Brief Information of the Cell Line and Protein
Cell Line ID: CL000011 , CHO
Synonyms
Chinese Hamster Ovary
CHO-ori
Category Spontaneously immortalized cell line
Organism
Cricetulus griseus (Chinese hamster)
Cellosaurus ID
CVCL_0213
Protein ID: PT01836 , Gonadotropin-releasing hormone receptor
Gene Name GNRHR
Organism Homo sapiens, Human
Protein Classification Membrane receptor
Uniprot ID P30968
Table of Molecular Bioactivities Related to the Cell Line and Protein
Cell Line ID: CL000011  Protein ID: PT01836
 
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   Show/Hide
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
   LO
   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
   LO
   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
   LO
   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
   LI
   LO
   TS
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
   TI
   LI
   LO
   TS
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
   TI
   LI
   LO
   TS
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
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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
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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
   TI
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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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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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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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   TS
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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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
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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
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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
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2
IC50 = 486 nM
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   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
   LI
   LO
   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
   LI
   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
   LI
   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
   LI
   LO
   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
   LI
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   TS
2
IC50 = 1150 nM
   TI
   LI
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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
   LI
   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
   TI
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   TS
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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   TS
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
   TI
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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
   TI
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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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   TS
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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   TS
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
   TI
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   TS
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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   TS
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
   Show/Hide
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
   Show/Hide
C28H30N2O5S
 1
1
IC50 = 500 nM
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   TS
CP0486699
ethyl 7-benzyl-3-[[benzyl(methyl)amino]methyl]-2-(3-methoxyphenyl)-4-oxothieno[2,3-b]pyridine-5-carboxylate
   Show/Hide
C33H32N2O4S
 1
1
IC50 = 500 nM
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   TS
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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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
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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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