC50 = 6.3 nM
22 IC50 = 8.5 nM
23 IC50 = 9.7 nM
24 IC50 = 10 nM
25 IC50 = 12.1 nM
26 IC50 = 23.4 nM
27 IC50 = 24.4 nM
28 IC50 = 94.9 nM
29 IC50 = 108 nM
30 IC50 = 115 nM
31 IC50 = 148 nM
32 IC50 = 192 nM
33 IC50 = 193 nM
34 IC50 = 240 nM
35 IC50 = 242 nM
36 IC50 = 470 nM
37 IC50 = 1070 nM
38 Ki = 0.2 nM
CP0778924
3-[(Benzyl-methyl-amino)-methyl]-7-(2,6-difluoro-benzyl)-2-(4-isobutyrylamino-phenyl)-4-oxo-4,7-dihydro-thieno[2,3-b]pyridine-5-carboxylic acid isopropyl ester hydrochloride
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C37H38ClF2N3O4S
 1
1 IC50 = 0.2 nM
CP0227902
5-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-1-methyl-1H-pyridin-2-one
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C38H48N4O2
 1
1 IC50 = 0.2 nM
CP0039874
3-[(Benzyl-methyl-amino)-methyl]-7-(2,6-difluoro-benzyl)-2-(4-isobutyrylamino-phenyl)-4-oxo-4,7-dihydro-thieno[2,3-b]pyridine-5-carboxylic acid isopropyl ester; hydrochloride
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C37H37F2N3O4S
 4
1 IC50 = 0.2 nM
2 IC50 = 4 nM
3 IC50 = 60 nM
4 Ki = 0.2 nM
CP0091820
ELIGARD
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C59H84N16O12
 2
1 IC50 = 0.3 nM
2 IC50 = 0.8 nM
CP0095035
7-Chloro-2-oxo-4-((S)-2-piperidin-2-yl-ethoxy)-3-(3,4,5-trimethyl-phenyl)-1,2-dihydro-quinoline-6-carboxylic acid pyrimidin-4-ylamide
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C30H32ClN5O3
 1
1 IC50 = 0.3 nM
CP0213550
5-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-1H-pyridin-2-one
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C37H46N4O2
 1
1 IC50 = 0.3 nM
CP0122740
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-1-methyl-2-[2-(1-oxy-pyridin-4-yl)-ethylamino]-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
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C37H46N4O2
 1
1 IC50 = 0.3 nM
CP0361002
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-1-methyl-2-[2-(2-methyl-1-oxy-pyridin-4-yl)-ethylamino]-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
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C38H48N4O2
 1
1 IC50 = 0.3 nM
CP0076599
1-(1S,4R)-2-Aza-bicyclo[2.2.1]hept-2-yl-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
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C38H48N4O
 1
1 IC50 = 0.4 nM
CP0272840
5-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-1-methyl-piperidin-2-one
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C38H52N4O2
 1
1 IC50 = 0.4 nM
CP0522236
5-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-1-methoxymethyl-1H-pyridin-2-one
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C39H50N4O3
 1
1 IC50 = 0.4 nM
CP0115024
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-2-[2-(2,6-dimethyl-pyridin-4-yl)-ethylamino]-1-methyl-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
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C39H50N4O
 1
1 IC50 = 0.4 nM
CP0299579
Acetic acid 4-(2-{(S)-2-[5-[2-(2-aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-pyridin-2-ylmethyl ester
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C40H50N4O3
 1
1 IC50 = 0.4 nM
CP0464146
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-2-[2-(2-hydroxymethyl-pyridin-4-yl)-ethylamino]-1-methyl-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
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C38H48N4O2
 1
1 IC50 = 0.4 nM
CP0257614
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-[3-{(S)-2-[2-(2,6-dimethyl-1-oxy-pyridin-4-yl)-ethylamino]-1-methyl-ethyl}-2-(3,5-dimethyl-phenyl)-1H-indol-5-yl]-2-methyl-propan-1-one
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C39H50N4O2
 1
1 IC50 = 0.5 nM
CP0046868
(R)-1-(2,6-difluorobenzyl)-3-(2-amino-2-phenylethyl)-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4(1H,3H)-dione
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C27H24F3N3O3
 48
1 IC50 = 0.5 nM
2 IC50 = 0.6 nM
3 IC50 = 0.7 nM
4 IC50 = 0.8 nM
5 IC50 = 0.9 nM
6 IC50 = 1 nM
7 IC50 = 1.1 nM
8 IC50 = 1.2 nM
9 IC50 = 1.3 nM
10 IC50 = 1.4 nM
11 IC50 = 1.5 nM
12 IC50 = 1.6 nM
13 IC50 = 1.7 nM
14 IC50 = 1.8 nM
15 IC50 = 2.3 nM
16 IC50 = 2.4 nM
17 IC50 = 2.5 nM
18 IC50 = 2.6 nM
19 IC50 = 2.7 nM
20 IC50 = 2.8 nM
21 IC50 = 3 nM
22 IC50 = 3.1 nM
23 IC50 = 3.2 nM
24 IC50 = 3.4 nM
25 IC50 = 3.7 nM
26 IC50 = 5.5 nM
27 IC50 = 5.7 nM
28 IC50 = 6.6 nM
29 IC50 = 7.5 nM
30 IC50 = 8 nM
31 IC50 = 8.9 nM
32 IC50 = 9.2 nM
33 IC50 = 11.4 nM
34 IC50 = 13.9 nM
35 IC50 = 15.2 nM
36 IC50 = 24.2 nM
37 IC50 = 42.7 nM
38 IC50 = 80 nM
39 IC50 = 123 nM
40 IC50 = 182 nM
41 IC50 = 262 nM
42 IC50 = 980 nM
43 IC50 = 4200 nM
44 IC50 = 5000 nM
45 IC50 = 5030 nM
46 IC50 = 5200 nM
47 Ki = 0.56 nM
48 Ki = 3.5 nM
CP0135587
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(2-pyridin-3-yl-ethylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
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C37H46N4O
 1
1 IC50 = 0.6 nM
CP0213240
(S)-1-(2-aza-bicyclo[2.2.2]octan-2-yl)-2-(2-(3,5-dimethylphenyl)-3-(1-(2-(pyridin-4-yl)ethylamino)propan-2-yl)-1H-indol-5-yl)-2-methylpropan-1-one
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C37H46N4O
 1
1 IC50 = 0.6 nM
CP0246348
2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-1-(1,4-dioxa-8-aza-spiro[4.5]dec-8-yl)-2-methyl-propan-1-one
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C39H50N4O3
 1
1 IC50 = 0.6 nM
CP0371321
5-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-1,3-dimethyl-1H-pyridin-2-one
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C39H50N4O2
 1
1 IC50 = 0.6 nM
CP0215042
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-[2-(3,5-dimethyl-phenyl)-3-((S)-2-{2-[2-(1-hydroxy-ethyl)-pyridin-4-yl]-ethylamino}-1-methyl-ethyl)-1H-indol-5-yl]-2-methyl-propan-1-one
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C39H50N4O2
 1
1 IC50 = 0.6 nM
CP0463978
2-[3-{(S)-2-[2-(2-Acetyl-pyridin-4-yl)-ethylamino]-1-methyl-ethyl}-2-(3,5-dimethyl-phenyl)-1H-indol-5-yl]-1-(2-aza-bicyclo[2.2.2]oct-2-yl)-2-methyl-propan-1-one
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C39H48N4O2
 1
1 IC50 = 0.6 nM
CP0063211
1-(7-Aza-bicyclo[2.2.1]hept-7-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
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C38H48N4O
 1
1 IC50 = 0.7 nM
CP0136681
1-(3,3-Dimethyl-azetidin-1-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
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C37H48N4O
 1
1 IC50 = 0.7 nM
CP0155115
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-2-[2-(2-methoxymethyl-pyridin-4-yl)-ethylamino]-1-methyl-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
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C39H50N4O2
 1
1 IC50 = 0.7 nM
CP0194543
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-[2-(3,5-dimethyl-phenyl)-3-((S)-2-{2-[2-(1-hydroxy-1-methyl-ethyl)-pyridin-4-yl]-ethylamino}-1-methyl-ethyl)-1H-indol-5-yl]-2-methyl-propan-1-one
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C40H52N4O2
 1
1 IC50 = 0.7 nM
CP0221205
4-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-pyridine-2-carbonitrile
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C38H45N5O
 1
1 IC50 = 0.7 nM
CP0196863
1-(7-Aza-bicyclo[2.2.1]hept-7-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(2-pyridin-4-yl-ethylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
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C36H44N4O
 1
1 IC50 = 0.8 nM
CP0334675
1-(8-Aza-bicyclo[3.2.1]oct-8-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
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C39H50N4O
 1
1 IC50 = 0.8 nM
CP0172193
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-1-methyl-2-[2-(3-methyl-pyridin-4-yl)-ethylamino]-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
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C38H48N4O
 1
1 IC50 = 0.8 nM
CP0215181
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-1-methyl-2-[2-(3-methyl-1-oxy-pyridin-4-yl)-ethylamino]-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
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C38H48N4O2
 1
1 IC50 = 0.8 nM
CP0082419
4-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-pyridine-2-carboxylic acid methyl ester
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C39H48N4O3
 1
1 IC50 = 0.9 nM
CP0208585
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-1-methyl-2-[2-(2-methyl-pyridin-4-yl)-ethylamino]-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
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C38H48N4O
 1
1 IC50 = 0.9 nM
CP0216361
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
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C39H50N4O
 1
1 IC50 = 1 nM
CP0219557
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-2-[2-(6-methoxy-pyridin-3-yl)-ethylamino]-1-methyl-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
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C38H48N4O2
 1
1 IC50 = 1 nM
CP0327922
1-(1R,4S)-2-Aza-bicyclo[2.2.1]hept-2-yl-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
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C38H48N4O
 1
1 IC50 = 1 nM
CP0299019
1-(1R,4S)-2-Aza-bicyclo[2.2.1]hept-2-yl-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(2-pyridin-4-yl-ethylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
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C36H44N4O
 1
1 IC50 = 1.2 nM
CP0223103
2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-1-(4,4-dimethyl-piperidin-1-yl)-2-methyl-propan-1-one
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C39H52N4O
 1
1 IC50 = 1.3 nM
CP0225806
2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-1-(3aR,7aS)-octahydro-isoindol-2-yl-propan-1-one
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C40H52N4O
 1
1 IC50 = 1.4 nM
CP0236982
1-(7-Aza-bicyclo[2.2.1]hept-7-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
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C37H46N4O
 1
1 IC50 = 1.4 nM
CP0070855
(S)-1-(3-(1-(4-(1H-tetrazol-5-yl)phenethylamino)propan-2-yl)-2-(3,5-dimethylphenyl)-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-5(4H)-yl)-2-(2-fluoro-6-(trifluoromethyl)phenyl)ethanone
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C36H37F4N7O
 1
1 IC50 = 1.5 nM
CP0202958
5-((4-(2-(4-tert-butylphenyl)-1H-benzo[d]imidazol-4-yl)piperazin-1-yl)methyl)-1-ethylpyrimidine-2,4(1H,3H)-dione
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C28H34N6O2
 2
1 IC50 = 1.6 nM
2 IC50 = 1.7 nM
CP0332602
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid cyclooctyl-ethyl-amide
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C38H50N4O
 1
1 IC50 = 1.9 nM
CP0196182
1-(3-Aza-bicyclo[3.2.2]non-3-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
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C40H52N4O
 1
1 IC50 = 2.1 nM
CP0309400
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid cyclohexyl-ethyl-amide
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C36H46N4O
 1
1 IC50 = 2.3 nM
CP0524086
1-(8-Aza-spiro[4.5]dec-8-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
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C41H54N4O
 1
1 IC50 = 2.7 nM
CP0288623
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid cyclohexyl-ethyl-amide
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C36H46N4O
 1
1 IC50 = 2.8 nM
CP0055695
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-2-[2-(2-ethyl-pyridin-4-yl)-ethylamino]-1-methyl-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
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C39H50N4O
 1
1 IC50 = 3.3 nM
CP0286926
[2-(3,5-dimethylphenyl)-3-[2-(4-pyridin-3-ylbutylamino)ethyl]-1H-indol-5-yl]-(2,5-dimethylpyrrolidin-1-yl)methanone
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C34H42N4O
 1
1 IC50 = 3.6 nM
CP0223421
2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-1-(4-ethanesulfonyl-piperazin-1-yl)-2-methyl-propan-1-one
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C38H51N5O3S
 1
1 IC50 = 4.4 nM
CP0193348
1-(2-Aza-bicyclo[2.2.2]oct-2-yl)-2-(2-(3,5-dimethyl-phenyl)-3-{(S)-1-methyl-2-[2-(2-propyl-pyridin-4-yl)-ethylamino]-ethyl}-1H-indol-5-yl)-2-methyl-propan-1-one
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C40H52N4O
 1
1 IC50 = 4.6 nM
CP0336314
1-(6-Aza-bicyclo[3.2.1]oct-6-yl)-2-{2-(3,5-dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propan-1-one
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C39H50N4O
 1
1 IC50 = 4.8 nM
CP0364803
2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-1-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-propan-1-one
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C42H56N4O
 1
1 IC50 = 4.8 nM
CP0045709
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid diisobutylamide
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C36H48N4O
 1
1 IC50 = 5 nM
CP0299531
3-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-1-methyl-1H-pyridin-2-one
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C38H48N4O2
 1
1 IC50 = 5.3 nM
CP0219252
2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-N,N-diisobutyl-isobutyramide
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C40H56N4O
 1
1 IC50 = 5.6 nM
CP0091943
2-(4-tert-butylphenyl)-4-(4-((1-ethyl-5-methyl-1H-imidazol-4-yl)methyl)piperazin-1-yl)-1H-benzo[d]imidazole
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C28H36N6
 2
1 IC50 = 5.8 nM
2 IC50 = 7 nM
CP0112281
3-[(Benzyl-methyl-amino)-methyl]-7-(2,6-difluoro-benzyl)-2-(4-methoxy-phenyl)-4-oxo-4,7-dihydro-thieno[2,3-b]pyridine-5-carboxylic acid ethyl ester
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C33H30F2N2O4S
 1
1 IC50 = 6 nM
CP0110348
(S)-1-((S)-2-((S)-2-(2-((S)-2-((S)-2-((S)-2-((S)-3-(1H-imidazol-5-yl)-2-((S)-2-oxopyrrolidine-5-carboxamido)propanamido)-3-(1H-indol-2-yl)propanamido)-3-hydroxypropanamido)-3-(4-hydroxyphenyl)propanamido)acetamido)-4-methylpentanamido)-5-(diaminomethylene
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C53H72N16O12
 1
1 IC50 = 6 nM
CP0196914
4-(2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-2-methyl-propionyl)-piperazine-1-carboxylic acid tert-butyl ester
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C41H55N5O3
 1
1 IC50 = 6.1 nM
CP0080593
3-((R)-2-Amino-2-cyclohexyl-ethyl)-1-(2,6-difluoro-benzyl)-5-(2-fluoro-3-methoxy-phenyl)-6-methyl-1H-pyrimidine-2,4-dione
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C27H30F3N3O3
 3
1 IC50 = 6.5 nM
2 Ki = 6.5 nM
3 Ki = 120 nM
CP0054992
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid diisobutylamide
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C36H48N4O
 1
1 IC50 = 7.1 nM
CP0070868
2-(4-tert-butylphenyl)-4-(4-((2-methyl-1H-imidazol-4-yl)methyl)piperazin-1-yl)-1H-benzo[d]imidazole
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C26H32N6
 1
1 IC50 = 7.5 nM
CP0211626
2-(4-tert-butylphenyl)-4-(4-((1,2-diethyl-5-methyl-1H-imidazol-4-yl)methyl)piperazin-1-yl)-1H-benzo[d]imidazole
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C30H40N6
 1
1 IC50 = 8 nM
CP0363826
4-(2-{(S)-2-[5-[2-(2-Aza-bicyclo[2.2.2]oct-2-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethyl-phenyl)-1H-indol-3-yl]-propylamino}-ethyl)-pyridine-2-carboxylic acid
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C38H46N4O3
 1
1 IC50 = 8.2 nM
CP0191989
2-(4-tert-butylphenyl)-4-(4-((1,2-dimethyl-1H-imidazol-4-yl)methyl)piperazin-1-yl)-1H-benzo[d]imidazole
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C27H34N6
 1
1 IC50 = 10 nM
CP0368048
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid ethyl-isopropyl-amide
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C33H42N4O
 1
1 IC50 = 11 nM
CP0043368
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid diethylamide
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C32H40N4O
 1
1 IC50 = 18 nM
CP0152863
2-(4-tert-butylphenyl)-4-(4-((2-methyl-1-propyl-1H-imidazol-4-yl)methyl)piperazin-1-yl)-1H-benzo[d]imidazole
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C29H38N6
 1
1 IC50 = 18 nM
CP0167736
(S)-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)-6-methyl-3-(2-(methylamino)-3-phenylpropyl)pyrimidine-2,4(1H,3H)-dione
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C29H28F3N3O3
 3
1 IC50 = 20 nM
2 Ki = 8.1 nM
3 Ki = 200 nM
CP0149717
2-{2-(3,5-Dimethyl-phenyl)-3-[(S)-1-methyl-2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-1-(dodecahydro-carbazol-9-yl)-2-methyl-propan-1-one
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C44H58N4O
 1
1 IC50 = 21 nM
CP0105024
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid diethylamide
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C32H40N4O
 1
1 IC50 = 23 nM
CP0342019
5-((4-(2-(4-tert-butylphenyl)-1H-benzo[d]imidazol-4-yl)piperazin-1-yl)methyl)quinoxaline
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C30H32N6
 1
1 IC50 = 26 nM
CP0033448
BAY-784
   Show/Hide
C29H26ClF4N3O5S2
 2
1 IC50 = 27 nM
2 IC50 ~ 27 nM
CP0214050
(7-Aza-bicyclo[2.2.1]hept-7-yl)-{2-(3,5-dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indol-5-yl}-methanone
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C34H40N4O
 1
1 IC50 = 32 nM
CP0376521
2-{2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indol-5-yl}-isobutyramide
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C31H38N4O
 1
1 IC50 = 32 nM
CP0041665
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid ethyl-(2-hydroxy-ethyl)-amide
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C32H40N4O2
 1
1 IC50 = 36 nM
CP0297942
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-4-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid bis-(2,2,2-trifluoro-ethyl)-amide
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C32H34F6N4O
 1
1 IC50 = 36 nM
CP0352069
2-(3,5-Dimethyl-phenyl)-3-{2-[methyl-(4-pyridin-4-yl-butyl)-amino]-ethyl}-1H-indole-5-carboxylic acid diethylamide
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C33H42N4O
 1
1 IC50 = 36 nM
CP0258027
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid bis-(2-methoxy-ethyl)-amide
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C34H44N4O3
 1
1 IC50 = 45 nM
CP0071049
4-(4-((1-butyl-5-methyl-1H-imidazol-4-yl)methyl)piperazin-1-yl)-2-(4-tert-butylphenyl)-1H-benzo[d]imidazole
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C30H40N6
 1
1 IC50 = 46 nM
CP0256086
2-(3,5-Dimethyl-phenyl)-3-[2-(4-pyridin-3-yl-butylamino)-ethyl]-1H-indole-5-carboxylic acid isopropylamide
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C31H38N4O
 1
1 IC50 = 55 nM
CP0182886
3-[(Benzyl-methyl-amino)-methyl]-7-(2-methoxy-benzyl)-2-(4-methoxy-phenyl)-4-oxo-4,7-dihydro-thieno[2,3-b]pyridine-5-carboxylic acid ethyl ester
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C34H34N2O5S
 1
1 IC50 = 70 nM
CP0076365
7-(2-Methoxy-benzyl)-2-(4-methoxy-phenyl)-3-methylaminomethyl-4-oxo-4,7-dihydro-thieno[2,3-b]pyridine-5-carboxylic acid ethyl ester
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C27H28N2O5S
 1
1 IC50 = 2000 nM
CP0061893
1-(4-(1-(2,6-difluorobenzyl)-5-((benzyl(methyl)amino)methyl)-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-ethylurea
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C37H33F2N5O3S
 1
1 Ki = 0.4 nM
CP0158198
(R)-1-(2-fluoro-6-(trifluoromethyl)benzyl)-3-(2-amino-2-phenylethyl)-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4(1H,3H)-dione
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C28H24F5N3O3
 1
1 Ki = 0.5 nM
CP0061892
1-(2,6-Difluoro-benzyl)-5-{[methyl-(2-pyridin-2-yl-ethyl)-amino]-methyl}-6-(4-nitro-phenyl)-3-phenyl-1H-thieno[2,3-d]pyrimidine-2,4-dione
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C34H27F2N5O4S
 1
1 Ki = 0.6 nM
CP0043839
(R)-1-(2-fluoro-6-(trifluoromethyl)benzyl)-3-(2-amino-2-phenylethyl)-5-(2-fluoro-3-methoxyphenyl)pyrimidine-2,4(1H,3H)-dione
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C27H22F5N3O3
 1
1 Ki = 0.64 nM
CP0272654
N-[4-[5-[[benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]propanamide
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C37H32F2N4O3S
 1
1 Ki = 0.8 nM
CP0288327
(R)-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)-6-methyl-3-(2-(pyridin-2-ylmethylamino)propyl)pyrimidine-2,4(1H,3H)-dione
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C28H27F3N4O3
 1
1 Ki = 1.1 nM
CP0080596
1-(2,6-Difluoro-benzyl)-5-(2-fluoro-3-methoxy-phenyl)-6-methyl-3-((R)-4-methyl-2-methylamino-pentyl)-1H-pyrimidine-2,4-dione
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C26H30F3N3O3
 1
1 Ki = 1.2 nM
CP0211775
A-198401
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C47H69Cl2N3O13
 1
1 Ki = 1.995 nM
CP0124091
(R)-1-(2,6-difluorobenzyl)-3-(2-amino-2-phenylethyl)-5-(5-chlorothiophen-2-yl)-6-methylpyrimidine-2,4(1H,3H)-dione
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C24H20ClF2N3O2S
 1
1 Ki = 2 nM
CP0182660
7-(4-Butyrylamino-phenyl)-1-(2-fluoro-benzyl)-6-{[methyl-(2-pyridin-2-yl-ethyl)-amino]-methyl}-4-oxo-1,4-dihydro-pyrrolo[1,2-a]pyrimidine-3-carboxylic acid 1-ethyl-propyl ester
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C39H44FN5O4
 1
1 Ki = 2.7 nM
CP0193577
N-[4-[5-[[benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-2-methylpropanamide
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C38H34F2N4O3S
 1
1 Ki = 2.9 nM
CP0176635
(R)-1-(2,6-difluorobenzyl)-3-(1-(2-methoxybenzylamino)propan-2-yl)-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4(1H,3H)-dione
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C30H30F3N3O4
 1
1 Ki = 3.7 nM
CP0061901
N-[4-[5-[[benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]acetamide
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C36H30F2N4O3S
 1
1 Ki = 4.1 nM
CP0156900
(S)-1-(2,6-difluorobenzyl)-3-(2-(cyclopentylamino)propyl)-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4(1H,3H)-dione
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C27H30F3N3O3
 1
1 Ki = 4.5 nM
CP0439838
(R)-1-(2,6-difluorobenzyl)-5-(3-methoxyphenyl)-6-methyl-3-(2-(methyl(2-(pyridin-2-yl)ethyl)amino)propyl)pyrimidine-2,4(1H,3H)-dione
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C30H32F2N4O3
 1
1 Ki = 5.2 nM
CP0124188
(R)-1-(2,6-difluorobenzyl)-3-(2-amino-2-phenylethyl)-5-(2-fluoro-3-methoxyphenyl)pyrimidine-2,4(1H,3H)-dione
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C26H22F3N3O3
 1
1 Ki = 5.3 nM
CP0088206
(R)-1-(2,6-difluorobenzyl)-5-(3-methoxyphenyl)-6-methyl-3-(2-(methyl(pyridin-2-ylmethyl)amino)propyl)pyrimidine-2,4(1H,3H)-dione
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C29H30F2N4O3
 2
1 Ki = 5.5 nM
2 Ki = 102 nM
CP0165712
5-((3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)methyl)-N-(2,4,6-trimethoxyphenyl)furan-2-carboxamide
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C30H37NO5
 1
1 Ki = 6 nM
CP0290843
3-((R)-2-Amino-4-methyl-pentyl)-1-(2,6-difluoro-benzyl)-5-(2-fluoro-3-methoxy-phenyl)-6-methyl-1H-pyrimidine-2,4-dione
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C25H28F3N3O3
 1
1 Ki = 6.4 nM
CP0367573
1-(2,6-Difluoro-benzyl)-3-((S)-2-dimethylamino-3-phenyl-propyl)-5-(2-fluoro-3-methoxy-phenyl)-6-methyl-1H-pyrimidine-2,4-dione
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C30H30F3N3O3
 1
1 Ki = 7.9 nM
CP0292322
(R)-1-(2,6-difluorobenzyl)-3-(2-amino-2-phenylethyl)-5-(2-fluoro-3-methoxyphenyl)-1,3,5-triazinane-2,4,6-trione
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C25H21F3N4O4
 1
1 Ki = 9 nM
CP0288326
(R)-1-(2,6-difluorobenzyl)-5-(3-methoxyphenyl)-6-methyl-3-(2-(pyridin-2-ylmethylamino)propyl)pyrimidine-2,4(1H,3H)-dione
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C28H28F2N4O3
 1
1 Ki = 15 nM
CP0306971
1-(2,6-difluorobenzyl)-6-(4-(methylthio)benzyl)-3-(2-(methyl(2-(pyridin-2-yl)ethyl)amino)ethyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine-2,4(1H,3H)-dione
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C32H35F2N5O2S
 1
1 Ki = 15 nM
CP0046850
3-((S)-2-Amino-3-phenyl-propyl)-1-(2,6-difluoro-benzyl)-5-(2-fluoro-3-methoxy-phenyl)-6-methyl-1H-pyrimidine-2,4-dione
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C28H26F3N3O3
 1
1 Ki = 16 nM
CP0276324
1-(2,6-difluoro-benzyl)-5-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-6-methyl-3-{2-[methyl-(2-pyridin-2-yl-ethyl)-amino]-ethyl}-1H-pyrimidine-2,4-dione
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C30H30F2N4O4
 1
1 Ki = 24 nM
CP0167737
1-((R)-2-Amino-2-phenyl-ethyl)-3-(2-bromo-6-fluoro-benzyl)-5-(2-fluoro-3-methoxy-phenyl)-[1,3,5]triazinane-2,4,6-trione
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C25H21BrF2N4O4
 1
1 Ki = 24 nM
CP0124192
(R)-methyl 4-(2-(3-(2-fluoro-6-(trifluoromethyl)benzyl)-5-(2-fluoro-3-methoxyphenyl)-2,6-dioxo-2,3-dihydropyrimidin-1(6H)-yl)-1-phenylethylamino)butanoate
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C32H30F5N3O5
 1
1 Ki = 32 nM
CP0257980
1-(2,6-Difluoro-benzyl)-5-(3-methoxy-phenyl)-6-methyl-3-[2-(2-pyridin-2-yl-ethylamino)-ethyl]-1H-pyrimidine-2,4-dione
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C28H28F2N4O3
 1
1 Ki = 34 nM
CP0061891
1-(2,6-difluorobenzyl)-6-(4-aminophenyl)-5-((benzyl(methyl)amino)methyl)-3-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
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C34H28F2N4O2S
 1
1 Ki = 36 nM
CP0039878
(R)-1-(2,6-difluorobenzyl)-3-(2-amino-2-phenylethyl)-5-(3-methoxyphenyl)-1,3,5-triazinane-2,4,6-trione
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C25H22F2N4O4
 1
1 Ki = 37 nM
CP0266590
5-Benzo[1,3]dioxol-5-yl-1-(2,6-difluoro-benzyl)-6-methyl-3-{2-[methyl-(2-pyridin-2-yl-ethyl)-amino]-ethyl}-1H-pyrimidine-2,4-dione
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C29H28F2N4O4
 1
1 Ki = 38 nM
CP0167734
3-((S)-2-Amino-4-methyl-pentyl)-1-(2,6-difluoro-benzyl)-5-(2-fluoro-3-methoxy-phenyl)-6-methyl-1H-pyrimidine-2,4-dione
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C25H28F3N3O3
 1
1 Ki = 39 nM
CP0344191
6-[(Benzyl-methyl-amino)-methyl]-1-(2-fluoro-benzyl)-7-(4-isobutyrylamino-phenyl)-4-oxo-1,4-dihydro-pyrrolo[1,2-a]pyrimidine-3-carboxylic acid ethyl ester
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C36H37FN4O4
 1
1 Ki = 44 nM
CP0363522
3-((S)-2-Amino-2-cyclohexyl-ethyl)-1-(2,6-difluoro-benzyl)-5-(2-fluoro-3-methoxy-phenyl)-6-methyl-1H-pyrimidine-2,4-dione
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C27H30F3N3O3
 1
1 Ki = 46 nM
CP0167735
3-((R)-2-Amino-3-methyl-butyl)-1-(2,6-difluoro-benzyl)-5-(2-fluoro-3-methoxy-phenyl)-6-methyl-1H-pyrimidine-2,4-dione
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C24H26F3N3O3
 1
1 Ki = 51 nM
CP0057956
1-(2-Fluoro-benzyl)-7-(4-methoxy-phenyl)-6-{[methyl-(2-pyridin-2-yl-ethyl)-amino]-methyl}-4-oxo-1,4-dihydro-pyrrolo[1,2-a]pyrimidine-3-carboxylic acid ethyl ester
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C33H33FN4O4
 1
1 Ki = 55 nM
CP0363519
3-((R)-2-Amino-3-phenyl-propyl)-1-(2,6-difluoro-benzyl)-5-(2-fluoro-3-methoxy-phenyl)-6-methyl-1H-pyrimidine-2,4-dione
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C28H26F3N3O3
 1
1 Ki = 66 nM
CP0263178
2-[3-((R)-2-Amino-2-phenyl-ethyl)-5-(2-fluoro-3-methoxy-phenyl)-2,4,6-trioxo-[1,3,5]triazinan-1-ylmethyl]-benzonitrile
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C26H22FN5O4
 1
1 Ki = 86 nM
CP0112996
8-Cyano-1-(2-fluoro-benzyl)-7-(4-isobutoxy-phenyl)-6-{[methyl-(2-pyridin-2-yl-ethyl)-amino]-methyl}-4-oxo-1,4-dihydro-pyrrolo[1,2-a]pyrimidine-3-carboxylic acid ethyl ester
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C37H38FN5O4
 1
1 Ki = 100 nM
CP0137688
(R)-ethyl 2-(4-(1-(2-fluoro-6-(trifluoromethyl)benzyl)-3-(2-amino-2-phenylethyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)benzylamino)acetate
   Show/Hide
C31H30F4N4O4
 1
1 Ki = 110 nM
CP0061904
1-(2,6-Difluoro-benzyl)-5-[(methyl-phenethyl-amino)-methyl]-6-(4-nitro-phenyl)-3-phenyl-1H-thieno[2,3-d]pyrimidine-2,4-dione
   Show/Hide
C35H28F2N4O4S
 1
1 Ki = 170 nM
CP0220826
1-(2,6-difluorobenzyl)-5-((benzyl(methyl)amino)methyl)-6-(4-nitrophenyl)-3-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
   Show/Hide
C34H26F2N4O4S
 1
1 Ki = 180 nM
CP0186211
1-(2,6-Difluoro-benzyl)-5-(4-methoxy-phenyl)-6-methyl-3-{2-[methyl-(2-pyridin-2-yl-ethyl)-amino]-ethyl}-1H-pyrimidine-2,4-dione
   Show/Hide
C29H30F2N4O3
 1
1 Ki = 230 nM
CP0370351
1-((R)-2-Amino-2-phenyl-ethyl)-3-(2-fluoro-3-methoxy-phenyl)-5-(2-trifluoromethoxy-benzyl)-[1,3,5]triazinane-2,4,6-trione
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C26H22F4N4O5
 1
1 Ki = 240 nM
CP0190830
1-(2,6-Difluoro-benzyl)-6-methyl-3-{2-[methyl-(2-pyridin-2-yl-ethyl)-amino]-ethyl}-5-phenyl-1H-pyrimidine-2,4-dione
   Show/Hide
C28H28F2N4O2
 1
1 Ki = 400 nM
CP0288325
(S)-1-(2,6-difluorobenzyl)-5-(3-methoxyphenyl)-6-methyl-3-(2-(methyl(2-(pyridin-2-yl)ethyl)amino)propyl)pyrimidine-2,4(1H,3H)-dione
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C30H32F2N4O3
 1
1 Ki = 470 nM
CP0080594
3-((R)-2-Amino-propyl)-1-(2,6-difluoro-benzyl)-5-(2-fluoro-3-methoxy-phenyl)-6-methyl-1H-pyrimidine-2,4-dione
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C22H22F3N3O3
 1
1 Ki = 600 nM
CP0363523
3-((S)-2-Amino-3-methyl-butyl)-1-(2,6-difluoro-benzyl)-5-(2-fluoro-3-methoxy-phenyl)-6-methyl-1H-pyrimidine-2,4-dione
   Show/Hide
C24H26F3N3O3
 1
1 Ki = 970 nM
CP0137685
(R)-2-(4-(1-(2-fluoro-6-(trifluoromethyl)benzyl)-3-(2-amino-2-phenylethyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)benzylamino)acetic acid
   Show/Hide
C29H26F4N4O4
 1
1 Ki = 3900 nM
CP0080595
3-((S)-2-Amino-propyl)-1-(2,6-difluoro-benzyl)-5-(2-fluoro-3-methoxy-phenyl)-6-methyl-1H-pyrimidine-2,4-dione
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C22H22F3N3O3
 1
1 Ki > 10000 nM
CP0267018
(R)-2-(4-(1-(2-fluoro-6-(trifluoromethyl)benzyl)-3-(2-amino-2-phenylethyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)benzyloxy)acetic acid
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C29H25F4N3O5
 1
1 Ki > 10000 nM
Clinical Information about the Protein
Target 1 ( Gonadotropin-releasing hormone receptor (GNRHR) )
Target Type Successful Target
Disease 9 Target-related Diseases  9
1 Prostate cancer [ICD-11: 2C82.0]
2 Ovarian stimulation [ICD-11: LB45.1]
3 Endometriosis [ICD-11: GA10]
4 Ovulation dysfunction [ICD-11: 5A80]
5 Hypothalamic hypogonadism [ICD-11: 5A61.2]
6 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
7 Uterine fibroids [ICD-11: 2E86.0]
8 Hormone deficiency [ICD-11: 5A61.1]
9 Coronavirus infection [ICD-11: 1D92]
Approved Drug(s) 10 Approved Drugs  10
1 Abarelix Approved
Prostate cancer
2 Cetrorelix Approved
Ovarian stimulation
3 Degarelix Approved
Prostate cancer
4 Elagolix sodium Approved
Endometriosis
5 Ganirelix Approved
Ovulation dysfunction
6 Gonadorelin Approved
Hypothalamic hypogonadism
7 Leuprorelin acetate Approved
Prostate cancer
8 Nafarelin Approved
Endometriosis
9 Triptorelin Approved
Solid tumour/cancer
10 Relugolix Approved
Prostate cancer
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 ACYLINE Phase 2
Prostate cancer
2 KLH-2109 Phase 2
Endometriosis
Discontinued Drug(s) 3 Discontinued Drugs  3
1 TAK-013 Discontinued in Phase 2
Uterine fibroids
2 A-75998 Discontinued in Phase 1
Hormone deficiency
3 NBI-42902 Discontinued in Phase 1
Prostate cancer
Preclinical Drug(s) 1 Preclinical Drug  1
1 5-(N,N-hexamethylene)-amiloride Preclinical
Coronavirus infection
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01997 Gonadotropin-releasing hormone receptor Rattus norvegicus, Rat
PT02079 Gonadotropin-releasing hormone receptor Macaca mulatta, Rhesus macaque