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: PT00914 , Melanocortin receptor 4
Gene Name MC4R
Organism Homo sapiens, Human
Protein Classification Membrane receptor
Uniprot ID P32245
Table of Molecular Bioactivities Related to the Cell Line and Protein
Cell Line ID: CL000011  Protein ID: PT00914
 
Compound ID Compound Name Compound Formula
CP0404503
(3S)-N-[(2R)-1-[[(2S)-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-(4-iodophenyl)-1-oxopropan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
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C36H42IN9O4
 3
1
Activity = 0.3 nM
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2
Kd = 0.7943 nM
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3
Ki = 0.79 nM
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CP0374300
(3S,6S,9R,12S,15S,23S)-15-[[(2S)-2-acetamidohexanoyl]amino]-9-benzyl-6-[3-(diaminomethylideneamino)propyl]-12-(4H-imidazol-5-ylmethyl)-3-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-23-carboxamide
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C50H69N15O9
 1
1
EC50 = 0.11 nM
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CP0458781
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-1-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methylpropan-1-one
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C37H48ClF2N3O3
 2
1
EC50 = 0.25 nM
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2
IC50 = 0.53 nM
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CP0411217
(3S,11S,14S,17S,20R,23S)-3-[[(2S)-2-acetamidohexanoyl]amino]-20-benzyl-17-[3-(diaminomethylideneamino)propyl]-14-(1H-indol-3-ylmethyl)-2,5,13,16,19,22-hexaoxo-1,6,12,15,18,21-hexazabicyclo[21.3.0]hexacosane-11-carboxamide
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C49H69N13O9
 1
1
EC50 = 0.34 nM
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CP0373322
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-1-[(3S)-3-hydroxypyrrolidin-1-yl]-2-methylpropan-1-one
   Show/Hide
C37H48ClF2N3O3
 2
1
EC50 = 0.37 nM
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2
IC50 = 0.89 nM
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CP0397988
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-2-methyl-1-morpholin-4-ylpropan-1-one
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C37H48ClF2N3O3
 2
1
EC50 = 0.38 nM
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2
IC50 = 0.85 nM
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CP0375196
1-(azetidin-1-yl)-2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-2-methylpropan-1-one
   Show/Hide
C36H46ClF2N3O2
 2
1
EC50 = 0.59 nM
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2
IC50 = 1.1 nM
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CP0383644
(S)-(6-chloro-5-methyl-3-(2-morpholinopropan-2-yl)-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)((3S,4R)-4-(2,4-difluorophenyl)-1-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl)methanone
   Show/Hide
C36H46ClF2N3O4
 2
1
EC50 = 0.6 nM
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2
IC50 = 1 nM
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CP0436625
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-1-[(3R)-3-methoxypyrrolidin-1-yl]-2-methylpropan-1-one
   Show/Hide
C38H50ClF2N3O3
 2
1
EC50 = 0.69 nM
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2
IC50 = 1.4 nM
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CP0436185
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-2-methyl-1-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]propan-1-one
   Show/Hide
C38H48ClF2N3O3
 2
1
EC50 = 0.76 nM
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2
IC50 = 1.6 nM
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CP0383645
(S)-(6-chloro-3-(2-((S)-3-hydroxypyrrolidin-1-yl)propan-2-yl)-5-methyl-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)((3S,4R)-4-(2,4-difluorophenyl)-1-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl)methanone
   Show/Hide
C36H46ClF2N3O4
 2
1
EC50 = 0.8 nM
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2
IC50 = 1.4 nM
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CP0436634
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-N-cyclopropyl-2-methylpropanamide
   Show/Hide
C36H46ClF2N3O2
 2
1
EC50 = 0.8 nM
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2
IC50 = 2.2 nM
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CP0376062
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-N,N,2-trimethylpropanamide
   Show/Hide
C35H46ClF2N3O2
 2
1
EC50 = 0.87 nM
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2
IC50 = 0.71 nM
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CP0458785
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-N,2-dimethylpropanamide
   Show/Hide
C34H44ClF2N3O2
 2
1
EC50 = 0.91 nM
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2
IC50 = 2.6 nM
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CP0397987
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-2-methylpropan-1-one
   Show/Hide
C37H47ClF3N3O2
 2
1
EC50 = 0.98 nM
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2
IC50 = 1.4 nM
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CP0458787
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-2-methyl-1-pyrrolidin-1-ylpropan-1-one
   Show/Hide
C37H48ClF2N3O2
 2
1
EC50 = 1 nM
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2
IC50 = 1.8 nM
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CP0398561
2-((S)-1'-((3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl)-6-chloro-5-methyl-3H-spiro[isobenzofuran-1,4'-piperidine]-3-yl)-2-methylpropanenitrile
   Show/Hide
C32H38ClF2N3O2
 2
1
EC50 = 1.1 nM
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2
IC50 = 0.9 nM
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CP0373321
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-1-[(3R)-3-fluoropyrrolidin-1-yl]-2-methylpropan-1-one
   Show/Hide
C37H47ClF3N3O2
 2
1
EC50 = 1.1 nM
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2
IC50 = 1.6 nM
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CP0502886
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-N-(2-fluoroethyl)-2-methylpropanamide
   Show/Hide
C35H45ClF3N3O2
 2
1
EC50 = 1.1 nM
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2
IC50 = 2.6 nM
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CP0458782
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-1-[(3S)-3-methoxypyrrolidin-1-yl]-2-methylpropan-1-one
   Show/Hide
C38H50ClF2N3O3
 2
1
EC50 = 1.2 nM
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2
IC50 = 2.3 nM
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CP0501239
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-N-(2-hydroxyethyl)-2-methylpropanamide
   Show/Hide
C35H46ClF2N3O3
 2
1
EC50 = 1.3 nM
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2
IC50 = 2.6 nM
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CP0375193
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-N-ethyl-2-methylpropanamide
   Show/Hide
C35H46ClF2N3O2
 2
1
EC50 = 1.4 nM
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2
IC50 = 3.1 nM
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CP0501574
(S)-(6-chloro-3-(2-(dimethylamino)propan-2-yl)-5-methyl-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)((3S,4R)-4-(2,4-difluorophenyl)-1-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl)methanone
   Show/Hide
C34H44ClF2N3O3
 2
1
EC50 = 1.5 nM
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2
IC50 = 2.4 nM
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CP0373323
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-N-ethyl-N,2-dimethylpropanamide
   Show/Hide
C36H48ClF2N3O2
 2
1
EC50 = 1.6 nM
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2
IC50 = 2.1 nM
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CP0458340
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-N,N-diethyl-2-methylpropanamide
   Show/Hide
C37H50ClF2N3O2
 2
1
EC50 = 1.7 nM
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2
IC50 = 2.6 nM
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CP0045108
(4S)-4-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-[({[(2S)-6-amino-1-[(2S)-2-{[(1S)-1-carbamoyl-2-methylpropyl]carbamoyl}pyrrolidin-1-yl]-1-oxohexan-2-yl]carbamoyl}methyl)carbamoyl]-2-(1H-indol-3-yl)ethyl]carbamoyl}-4-carbamimidamidobutyl]carbamoyl}-2-phenylethyl]carbamoyl}-2-(1H-imidazol-5-yl)ethyl]carbamoyl}-4-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-acetamido-3-hydroxypropanamido]-3-(4-hydroxyphenyl)propanamido]-3-hydroxypropanamido]-4-(methylsulfanyl)butanamido]butanoic acid
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C77H109N21O19S
 4
1
EC50 = 1.9 nM
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2
EC50 = 2.2 nM
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3
IC50 = 19 nM
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4
Ki = 21 nM
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CP0436184
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-N-(1-hydroxy-2-methylpropan-2-yl)-2-methylpropanamide
   Show/Hide
C37H50ClF2N3O3
 2
1
EC50 = 1.9 nM
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2
IC50 = 3.9 nM
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CP0083436
N-[(1S)-1-[2-[1-[(3S,4R)-4-(4-bromo-2-fluorophenyl)-1-tert-butylpyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
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C31H40BrClFN3O2
 2
1
EC50 = 2.1 nM
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2
IC50 = 4 nM
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CP0375191
N-[2-[(1R)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]propan-2-yl]-N-methylacetamide
   Show/Hide
C35H46ClF2N3O2
 2
1
EC50 = 2.1 nM
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2
IC50 = 8.5 nM
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CP0474889
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-2-methyl-N-(oxan-4-yl)propanamide
   Show/Hide
C38H50ClF2N3O3
 2
1
EC50 = 2.3 nM
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2
IC50 = 2.5 nM
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CP0493345
2-((S)-6-chloro-1'-((3S,4R)-4-(2,4-difluorophenyl)-1-(1-hydroxy-2-methylpropan-2-yl)pyrrolidine-3-carbonyl)-5-methyl-3H-spiro[isobenzofuran-1,4'-piperidine]-3-yl)-2-methylpropanenitrile
   Show/Hide
C32H38ClF2N3O3
 2
1
EC50 = 2.6 nM
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2
IC50 = 2.8 nM
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CP0283823
2-((S)-6-chloro-1'-((3S,4R)-4-(2,4-difluorophenyl)-1-(tetrahydro-2H-pyran-4-yl)pyrrolidine-3-carbonyl)-5-methyl-3H-spiro[isobenzofuran-1,4'-piperidine]-3-yl)-2-methylpropanenitrile
   Show/Hide
C33H38ClF2N3O3
 2
1
EC50 = 2.7 nM
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2
IC50 = 2 nM
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CP0202447
N-[(1S)-1-[2-[1-[(3S,4R)-1-tert-butyl-4-(4-chloro-2-fluorophenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C31H40Cl2FN3O2
 2
1
EC50 = 2.8 nM
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2
IC50 = 6.2 nM
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CP0464643
N-[(2R)-1-[[(2R)-1-(4-butanoyl-4-cyclohexylpiperidin-1-yl)-3-(4-chlorophenyl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-2-yl)-1-oxopropan-2-yl]benzamide
   Show/Hide
C37H46ClN5O4
 1
1
EC50 = 2.9 nM
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CP0487086
(S)-(6-chloro-3-(2-(3,3-difluoropyrrolidin-1-yl)propan-2-yl)-5-methyl-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)((3S,4R)-4-(2,4-difluorophenyl)-1-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl)methanone
   Show/Hide
C36H44ClF4N3O3
 2
1
EC50 = 2.9 nM
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2
IC50 = 2.4 nM
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CP0458786
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-2-methyl-N-propan-2-ylpropanamide
   Show/Hide
C36H48ClF2N3O2
 2
1
EC50 = 2.9 nM
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2
IC50 = 5.9 nM
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CP0453783
(S)-(6-chloro-5-methyl-3-(2-(pyrrolidin-1-yl)propan-2-yl)-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)((3S,4R)-4-(2,4-difluorophenyl)-1-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl)methanone
   Show/Hide
C36H46ClF2N3O3
 2
1
EC50 = 3.1 nM
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2
IC50 = 1.6 nM
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CP0401729
(S)-(6-chloro-3-(2-(ethylamino)propan-2-yl)-5-methyl-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)((3S,4R)-4-(2,4-difluorophenyl)-1-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl)methanone
   Show/Hide
C34H44ClF2N3O3
 2
1
EC50 = 3.3 nM
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2
IC50 = 2.3 nM
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CP0401382
N-[2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]propan-2-yl]acetamide
   Show/Hide
C34H44ClF2N3O2
 2
1
EC50 = 3.3 nM
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2
IC50 = 4.5 nM
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CP0378145
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(R)-1-(4-chloro-benzyl)-2-oxo-2-(4-{2-[1-(piperidin-3-ylamino)-ethyl]-phenyl}-piperazin-1-yl)-ethyl]-amide
   Show/Hide
C36H45ClN6O2
 2
1
EC50 = 3.8 nM
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2
EC50 = 4.7 nM
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CP0398565
(S)-(6-chloro-5-methyl-3-(2-(methylamino)propan-2-yl)-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)((3S,4R)-4-(2,4-difluorophenyl)-1-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl)methanone
   Show/Hide
C33H42ClF2N3O3
 2
1
EC50 = 3.8 nM
   TI
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2
IC50 = 3.6 nM
   TI
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CP0436186
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-1-(3,3-difluoropyrrolidin-1-yl)-2-methylpropan-1-one
   Show/Hide
C37H46ClF4N3O2
 2
1
EC50 = 3.8 nM
   TI
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2
IC50 = 2 nM
   TI
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CP0383465
((3R,4S)-4-(2,4-difluorophenyl)-1-(pyrimidin-4-yl)pyrrolidin-3-yl)((3S,4S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C28H30F2N4O2
 2
1
EC50 = 4 nM
   TI
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2
Ki = 64 nM
   TI
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CP0896615
(3R,4R,5S)-1-{[(3S,4R)-4-(2,4-Difluorophenyl)-1-pyridazin-3-ylpyrrolidin-3-yl]carbonyl}-4-(4-fluorophenyl)-3,5-dimethylpiperidin-4-ol Hydrochloride
   Show/Hide
C28H30ClF3N4O2
 1
1
EC50 = 4 nM
   TI
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   TS
CP0524744
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-2-methyl-N-(2,2,2-trifluoroethyl)propanamide
   Show/Hide
C35H43ClF5N3O2
 2
1
EC50 = 4.2 nM
   TI
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2
IC50 = 5.4 nM
   TI
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CP0458338
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-1-(3,3-difluoroazetidin-1-yl)-2-methylpropan-1-one
   Show/Hide
C36H44ClF4N3O2
 2
1
EC50 = 4.3 nM
   TI
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2
IC50 = 1.8 nM
   TI
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CP0474317
N-[2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]propan-2-yl]-N-methylacetamide
   Show/Hide
C35H46ClF2N3O2
 2
1
EC50 = 4.3 nM
   TI
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2
IC50 = 2.5 nM
   TI
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CP0161427
N-[(1S)-1-[2-[1-[(3S,4R)-1-tert-butyl-4-(2-fluoro-4-methoxyphenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C32H43ClFN3O3
 2
1
EC50 = 4.6 nM
   TI
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2
IC50 = 11.2 nM
   TI
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   TS
CP0377765
N-[2-[(1R)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]propan-2-yl]acetamide
   Show/Hide
C34H44ClF2N3O2
 2
1
EC50 = 4.6 nM
   TI
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2
IC50 = 13 nM
   TI
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   TS
CP0430472
((3R,4S)-4-(2,4-difluorophenyl)-1-(pyridin-3-yl)pyrrolidin-3-yl)((3S,4S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C29H31F2N3O2
 2
1
EC50 = 5 nM
   TI
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2
Ki = 50 nM
   TI
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CP0382248
(2S)-2-amino-N-[(1S)-1-[2-[4-[(3S,4R)-4-(4-chlorophenyl)-1-(oxan-4-yl)pyrrolidine-3-carbonyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]propanamide
   Show/Hide
C34H48ClN5O3
 1
1
EC50 = 5.2 nM
   TI
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   TS
CP0149367
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(R)-1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-amide
   Show/Hide
C33H41ClN6O2
 2
1
EC50 = 5.7 nM
   TI
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2
IC50 = 1.2 nM
   TI
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CP0382253
3-amino-N-[(1S)-1-[2-[4-[(3S,4R)-4-(4-chlorophenyl)-1-(oxan-4-yl)pyrrolidine-3-carbonyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]propanamide
   Show/Hide
C34H48ClN5O3
 1
1
EC50 = 6 nM
   TI
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   TS
CP0374301
((3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4R,5R)-4-(3-fluorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)methanone
   Show/Hide
C28H35F3N2O2
 2
1
EC50 = 6 nM
   TI
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2
Ki = 97 nM
   TI
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CP0400031
((3R,4S)-4-(2,4-difluorophenyl)-1-(pyridazin-3-yl)pyrrolidin-3-yl)((3S,4S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C28H30F2N4O2
 2
1
EC50 = 6 nM
   TI
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2
Ki = 10 nM
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CP0460887
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-(2-dimethylaminomethyl-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C32H38ClN5O2
 1
1
EC50 = 7 nM
   TI
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CP0430471
((3R,4S)-4-(2,4-difluorophenyl)-1-(pyridazin-3-yl)pyrrolidin-3-yl)((3S,4S,5R)-4-hydroxy-3,5-dimethyl-4-(pyridin-2-yl)piperidin-1-yl)methanone
   Show/Hide
C27H29F2N5O2
 2
1
EC50 = 7 nM
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2
Ki = 52 nM
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CP0415239
N-[2-[(1S)-5-chloro-1'-[(3S,4R)-4-(2,4-difluorophenyl)-1-(oxan-4-yl)pyrrolidine-3-carbonyl]-6-methylspiro[1H-2-benzofuran-3,4'-piperidine]-1-yl]propan-2-yl]acetamide
   Show/Hide
C34H42ClF2N3O4
 2
1
EC50 = 7.4 nM
   TI
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2
IC50 = 6.2 nM
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CP0493346
2-((S)-1'-((3S,4R)-4-(2,4-difluorophenyl)-1-(tetrahydro-2H-pyran-4-yl)pyrrolidine-3-carbonyl)-5,6-difluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-3-yl)-2-methylpropanenitrile
   Show/Hide
C32H35F4N3O3
 2
1
EC50 = 8.4 nM
   TI
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2
IC50 = 7.6 nM
   TI
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CP0372778
2-amino-N-[(1S)-1-[2-[4-[(3S,4R)-4-(4-chlorophenyl)-1-(oxan-4-yl)pyrrolidine-3-carbonyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]acetamide
   Show/Hide
C33H46ClN5O3
 1
1
EC50 = 9.1 nM
   TI
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CP0415246
2-((S)-6-chloro-1'-((3S,4R)-4-(2,4-difluorophenyl)-1-isopropylpyrrolidine-3-carbonyl)-5-methyl-3H-spiro[isobenzofuran-1,4'-piperidine]-3-yl)-2-methylpropanenitrile
   Show/Hide
C31H36ClF2N3O2
 2
1
EC50 = 9.8 nM
   TI
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2
IC50 = 6.6 nM
   TI
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CP0508622
N-tert-butyl-2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-2-methylpropanamide
   Show/Hide
C37H50ClF2N3O2
 2
1
EC50 = 9.9 nM
   TI
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2
IC50 = 12 nM
   TI
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CP0377910
1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(R)-1-(4-chloro-benzyl)-2-oxo-2-(4-{2-[1-((S)-pyrrolidin-3-ylamino)-ethyl]-phenyl}-piperazin-1-yl)-ethyl]-amide
   Show/Hide
C35H43ClN6O2
 1
1
EC50 = 12 nM
   TI
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   TS
CP0849936
(3R,4R,5S)-1-{[(3S,4R)-1-tert-Butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]carbonyl}-3,5-dimethyl-4-phenylpiperidin-4-ol Hydrochloride
   Show/Hide
C28H37ClF2N2O2
 2
1
EC50 = 12 nM
   TI
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2
Ki = 27 nM
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CP0458784
2-[(1R)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-N,2-dimethylpropanamide
   Show/Hide
C34H44ClF2N3O2
 2
1
EC50 = 12 nM
   TI
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2
IC50 = 47 nM
   TI
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CP0853376
(S)-2-[(R)-2-(4-tert-Butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethylcarbamoyl]-4-methyl-piperazine-1-carboxylic acid tert-butyl ester
   Show/Hide
C35H54FN5O5
 2
1
EC50 = 13 nM
   TI
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2
IC50 = 18 nM
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CP0462980
(3R,5S)-N-[(2R)-1-[4-(tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-3,5-diethylpiperazine-1-carboxamide
   Show/Hide
C34H54FN5O3
 2
1
EC50 = 13 nM
   TI
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2
IC50 = 4.7 nM
   TI
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CP0162604
N-[(1S)-1-[2-[1-[(3R,4S)-4-(4-bromo-2-fluorophenyl)-1-tert-butylpyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C31H40BrClFN3O2
 2
1
EC50 = 13.4 nM
   TI
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2
IC50 = 4.1 nM
   TI
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CP0213531
(S)-4-(4-{2-[1-(Acetyl-ethyl-amino)-ethyl]-phenyl}-piperazin-1-yl)-3-(4-chloro-benzyl)-N-cyclobutyl-4-oxo-butyramide
   Show/Hide
C31H41ClN4O3
 1
1
EC50 = 15 nM
   TI
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CP0374520
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(R)-2-(4-{2-[1-((S)-2-amino-cyclohexylamino)-ethyl]-phenyl}-piperazin-1-yl)-1-(4-chloro-benzyl)-2-oxo-ethyl]-amide
   Show/Hide
C37H47ClN6O2
 1
1
EC50 = 15 nM
   TI
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   TS
CP0374304
((3R,4S)-4-(2,4-difluorophenyl)-1-(pyridin-2-yl)pyrrolidin-3-yl)((3S,4S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C29H31F2N3O2
 2
1
EC50 = 15 nM
   TI
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2
Ki = 79 nM
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CP0845517
(3R,4R,5S)-1-{[(3S,4R)-1-tert-Butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]carbonyl}-4-(3,4-difluorophenyl)-3,5-dimethylpiperidin-4-ol Hydrochloride
   Show/Hide
C28H35ClF4N2O2
 1
1
EC50 = 15 nM
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CP0440988
N-[(1S)-1-[2-[4-[(3S,4R)-4-(4-chlorophenyl)-1-propan-2-ylpyrrolidine-3-carbonyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]-3-(dimethylamino)propanamide
   Show/Hide
C34H50ClN5O2
 1
1
EC50 = 16 nM
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CP0440984
(2R)-2-amino-N-[(1S)-1-[2-[4-[(3S,4R)-4-(4-chlorophenyl)-1-(oxan-4-yl)pyrrolidine-3-carbonyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]propanamide
   Show/Hide
C34H48ClN5O3
 1
1
EC50 = 17 nM
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CP0415240
2-((S)-5-chloro-1'-((3S,4R)-4-(2,4-difluorophenyl)-1-(tetrahydro-2H-pyran-4-yl)pyrrolidine-3-carbonyl)-6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-3-yl)-2-methylpropanenitrile
   Show/Hide
C32H35ClF3N3O3
 2
1
EC50 = 17.1 nM
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2
IC50 = 7.3 nM
   TI
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CP0316843
N-[(1S)-1-[2-[1-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C31H40ClF2N3O2
 3
1
EC50 = 17.9 nM
   TI
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2
EC50 = 18 nM
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3
IC50 = 70 nM
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CP0393473
1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid ((R)-1-(4-chloro-benzyl)-2-{4-[2-((S)-2-methyl-5-(S)-methyl-piperazin-1-ylmethyl)-phenyl]-piperazin-1-yl}-2-oxo-ethyl)-amide
   Show/Hide
C36H45ClN6O2
 1
1
EC50 = 18 nM
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CP0402318
((3R,4S)-4-(2,4-difluorophenyl)-1-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl)((3S,4S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C29H36F2N2O3
 2
1
EC50 = 18 nM
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2
Ki = 36 nM
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CP0845107
(3R,4R,5S)-1-{[(3S,4R)-1-tert-Butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]carbonyl}-4-(4-fluorophenyl)-3,5-dimethylpiperidin-4-ol Hydrochloride
   Show/Hide
C28H36ClF3N2O2
 2
1
EC50 = 18 nM
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2
Ki = 36 nM
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CP0378158
(3R,5R)-N-[(2R)-1-[4-(tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-3,5-dimethylpiperazine-1-carboxamide
   Show/Hide
C32H50FN5O3
 2
1
EC50 = 18 nM
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2
IC50 = 11 nM
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CP0433110
N-[(1S)-1-[2-[4-[(3S,4R)-4-(4-chlorophenyl)-1-(oxan-4-yl)pyrrolidine-3-carbonyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]-2-(methylamino)acetamide
   Show/Hide
C34H48ClN5O3
 1
1
EC50 = 19 nM
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CP0505882
((3R,4S)-4-(2,4-difluorophenyl)-1-propylpyrrolidin-3-yl)((3S,4S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C27H34F2N2O2
 1
1
EC50 = 19 nM
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CP0378167
(1S,4R,6R)-N-[(2R)-1-[4-(tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-2-azabicyclo[2.2.2]octane-6-carboxamide
   Show/Hide
C33H49FN4O3
 2
1
EC50 = 20 nM
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2
IC50 = 16 nM
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CP0440983
N-[(1S)-1-[2-[4-[(3S,4R)-4-(4-chlorophenyl)-1-propan-2-ylpyrrolidine-3-carbonyl]piperazin-1-yl]-3-fluorophenyl]-2-methylpropyl]-3-(dimethylamino)propanamide
   Show/Hide
C33H47ClFN5O2
 1
1
EC50 = 20 nM
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CP0845516
(3R,4R,5S)-1-{[(3S,4R)-4-(2,4-Difluorophenyl)-1-pyridazin-3-ylpyrrolidin-3-yl]carbonyl}-3,5-dimethyl-4-propylpiperidin-4-ol Hydrochloride
   Show/Hide
C25H33ClF2N4O2
 2
1
EC50 = 21 nM
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2
Ki = 56 nM
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CP0315803
(3S,5R)-N-[(2R)-1-[4-(tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-3,5-dimethylpiperazine-1-carboxamide
   Show/Hide
C32H50FN5O3
 2
1
EC50 = 22 nM
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2
IC50 = 4.9 nM
   TI
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CP0185277
(4-(2-((S)-1-amino-2-methylpropyl)-4-methylphenyl)piperazin-1-yl)((3S,4R)-4-(4-chlorophenyl)-1-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl)methanone
   Show/Hide
C31H43ClN4O2
 1
1
EC50 = 24 nM
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CP0440987
N-[(1S)-1-[2-[4-[(3S,4R)-4-(4-chlorophenyl)-1-propanoylpyrrolidine-3-carbonyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]-3-(dimethylamino)propanamide
   Show/Hide
C34H48ClN5O3
 1
1
EC50 = 27 nM
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CP0441550
2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-2-methyl-N-(2-methylpropyl)propanamide
   Show/Hide
C37H50ClF2N3O2
 2
1
EC50 = 27 nM
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2
IC50 = 6.6 nM
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CP0455734
2-[(1R)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-N-cyclopropyl-2-methylpropanamide
   Show/Hide
C36H46ClF2N3O2
 2
1
EC50 = 28 nM
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2
IC50 = 55 nM
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   TS
CP0877838
(S)-1-Methyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide dihydrochloride
   Show/Hide
C31H50Cl2FN5O3
 2
1
EC50 = 29 nM
   TI
   LI
   LO
   TS
2
IC50 = 87 nM
   TI
   LI
   LO
   TS
CP0539269
(2S)-1-[(3S,11S,14S,17S,20R,23S)-3-[[(2S)-2-acetamidohexanoyl]amino]-20-benzyl-17-[3-(diaminomethylideneamino)propyl]-14-(1H-indol-3-ylmethyl)-2,5,13,16,19,22-hexaoxo-1,6,12,15,18,21-hexazabicyclo[21.3.0]hexacosane-11-carbonyl]-N-[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]pyrrolidine-2-carboxamide
   Show/Hide
C59H85N15O11
 1
1
EC50 = 29 nM
   TI
   LI
   LO
   TS
CP0401418
((3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4R,5R)-4-(4-chlorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)methanone
   Show/Hide
C28H35ClF2N2O2
 2
1
EC50 = 30 nM
   TI
   LI
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   TS
2
Ki = 48 nM
   TI
   LI
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   TS
CP0374305
((3R,4S)-1-cyclobutyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C28H34F2N2O2
 2
1
EC50 = 32 nM
   TI
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   TS
2
Ki = 62 nM
   TI
   LI
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   TS
CP0425031
2-[(1R)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-N-ethyl-2-methylpropanamide
   Show/Hide
C35H46ClF2N3O2
 2
1
EC50 = 32 nM
   TI
   LI
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   TS
2
IC50 = 53 nM
   TI
   LI
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   TS
CP0398563
2-((S)-6-chloro-1'-((3S,4R)-4-(2,4-difluorophenyl)-1-(pentan-3-yl)pyrrolidine-3-carbonyl)-5-methyl-3H-spiro[isobenzofuran-1,4'-piperidine]-3-yl)-2-methylpropanenitrile
   Show/Hide
C33H40ClF2N3O2
 2
1
EC50 = 33.6 nM
   TI
   LI
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   TS
2
IC50 = 11.9 nM
   TI
   LI
   LO
   TS
CP0440318
1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(R)-2-(4-{2-[1-(4-amino-cyclohexylamino)-ethyl]-phenyl}-piperazin-1-yl)-1-(4-chloro-benzyl)-2-oxo-ethyl]-amide
   Show/Hide
C37H47ClN6O2
 1
1
EC50 = 34 nM
   TI
   LI
   LO
   TS
CP0406610
(1S,4R,6S)-2-Methyl-2-aza-bicyclo[2.2.2]octane-6-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide
   Show/Hide
C34H51FN4O3
 2
1
EC50 = 34 nM
   TI
   LI
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   TS
2
IC50 = 6 nM
   TI
   LI
   LO
   TS
CP0853375
(S)-4-Isobutyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide; compound with 2 TFA
   Show/Hide
C38H56F7N5O7
 2
1
EC50 = 34 nM
   TI
   LI
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   TS
2
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0485035
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(R)-1-(4-chloro-benzyl)-2-(4-{2-[(3-hydroxy-propylamino)-methyl]-phenyl}-piperazin-1-yl)-2-oxo-ethyl]-amide
   Show/Hide
C33H40ClN5O3
 1
1
EC50 = 36 nM
   TI
   LI
   LO
   TS
CP0408646
N-[(2R)-3-(4-chlorophenyl)-1-[4-cyclohexyl-4-(1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-1-oxopropan-2-yl]-3-(dimethylamino)propanamide
   Show/Hide
C28H41ClN6O2
 1
1
EC50 = 40 nM
   TI
   LI
   LO
   TS
CP0421162
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-(2-{[(2-hydroxy-ethyl)-methyl-amino]-methyl}-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C33H40ClN5O3
 1
1
EC50 = 40 nM
   TI
   LI
   LO
   TS
CP0915219
(3R,4R,5S)-1-{[(3S,4R)-4-(2,4-Difluorophenyl)-1-isopropylpyrrolidin-3-yl]carbonyl}-4-(3-fluorophenyl)-3,5-dimethylpiperidin-4-ol Hydrochloride
   Show/Hide
C27H34ClF3N2O2
 1
1
EC50 = 40 nM
   TI
   LI
   LO
   TS
CP0458339
N-benzyl-2-[(1S)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-2-methylpropanamide
   Show/Hide
C40H48ClF2N3O2
 2
1
EC50 = 42 nM
   TI
   LI
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   TS
2
IC50 = 12 nM
   TI
   LI
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   TS
CP0372779
N-[(1S)-1-[2-[4-[(3S,4R)-1-acetyl-4-(4-chlorophenyl)pyrrolidine-3-carbonyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]-3-(dimethylamino)propanamide
   Show/Hide
C33H46ClN5O3
 1
1
EC50 = 44 nM
   TI
   LI
   LO
   TS
CP0874910
(+/-)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-3-methoxy-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-(4-fluorophenyl)N-isopropylacetamide
   Show/Hide
C31H30FN5O4
 1
1
EC50 = 44.67 nM
   TI
   LI
   LO
   TS
CP0462856
((3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4R,5R)-4-(2,6-difluorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)methanone
   Show/Hide
C28H34F4N2O2
 2
1
EC50 = 45 nM
   TI
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   TS
2
Ki = 99 nM
   TI
   LI
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   TS
CP0402317
((3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4R,5R)-4-hydroxy-3,5-dimethyl-4-(pyridin-2-yl)piperidin-1-yl)methanone
   Show/Hide
C27H35F2N3O2
 2
1
EC50 = 46 nM
   TI
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   TS
2
Ki = 350 nM
   TI
   LI
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   TS
CP0421163
1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-(2-{[(2-methoxy-ethyl)-methyl-amino]-methyl}-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C34H42ClN5O3
 1
1
EC50 = 51 nM
   TI
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   TS
CP0858959
(3R,4R,5S)-4-(2,4-Difluorophenyl)-1-{[(3S,4R)-4-(2,4-difluorophenyl)-1-ethylpyrrolidin-3-yl]carbonyl}-3,5-dimethylpiperidin-4-ol Hydrochloride
   Show/Hide
C26H31ClF4N2O2
 1
1
EC50 = 51 nM
   TI
   LI
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   TS
CP0406608
(1S,4S,6S)-2-Aza-bicyclo[2.2.2]octane-6-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide
   Show/Hide
C33H49FN4O3
 2
1
EC50 = 52 nM
   TI
   LI
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   TS
2
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0869660
(S)-4-(2,2-Difluoro-ethyl)-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide; compound with 2 TFA
   Show/Hide
C36H50F9N5O7
 2
1
EC50 = 52 nM
   TI
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   TS
2
IC50 = 13 nM
   TI
   LI
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   TS
CP0895694
(S)-4-Ethyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide; compound with 2 TFA
   Show/Hide
C36H52F7N5O7
 2
1
EC50 = 52 nM
   TI
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   TS
2
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0520424
((3S,4R)-4-(2,4-difluorophenyl)-1-isopropylpyrrolidin-3-yl)((3S,4R,5R)-4-(4-fluorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)methanone
   Show/Hide
C27H33F3N2O2
 1
1
EC50 = 52 nM
   TI
   LI
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   TS
CP0859527
(3R,4R,5S)-1-{[(3S,4R)-1-tert-Butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]carbonyl}-4-(4-methoxyphenyl)-3,5-dimethylpiperidin-4-ol Hydrochloride
   Show/Hide
C29H39ClF2N2O3
 1
1
EC50 = 53 nM
   TI
   LI
   LO
   TS
CP0377057
2-[(1R)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-N,N,2-trimethylpropanamide
   Show/Hide
C35H46ClF2N3O2
 2
1
EC50 = 53 nM
   TI
   LI
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   TS
2
IC50 = 59 nM
   TI
   LI
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   TS
CP0374306
((3R,4S)-1-cyclopropyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C27H32F2N2O2
 2
1
EC50 = 55 nM
   TI
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   TS
2
Ki = 290 nM
   TI
   LI
   LO
   TS
CP0422856
(3S,5S)-N-[(2R)-1-[4-(tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-3,5-dimethylpiperazine-1-carboxamide
   Show/Hide
C32H50FN5O3
 2
1
EC50 = 58 nM
   TI
   LI
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   TS
2
IC50 = 12 nM
   TI
   LI
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   TS
CP0438966
(3R,5S)-N-[(2R)-1-[4-(tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-3,4,5-trimethylpiperazine-1-carboxamide
   Show/Hide
C33H52FN5O3
 2
1
EC50 = 60 nM
   TI
   LI
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   TS
2
IC50 = 16 nM
   TI
   LI
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   TS
CP0391026
((3S,4R)-4-(2,4-difluorophenyl)-1-ethylpyrrolidin-3-yl)((3S,4R,5R)-4-(3-fluorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)methanone
   Show/Hide
C26H31F3N2O2
 2
1
EC50 = 61 nM
   TI
   LI
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   TS
2
Ki = 355 nM
   TI
   LI
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   TS
CP0391042
((3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4R,5R)-4-(2,4-difluorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)methanone
   Show/Hide
C28H34F4N2O2
 2
1
EC50 = 62 nM
   TI
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   LO
   TS
2
Ki = 176 nM
   TI
   LI
   LO
   TS
CP0394884
N-[(1S)-1-[2-[1-[(3S,4R)-1-tert-butyl-4-[4-(trifluoromethyl)phenyl]pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C32H41ClF3N3O2
 2
1
EC50 = 67.2 nM
   TI
   LI
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   TS
2
IC50 = 28.1 nM
   TI
   LI
   LO
   TS
CP0383468
((3S,4R)-4-(2,4-difluorophenyl)-1-isopropylpyrrolidin-3-yl)((3S,4R,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C27H34F2N2O2
 2
1
EC50 = 69 nM
   TI
   LI
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   TS
2
Ki = 114 nM
   TI
   LI
   LO
   TS
CP0921462
(3R,4R,5S)-4-(3,4-Difluorophenyl)-1-{[(3S,4R)-4-(2,4-difluorophenyl)-1-ethylpyrrolidin-3-yl]carbonyl}-3,5-dimethylpiperidin-4-ol Hydrochloride
   Show/Hide
C26H31ClF4N2O2
 1
1
EC50 = 69 nM
   TI
   LI
   LO
   TS
CP0374532
1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid ((R)-1-(4-chloro-benzyl)-2-{4-[2-(1-cyclopentylamino-ethyl)-phenyl]-piperazin-1-yl}-2-oxo-ethyl)-amide
   Show/Hide
C36H44ClN5O2
 1
1
EC50 = 72 nM
   TI
   LI
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   TS
CP0383452
((3R,4S)-4-(2,4-difluorophenyl)-1-isobutylpyrrolidin-3-yl)((3S,4S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C28H36F2N2O2
 1
1
EC50 = 73 nM
   TI
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   TS
CP0398564
2-((3S)-6-chloro-1'-((3S,4R)-4-(2,4-difluorophenyl)-1-(1-methoxypropan-2-yl)pyrrolidine-3-carbonyl)-5-methyl-3H-spiro[isobenzofuran-1,4'-piperidine]-3-yl)-2-methylpropanenitrile
   Show/Hide
C32H38ClF2N3O3
 2
1
EC50 = 73.2 nM
   TI
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   TS
2
IC50 = 44.3 nM
   TI
   LI
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   TS
CP0383642
2-((S)-6-chloro-1'-((3S,4R)-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl)-5-methyl-3H-spiro[isobenzofuran-1,4'-piperidine]-3-yl)-2-methylpropanenitrile
   Show/Hide
C28H30ClF2N3O2
 2
1
EC50 = 78.1 nM
   TI
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   TS
2
IC50 = 15 nM
   TI
   LI
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   TS
CP0454311
N-[(1S)-1-[2-[4-[(3S,4R)-4-(4-chlorophenyl)pyrrolidine-3-carbonyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]-3-(dimethylamino)propanamide
   Show/Hide
C31H44ClN5O2
 1
1
EC50 = 79 nM
   TI
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   TS
CP0509361
((3R,4S)-1-(cyclopropylmethyl)-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C28H34F2N2O2
 1
1
EC50 = 81 nM
   TI
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   TS
CP0918361
(R)-4-Methyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide dihydrochloride
   Show/Hide
C31H50Cl2FN5O3
 2
1
EC50 = 82 nM
   TI
   LI
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   TS
2
IC50 = 52 nM
   TI
   LI
   LO
   TS
CP0849935
(3R,4R,5S)-4-Cyclopropyl-1-{[(3S,4R)-4-(2,4-difluorophenyl)-1-pyridazin-3-ylpyrrolidin-3-yl]carbonyl}-3,5-dimethylpiperidin-4-ol Hydrochloride
   Show/Hide
C25H31ClF2N4O2
 2
1
EC50 = 82 nM
   TI
   LI
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   TS
2
Ki = 172 nM
   TI
   LI
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   TS
CP0925815
(3R,4R,5S)-1-{[(3S,4R)-4-(2,4-Difluorophenyl)-1-ethylpyrrolidin-3-yl]carbonyl}-3,5-dimethyl-4-phenylpiperidin-4-ol Hydrochloride
   Show/Hide
C26H33ClF2N2O2
 1
1
EC50 = 85 nM
   TI
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   TS
CP0382157
N-[(1S)-1-[2-[1-[(3S,4R)-1-tert-butyl-4-[2-fluoro-4-(trifluoromethyl)phenyl]pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C32H40ClF4N3O2
 2
1
EC50 = 88.8 nM
   TI
   LI
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   TS
2
IC50 = 22.7 nM
   TI
   LI
   LO
   TS
CP0896599
(3R,4R,5S)-1-{[(3S,4R)-4-(2,4-Difluorophenyl)-1-pyridazin-3-ylpyrrolidin-3-yl]carbonyl}-4-isopropyl-3,5-dimethylpiperidin-4-ol Hydrochloride
   Show/Hide
C25H33ClF2N4O2
 1
1
EC50 = 89 nM
   TI
   LI
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   TS
CP0421173
3-{2-[4-((R)-3-(4-Chloro-phenyl)-2-{[(R)-oxo-(1,2,3,4-tetrahydro-isoquinolin-3-yl)-methyl]-amino}-propionyl)-piperazin-1-yl]-benzylamino}-propionic acid
   Show/Hide
C33H38ClN5O4
 1
1
EC50 = 90 nM
   TI
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   TS
CP0421172
1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(R)-2-(4-{2-[(2-amino-ethylamino)-methyl]-phenyl}-piperazin-1-yl)-1-(4-chloro-benzyl)-2-oxo-ethyl]-amide
   Show/Hide
C32H39ClN6O2
 1
1
EC50 = 91 nM
   TI
   LI
   LO
   TS
CP0391023
((3S,4R,5R)-4-(4-chlorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)((3S,4R)-4-(2,4-difluorophenyl)-1-isopropylpyrrolidin-3-yl)methanone
   Show/Hide
C27H33ClF2N2O2
 1
1
EC50 = 91 nM
   TI
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   TS
CP0439009
1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(R)-1-(4-chloro-benzyl)-2-(4-{2-[(methyl-pyridin-3-ylmethyl-amino)-methyl]-phenyl}-piperazin-1-yl)-2-oxo-ethyl]-amide
   Show/Hide
C37H41ClN6O2
 1
1
EC50 = 94 nM
   TI
   LI
   LO
   TS
CP0493348
2-((S)-6-chloro-1'-((3S,4R)-4-(2,4-difluorophenyl)-1-((tetrahydro-2H-pyran-4-yl)methyl)pyrrolidine-3-carbonyl)-5-methyl-3H-spiro[isobenzofuran-1,4'-piperidine]-3-yl)-2-methylpropanenitrile
   Show/Hide
C34H40ClF2N3O3
 2
1
EC50 = 95.9 nM
   TI
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   TS
2
IC50 = 52.5 nM
   TI
   LI
   LO
   TS
CP0885254
(R)-3-(1H-Indazol-3-ylmethylene)-1-[2-oxoethyl-2-(2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)]-5-phenyl-1H-1,5-diazepine-2,4-dione
   Show/Hide
C31H29N5O3
 1
1
EC50 = 100 nM
   TI
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   TS
CP0449034
(4-(2-((S)-1-amino-2-methylpropyl)-4-methylphenyl)piperazin-1-yl)((3S,4R)-4-(4-chlorophenyl)-1-isopropylpyrrolidin-3-yl)methanone
   Show/Hide
C29H41ClN4O
 1
1
EC50 = 105 nM
   TI
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   TS
CP0374314
((3R,4S)-1-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C28H36F2N2O2
 2
1
EC50 = 105 nM
   TI
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   TS
2
Ki = 233 nM
   TI
   LI
   LO
   TS
CP0845518
(3R,4R,5S)-1-{[(3S,4R)-1-tert-Butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]carbonyl}-3,5-dimethyl-4-[4-(trifluoromethyl)phenyl]-piperidin-4-ol Hydrochloride
   Show/Hide
C29H36ClF5N2O2
 1
1
EC50 = 108 nM
   TI
   LI
   LO
   TS
CP0535084
N-[(1S)-1-[2-[1-[(3R,4S)-1-tert-butyl-4-(4-chloro-2-fluorophenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C31H40Cl2FN3O2
 2
1
EC50 = 110.8 nM
   TI
   LI
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   TS
2
IC50 = 13.23 nM
   TI
   LI
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   TS
CP0414895
((3R,4S)-4-(2,4-difluorophenyl)-1-(pyrazin-2-yl)pyrrolidin-3-yl)((3S,4S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C28H30F2N4O2
 1
1
EC50 = 111 nM
   TI
   LI
   LO
   TS
CP0401416
((3R,4S)-4-(2,4-difluorophenyl)-1-(pyrimidin-5-yl)pyrrolidin-3-yl)((3S,4S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C28H30F2N4O2
 1
1
EC50 = 117 nM
   TI
   LI
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   TS
CP0156912
N-[(1S)-1-[2-[1-[(3S,4R)-1-tert-butyl-4-naphthalen-2-ylpyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C35H44ClN3O2
 2
1
EC50 = 120.5 nM
   TI
   LI
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2
IC50 = 76.2 nM
   TI
   LI
   LO
   TS
CP0374312
((3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4R,5R)-4-hydroxy-3,5-dimethyl-4-propylpiperidin-1-yl)methanone
   Show/Hide
C25H38F2N2O2
 2
1
EC50 = 126 nM
   TI
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2
Ki = 844 nM
   TI
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CP0470207
((3S,4R,5R)-4-(4-chlorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)((3S,4R)-4-(2,4-difluorophenyl)-1-methylpyrrolidin-3-yl)methanone
   Show/Hide
C25H29ClF2N2O2
 1
1
EC50 = 130 nM
   TI
   LI
   LO
   TS
CP0437355
N-[(1S)-1-[2-[1-[(3S,4R)-1-tert-butyl-4-(2,4,5-trifluorophenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C31H39ClF3N3O2
 2
1
EC50 = 130.3 nM
   TI
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2
IC50 = 127.6 nM
   TI
   LI
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   TS
CP0393479
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-(2-{1-[(furan-2-ylmethyl)-amino]-ethyl}-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C36H40ClN5O3
 1
1
EC50 = 138 nM
   TI
   LI
   LO
   TS
CP0393472
1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid ((R)-1-(4-chloro-benzyl)-2-oxo-2-{4-[2-(4-pyrrolidin-1-yl-piperidin-1-ylmethyl)-phenyl]-piperazin-1-yl}-ethyl)-amide
   Show/Hide
C39H49ClN6O2
 1
1
EC50 = 146 nM
   TI
   LI
   LO
   TS
CP0919470
(3R,4R,5S)-1-{[(3S,4R)-4-(2,4-Difluorophenyl)-1-ethylpyrrolidin-3-yl]carbonyl}-4-(4-fluorophenyl)-3,5-dimethylpiperidin-4-ol Hydrochloride
   Show/Hide
C26H32ClF3N2O2
 1
1
EC50 = 147 nM
   TI
   LI
   LO
   TS
CP0873909
(+/-)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-N-(2-methyl-4-trifluoromethoxy)phenyl)acetamide
   Show/Hide
C31H28F3N5O4
 1
1
EC50 = 151.36 nM
   TI
   LI
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   TS
CP0437354
N-[(1S)-1-[2-[1-[(3S,4R)-1-tert-butyl-4-(2,4-dichlorophenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C31H40Cl3N3O2
 2
1
EC50 = 155.6 nM
   TI
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2
IC50 = 17.9 nM
   TI
   LI
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   TS
CP0509360
((3S,4R)-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4R,5R)-4-(3-fluorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)methanone
   Show/Hide
C24H27F3N2O2
 1
1
EC50 = 159 nM
   TI
   LI
   LO
   TS
CP0487168
1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-(2-cyclopentylaminomethyl-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C35H42ClN5O2
 1
1
EC50 = 164 nM
   TI
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   TS
CP0391988
(1R,4S,6S)-2-Methyl-2-aza-bicyclo[2.2.2]octane-6-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide
   Show/Hide
C34H51FN4O3
 2
1
EC50 = 165 nM
   TI
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2
IC50 = 28 nM
   TI
   LI
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   TS
CP0846176
(+/-)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-3-methoxy-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-(4-methoxyphenyl)N-isopropylacetamide
   Show/Hide
C32H33N5O5
 1
1
EC50 = 165.96 nM
   TI
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   TS
CP0440312
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid ((R)-1-(4-chloro-benzyl)-2-{4-[2-(1-cyclopropylamino-ethyl)-phenyl]-piperazin-1-yl}-2-oxo-ethyl)-amide
   Show/Hide
C34H40ClN5O2
 1
1
EC50 = 174 nM
   TI
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   TS
CP0846974
(+/-)-2-[2,4-Dioxo-3-(6-fluoro-1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-(4-fluorophenyl)-N-isopropylacetamide
   Show/Hide
C30H27F2N5O3
 1
1
EC50 = 177.83 nM
   TI
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   TS
CP0471478
N-[2-[4-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]piperazin-1-yl]-3,3-dimethylbutyl]-N-propan-2-ylacetamide
   Show/Hide
C30H48F2N4O2
 2
1
EC50 = 180 nM
   TI
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2
IC50 = 150 nM
   TI
   LI
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   TS
CP0374527
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-(2-{[methyl-(2-pyridin-2-yl-ethyl)-amino]-methyl}-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C38H43ClN6O2
 1
1
EC50 = 190 nM
   TI
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   TS
CP0398562
2-((R)-1'-((3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl)-6-chloro-5-methyl-3H-spiro[isobenzofuran-1,4'-piperidine]-3-yl)-2-methylpropanenitrile
   Show/Hide
C32H38ClF2N3O2
 2
1
EC50 = 195.6 nM
   TI
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2
IC50 = 31.4 nM
   TI
   LI
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   TS
CP0446667
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-oxo-2-[4-(2-{[(piperidin-4-ylmethyl)-amino]-methyl}-phenyl)-piperazin-1-yl]-ethyl}-amide
   Show/Hide
C36H45ClN6O2
 1
1
EC50 = 208 nM
   TI
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   TS
CP0435806
N-[(1S)-1-[2-[1-[(3S,4R)-1-tert-butyl-4-(2-chloro-4-fluorophenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C31H40Cl2FN3O2
 2
1
EC50 = 214.5 nM
   TI
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   TS
2
IC50 = 216.2 nM
   TI
   LI
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   TS
CP0383453
((3S,4R)-4-(2,4-difluorophenyl)-1-isopropylpyrrolidin-3-yl)((3S,4R,5R)-4-(2,4-difluorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)methanone
   Show/Hide
C27H32F4N2O2
 1
1
EC50 = 220 nM
   TI
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   TS
CP0391989
(1S,4R,6S)-2-Aza-bicyclo[2.2.2]octane-6-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide
   Show/Hide
C33H49FN4O3
 2
1
EC50 = 238 nM
   TI
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2
IC50 = 41 nM
   TI
   LI
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CP0370128
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-(2-diethylaminomethyl-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C34H42ClN5O2
 1
1
EC50 = 240 nM
   TI
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   TS
CP0400327
((3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)(4-(1-cyclohexyl-2-(isopropylamino)ethyl)piperazin-1-yl) methanone
   Show/Hide
C30H48F2N4O
 2
1
EC50 = 240 nM
   TI
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2
IC50 = 310 nM
   TI
   LI
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   TS
CP0374303
((3R,4S)-4-(2,4-difluorophenyl)-1-(pyrimidin-2-yl)pyrrolidin-3-yl)((3S,4S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C28H30F2N4O2
 2
1
EC50 = 243 nM
   TI
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2
Ki = 300 nM
   TI
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CP0458030
N-[(1S)-1-[2-[1-[(3R,4S)-1-tert-butyl-4-(2-fluoro-4-methoxyphenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C32H43ClFN3O3
 2
1
EC50 = 244.7 nM
   TI
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2
IC50 = 37.2 nM
   TI
   LI
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CP0485972
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-(2-cyclopropylaminomethyl-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C33H38ClN5O2
 1
1
EC50 = 253 nM
   TI
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   TS
CP0539614
((3S,4R)-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4R,5R)-4-(4-fluorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)methanone
   Show/Hide
C24H27F3N2O2
 1
1
EC50 = 255 nM
   TI
   LI
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   TS
CP0383425
((3S,4R)-4-(2,4-difluorophenyl)-1-isopropylpyrrolidin-3-yl)((3S,4R,5R)-4-(3,4-difluorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)methanone
   Show/Hide
C27H32F4N2O2
 1
1
EC50 = 257 nM
   TI
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CP0378443
(4-(2-((S)-1-amino-2-methylpropyl)-6-fluorophenyl)piperazin-1-yl)((3S,4R)-4-(4-chlorophenyl)-1-isopropylpyrrolidin-3-yl)methanone
   Show/Hide
C28H38ClFN4O
 1
1
EC50 = 270 nM
   TI
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CP0918363
(S)-4-(2-Amino-propionyl)-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide; compound with 2 TFA
   Show/Hide
C37H53F7N6O8
 2
1
EC50 = 270 nM
   TI
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2
IC50 = 30 nM
   TI
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CP0160526
(R)-N-((R)-1-(4-(2-(aminomethyl)phenyl)piperazin-1-yl)-3-(4-chlorophenyl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C30H34ClN5O2
 1
1
EC50 = 274 nM
   TI
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CP0509500
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-(2-{[(furan-2-ylmethyl)-amino]-methyl}-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C35H38ClN5O3
 1
1
EC50 = 274 nM
   TI
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CP0874312
(+/-)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-(4-fluorophenyl)-Nisopropylacetamide
   Show/Hide
C30H28FN5O3
 1
1
EC50 = 281.84 nM
   TI
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CP0391024
((3S,4R,5R)-4-(3,4-difluorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)((3S,4R)-4-(2,4-difluorophenyl)pyrrolidin-3-yl)methanone
   Show/Hide
C24H26F4N2O2
 1
1
EC50 = 288 nM
   TI
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   TS
CP0497004
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid ((R)-1-(4-chloro-benzyl)-2-oxo-2-{4-[2-(4-phenyl-piperazin-1-ylmethyl)-phenyl]-piperazin-1-yl}-ethyl)-amide
   Show/Hide
C40H45ClN6O2
 1
1
EC50 = 300 nM
   TI
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CP0493928
2-[(1R)-1'-[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]-5-chloro-6-methylspiro[1,2-dihydroindene-3,4'-piperidine]-1-yl]-2-methyl-N-(2,2,2-trifluoroethyl)propanamide
   Show/Hide
C35H43ClF5N3O2
 2
1
EC50 = 307 nM
   TI
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2
IC50 = 93 nM
   TI
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CP0874693
(+/-)-3-(1H-Indazol-3-ylmethylene)-1-[2-oxoethyl-2-(2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)]-5-phenyl-1H-1,5-diazepine-2,4-dione
   Show/Hide
C31H29N5O3
 1
1
EC50 = 323.59 nM
   TI
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CP0897229
(R)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-N-(4-methoxyphenyl)acetamide
   Show/Hide
C31H31N5O4
 1
1
EC50 = 338.84 nM
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CP0454313
3-(dimethylamino)-N-[(1S)-1-[3-fluoro-2-[4-[(3S,4R)-4-[3-fluoro-4-(trifluoromethyl)phenyl]-1-propan-2-ylpyrrolidine-3-carbonyl]piperazin-1-yl]phenyl]-2-methylpropyl]propanamide
   Show/Hide
C34H46F5N5O2
 1
1
EC50 = 340 nM
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CP0504289
4-((3S,4R,5R)-1-((3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl)-4-hydroxy-3,5-dimethylpiperidin-4-yl)benzonitrile
   Show/Hide
C29H35F2N3O2
 1
1
EC50 = 347 nM
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CP0453782
N-[2-[(1R)-5-chloro-1'-[(3S,4R)-4-(2,4-difluorophenyl)-1-(oxan-4-yl)pyrrolidine-3-carbonyl]-6-methylspiro[1H-2-benzofuran-3,4'-piperidine]-1-yl]propan-2-yl]acetamide
   Show/Hide
C34H42ClF2N3O4
 2
1
EC50 = 351.7 nM
   TI
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2
IC50 = 150.7 nM
   TI
   LI
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CP0874344
(+/-)-2-[2,4-Dioxo-3-(6-fluoro-1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-N-(4-methoxyphenyl)acetamide
   Show/Hide
C31H30FN5O4
 1
1
EC50 = 354.81 nM
   TI
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CP0234420
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(R)-1-(4-chloro-benzyl)-2-oxo-2-(4-{2-[(2-thiophen-2-yl-ethylamino)-methyl]-phenyl}-piperazin-1-yl)-ethyl]-amide
   Show/Hide
C36H40ClN5O2S
 1
1
EC50 = 357 nM
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   TS
CP0401674
((3S,4R)-4-(2,4-difluorophenyl)-1-methylpyrrolidin-3-yl)((3S,4R,5R)-4-(4-fluorophenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)methanone
   Show/Hide
C25H29F3N2O2
 2
1
EC50 = 365 nM
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2
Ki = 346 nM
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CP0507284
((3R,4S)-4-(2,4-difluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)((3S,4S,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C27H34F2N2O3
 1
1
EC50 = 374 nM
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CP0449031
(4-(2-((S)-1-amino-2-methylpropyl)-6-fluorophenyl)piperazin-1-yl)((3S,4R)-4-(4-chlorophenyl)-1-cyclopentylpyrrolidin-3-yl)methanone
   Show/Hide
C30H40ClFN4O
 1
1
EC50 = 400 nM
   TI
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CP0404969
N-[(1S)-1-[2-[4-[(3S,4R)-4-(3-chloro-4-fluorophenyl)-1-propan-2-ylpyrrolidine-3-carbonyl]piperazin-1-yl]-3-fluorophenyl]-2-methylpropyl]-3-(dimethylamino)propanamide
   Show/Hide
C33H46ClF2N5O2
 1
1
EC50 = 410 nM
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CP0861760
(+/-)-3-(6-Fluoro-1H-indazol-3-ylmethylene)-1-[2-oxoethyl-2-(2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)]-5-phenyl-1H-1,5-diazepine-2,4-dione
   Show/Hide
C31H28FN5O3
 1
1
EC50 = 436.52 nM
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CP0427925
(4-(2-((S)-1-amino-3-methylbutyl)-4-(trifluoromethyl)phenyl)piperazin-1-yl)((3S,4R)-1-isopropyl-4-(4-methoxyphenyl)pyrrolidin-3-yl)methanone
   Show/Hide
C31H43F3N4O2
 1
1
EC50 = 450 nM
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CP0485976
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-(2-{[2-(3-fluoro-phenyl)-ethylamino]-methyl}-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C38H41ClFN5O2
 1
1
EC50 = 460 nM
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CP0383467
((3S,4R)-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4R,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C24H28F2N2O2
 2
1
EC50 = 462 nM
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2
Ki = 264 nM
   TI
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   LO
   TS
CP0480693
1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-(2-{[2-(4-fluoro-phenyl)-ethylamino]-methyl}-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C38H41ClFN5O2
 1
1
EC50 = 487 nM
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CP0847013
(+/-)-2-[2,4-Dioxo-3-(6-fluoro-1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-N-phenylacetamide
   Show/Hide
C30H28FN5O3
 1
1
EC50 = 537.03 nM
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CP0357814
N-[(1S)-1-[2-[1-[(3R,4S)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C31H40ClF2N3O2
 2
1
EC50 = 565 nM
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2
IC50 = 640 nM
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CP0499970
((3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)(4-(1-cyclohexyl-2-(diethylamino)ethyl)piperazin-1-yl)methanone
   Show/Hide
C31H50F2N4O
 2
1
EC50 = 570 nM
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2
IC50 = 260 nM
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CP0522544
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(R)-1-(4-chloro-benzyl)-2-oxo-2-(4-{2-[1-(2-thiophen-2-yl-ethylamino)-ethyl]-phenyl}-piperazin-1-yl)-ethyl]-amide
   Show/Hide
C37H42ClN5O2S
 1
1
EC50 = 577 nM
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CP0514336
((3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4R,5R)-4-hydroxy-4-isopropyl-3,5-dimethylpiperidin-1-yl)methanone
   Show/Hide
C25H38F2N2O2
 1
1
EC50 = 626 nM
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CP0440310
(R)-1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [(R)-2-(4-{2-[(benzyl-methyl-amino)-methyl]-phenyl}-piperazin-1-yl)-1-(4-chloro-benzyl)-2-oxo-ethyl]-amide
   Show/Hide
C38H42ClN5O2
 1
1
EC50 = 632 nM
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CP0874634
3-[(3R,4R,5S)-1-{[(3S,4R)-1-tert-Butyl-4-(2,4-difluorophenyl)-pyrrolidin-3-yl]carbonyl}-4-hydroxy-3,5-dimethylpiperidin-4-yl]-benzonitrile Hydrochloride
   Show/Hide
C29H36ClF2N3O2
 1
1
EC50 = 644 nM
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CP0847012
(+/-)-2-[6-(6-Fluoro-1H-indazol-3-ylmethylene)-5,7-dioxo-4-(3-pyridinyl)-4,5,6,7-tetrahydro-1H-1,4-diazepin-1-yl]-N-(1-methylethyl)-N-[4-(methyloxy)phenyl]acetamide
   Show/Hide
C30H29FN6O4
 1
1
EC50 = 660.69 nM
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CP0885253
(+/-)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-N-(4-methoxyphenyl)acetamide
   Show/Hide
C31H31N5O4
 1
1
EC50 = 707.95 nM
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CP0469770
((3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)(4-(1-cyclohexyl-2-(dipropylamino)ethyl)piperazin-1-yl)methanone
   Show/Hide
C33H54F2N4O
 2
1
EC50 = 710 nM
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2
IC50 = 200 nM
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CP0858960
(3R,4R,5S)-1-{[(3S,4R)-4-(2,4-Difluorophenyl)-1-methylpyrrolidin-3-yl]carbonyl}-3,5-dimethyl-4-phenylpiperidin-4-ol Hydrochloride
   Show/Hide
C25H31ClF2N2O2
 2
1
EC50 = 717 nM
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2
Ki = 107 nM
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CP0873910
(S)-3-(1H-Indazol-3-ylmethylene)-1-[2-oxoethyl-2-(2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)]-5-phenyl-1H-1,5-diazepine-2,4-dione
   Show/Hide
C31H29N5O3
 1
1
EC50 = 794.33 nM
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CP0437137
1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-(2-{[2-(2-fluoro-phenyl)-ethylamino]-methyl}-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C38H41ClFN5O2
 1
1
EC50 = 910 nM
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CP0374315
((3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4R,5R)-4-cyclopropyl-4-hydroxy-3,5-dimethylpiperidin-1-yl)methanone
   Show/Hide
C25H36F2N2O2
 1
1
EC50 = 962 nM
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CP0381200
N-(4-hydroxyphenyl)-2-[6-(2H-indazol-3-ylmethyl)-5,7-dioxo-4-phenyl-1,4-diazepin-1-yl]-N-propan-2-ylacetamide
   Show/Hide
C30H29N5O4
 1
1
EC50 = 1000 nM
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CP0874311
2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-5-phenyl-2,3.4.5-tetrahydro-1H-1,5-diazepin-1-yl]-N-(4-hydroxyphenyl)-N-isopropylacetamide hydrochloride
   Show/Hide
C30H30ClN5O4
 1
1
EC50 = 1000 nM
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CP0453785
(3S,4R)-tert-butyl 3-((S)-6-chloro-3-(2-cyanopropan-2-yl)-5-methyl-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-ylcarbonyl)-4-(2,4-difluorophenyl)pyrrolidine-1-carboxylate
   Show/Hide
C33H38ClF2N3O4
 2
1
EC50 = 1006 nM
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2
IC50 = 479.2 nM
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CP0885306
(+/-)-2-(6-((1H-indazol-3-yl)methyl)-6-((1H-pyrazol-3-yl)methyl)-5,7-dioxo-4-phenyl-4,5,6,7-tetrahydro-1H-1,4-diazepin-1-yl)-N-isopropyl-N-(4-methoxyphenyl)acetamide
   Show/Hide
C35H35N7O4
 1
1
EC50 = 1047.13 nM
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CP0848954
(R)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-Nphenylacetamide
   Show/Hide
C30H29N5O3
 1
1
EC50 = 1071.52 nM
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CP0464913
(4-(2-((S)-1-amino-3-methylbutyl)-4-(trifluoromethyl)phenyl)piperazin-1-yl)((3S,4R)-4-(4-chlorophenyl)-1-isopropylpyrrolidin-3-yl)methanone
   Show/Hide
C30H40ClF3N4O
 1
1
EC50 = 1100 nM
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CP0373106
1-{[(3S,4R)-1-tert-Butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]-carbonyl}-4-phenylpiperidin-4-ol
   Show/Hide
C26H32F2N2O2
 1
1
EC50 = 1116 nM
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CP0921840
(R)-2-[2,4-Dioxo-3-(6-fluoro-1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-N-phenylacetamide
   Show/Hide
C30H28FN5O3
 1
1
EC50 = 1258.93 nM
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CP0379001
(4-(2-((S)-1-amino-2-methylpropyl)-6-fluorophenyl)piperazin-1-yl)((3S,4R)-4-(4-chlorophenyl)-1-isobutylpyrrolidin-3-yl)methanone
   Show/Hide
C29H40ClFN4O
 1
1
EC50 = 1400 nM
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CP0462566
1-((3S,4R)-3-(1-(2-((S)-1-amino-3-methylbutyl)-4-(trifluoromethyl)phenyl)piperazine-4-carbonyl)-4-(4-chlorophenyl)pyrrolidin-1-yl)ethanone
   Show/Hide
C29H36ClF3N4O2
 1
1
EC50 = 1900 nM
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CP0440574
N-[(1S)-1-[2-[1-[(3R,4S)-1-tert-butyl-4-naphthalen-2-ylpyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C35H44ClN3O2
 2
1
EC50 = 1922 nM
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2
IC50 = 528 nM
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CP0404723
1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-(2-{1-[2-(2-fluoro-phenyl)-ethylamino]-ethyl}-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C39H43ClFN5O2
 1
1
EC50 = 2060 nM
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CP0873848
(+/-)-2-[6-(1H-Indazol-3-ylmethyl)-5,7-dioxo-4-(3-pyridinyl)-4,5,6,7-tetrahydro-1H-1,4-diazepin-1-yl]-N-(1-methylethyl)-N-[4-(methyloxy)phenyl]acetamide
   Show/Hide
C30H30N6O4
 1
1
EC50 = 2884.03 nM
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CP0874694
(+/-)-2-[2,4-Dioxo-3-(1H-indazol-3-ylmethylene)-5-phenyl-2,3,4,5-tetrahydro-1H-1,5-diazepin-1-yl]-N-isopropyl-Nphenylacetamide
   Show/Hide
C30H29N5O3
 1
1
EC50 = 3235.94 nM
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CP0849922
(3R,4R,5S)-1-{[(3S,4R)-1-tert-Butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]carbonyl}-3,5-dimethyl-4-pyridin-3-ylpiperidin-4-ol Dihydrochloride
   Show/Hide
C27H37Cl2F2N3O2
 1
1
EC50 = 3630 nM
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CP0458029
N-[(1S)-1-[2-[1-[(3R,4S)-1-tert-butyl-4-(2,4,5-trifluorophenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C31H39ClF3N3O2
 2
1
EC50 = 3702 nM
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2
IC50 = 101.1 nM
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CP0896614
(1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)((3S,4s,5R)-4-hydroxy-3,5-dimethyl-4-phenylpiperidin-1-yl)methanone
   Show/Hide
C28H36F2N2O2
 1
1
EC50 = 3900 nM
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CP0426053
((3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl)(4-(1-cyclohexyl-2-(diisobutylamino)ethyl)piperazin-1-yl) methanone
   Show/Hide
C35H58F2N4O
 2
1
EC50 = 6700 nM
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2
IC50 = 1900 nM
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CP0427926
(4-(2-((S)-1-amino-3-methylbutyl)-4-(trifluoromethyl)phenyl)piperazin-1-yl)((3S,4R)-1-benzyl-4-(4-chlorophenyl)pyrrolidin-3-yl)methanone
   Show/Hide
C34H40ClF3N4O
 1
1
EC50 = 7300 nM
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CP0510106
(3R,4S,5S)-1-{[(3R,4S)-1-tert-Butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]carbonyl}-3,5-dimethyl-4-phenylpiperidin-4-ol
   Show/Hide
C28H36F2N2O2
 1
1
EC50 > 10000 nM
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CP0920690
(3R,4R,5S)-1-{[(3S,4R)-1-tert-Butyl-4-(2,4-difluorophenyl)-pyrrolidin-3-yl]carbonyl}-3,5-dimethyl-4-pyrimidin-5-ylpiperidin-4-ol Dihydrochloride
   Show/Hide
C26H36Cl2F2N4O2
 1
1
EC50 = 11100 nM
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CP0041451
CAS_75921-69-6
   Show/Hide
C78H111N21O19
 1
1
IC50 = 0.15 nM
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CP0375025
(4S)-4-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]hexanoylamino]-5-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-6-amino-1-[(2S)-2-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
   Show/Hide
C78H111N21O19
 2
1
IC50 = 0.16 nM
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2
Ki = 0.14 nM
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CP0459400
(3R)-N-[(2R)-3-(4-chlorophenyl)-1-{4-cyclohexyl-4-[(1-methyl-1H-1,2,3,4-tetrazol-5-yl)methyl]piperidin-1-yl}-1-oxopropan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C33H42ClN7O2
 1
1
IC50 = 0.3 nM
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CP0150320
1-[(R)-2-[((1S,2S)-1-Amino-1,2,3,4-tetrahydro-naphthalene-2-carbonyl)-amino]-3-(4-chloro-phenyl)-propionyl]-4-cyclohexyl-piperidine-4-carboxylic acid tert-butylamide
   Show/Hide
C36H49ClN4O3
 1
1
IC50 = 0.37 nM
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CP0537689
1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-amide
   Show/Hide
C33H41ClN6O2
 1
1
IC50 = 0.5 nM
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CP0497448
1-[2-[((R)-3-Amino-1,2,3,4-tetrahydro-naphthalene-2-carbonyl)-amino]-3-(4-chloro-phenyl)-propionyl]-4-cyclohexyl-piperidine-4-carboxylic acid tert-butylamide
   Show/Hide
C36H49ClN4O3
 1
1
IC50 = 0.56 nM
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CP0376413
(R)-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-cyclohexyl-4-(5,5-dimethyl-1,1-dioxo-1lambda*6*-isothiazolidin-2-ylmethyl)-piperidin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C36H49ClN4O4S
 1
1
IC50 = 0.62 nM
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CP0405831
1-[(R)-2-[((1R,2R)-1-Amino-1,2,3,4-tetrahydro-naphthalene-2-carbonyl)-amino]-3-(4-chloro-phenyl)-propionyl]-4-cyclohexyl-piperidine-4-carboxylic acid tert-butylamide
   Show/Hide
C36H49ClN4O3
 1
1
IC50 = 0.77 nM
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CP0378160
(3S,5R)-N-[(2R)-1-[4-(tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-chlorophenyl)-1-oxopropan-2-yl]-3,5-dimethylpiperazine-1-carboxamide
   Show/Hide
C32H50ClN5O3
 1
1
IC50 = 0.78 nM
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CP0451850
(R)-N-((R)-3-(4-chlorophenyl)-1-(4-cyclohexyl-4-((4,4-dimethyl-2-oxooxazolidin-3-yl)methyl)piperidin-1-yl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C36H47ClN4O4
 1
1
IC50 = 0.8 nM
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CP0432760
(R)-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-cyclohexyl-4-(1,1-dioxo-1lambda*6*-isothiazolidin-2-ylmethyl)-piperidin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C34H45ClN4O4S
 1
1
IC50 = 0.91 nM
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CP0466894
1-[(R)-2-[((1S,2S)-1-Amino-1-methyl-1,2,3,4-tetrahydro-naphthalene-2-carbonyl)-amino]-3-(4-chloro-phenyl)-propionyl]-4-cyclohexyl-piperidine-4-carboxylic acid tert-butylamide
   Show/Hide
C37H51ClN4O3
 1
1
IC50 = 1.1 nM
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CP0493433
1-[(2R)-2-[(5-amino-6,7,8,9-tetrahydro-5H-benzo[7]annulene-6-carbonyl)amino]-3-(4-chlorophenyl)propanoyl]-N-tert-butyl-4-cyclohexylpiperidine-4-carboxamide
   Show/Hide
C37H51ClN4O3
 1
1
IC50 = 1.1 nM
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CP0490856
(R)-N-((R)-3-(4-chlorophenyl)-1-(4-cyclohexyl-4-((2-methyl-2H-tetrazol-5-yl)methyl)piperidin-1-yl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C33H42ClN7O2
 1
1
IC50 = 1.2 nM
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CP0573125
(R)-1,2,3,4-Tetrahydro-quinoline-2-carboxylic acid [(R)-1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-amide
   Show/Hide
C33H41ClN6O2
 1
1
IC50 = 1.2 nM
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CP0376350
(R)-N-((R)-3-(4-chlorophenyl)-1-(4-cyclohexyl-4-(((R)-4-methyl-2-oxooxazolidin-3-yl)methyl)piperidin-1-yl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C35H45ClN4O4
 1
1
IC50 = 1.3 nM
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CP0490759
1-[2-[((R)-1-Amino-indane-2-carbonyl)-amino]-3-(4-chloro-phenyl)-propionyl]-4-cyclohexyl-piperidine-4-carboxylic acid tert-butylamide
   Show/Hide
C35H47ClN4O3
 1
1
IC50 = 1.9 nM
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CP0376349
(R)-N-((R)-3-(4-chlorophenyl)-1-(4-cyclohexyl-4-((N-isopropylmethan-2-ylsulfonamido)methyl)piperidin-1-yl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C35H49ClN4O4S
 1
1
IC50 = 2.1 nM
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CP0496616
3-[6-(4-Chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-N-(2-oxo-azepan-3-yl)-propionamide
   Show/Hide
C26H27ClN4O4S
 1
1
IC50 = 2.27 nM
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CP0463791
(4R,5S)-4-(4-Chloro-phenyl)-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
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C33H34Cl2N4O3S
 1
1
IC50 = 2.4 nM
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CP0847597
(2S,5S)-5-Ethyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide dihydrochloride
   Show/Hide
C32H52Cl2FN5O3
 1
1
IC50 = 3 nM
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CP0862697
(2S,5S)-5-Ethyl-4-methyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide dihydrochloride
   Show/Hide
C33H54Cl2FN5O3
 1
1
IC50 = 3 nM
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CP0404610
(4R,5S)-4-(2,4-Dichloro-phenyl)-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C33H33Cl3N4O3S
 1
1
IC50 = 3.2 nM
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CP0083437
N-[(1S)-1-[2-[1-[(3R,4S)-1-tert-butyl-4-(2,4-dichlorophenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C31H40Cl3N3O2
 1
1
IC50 = 3.3 nM
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CP0496773
(4R,5S)-4-(4-Trifluoromethyl-phenyl)-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C34H34ClF3N4O3S
 1
1
IC50 = 3.8 nM
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CP0501131
(R)-N-((R)-3-(4-chlorophenyl)-1-(4-cyclohexyl-4-((2-oxooxazolidin-3-yl)methyl)piperidin-1-yl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C34H43ClN4O4
 1
1
IC50 = 4 nM
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CP0845562
(2S,5S)-5-Isopropyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide dihydrochloride
   Show/Hide
C33H54Cl2FN5O3
 1
1
IC50 = 4 nM
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CP0376351
(R)-N-((R)-3-(4-chlorophenyl)-1-(4-cyclohexyl-4-((3-methyl-2-oxoimidazolidin-1-yl)methyl)piperidin-1-yl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C35H46ClN5O3
 1
1
IC50 = 4.3 nM
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CP0451849
(R)-N-((R)-3-(4-chlorophenyl)-1-(4-cyclohexyl-4-(((S)-4-methyl-2-oxooxazolidin-3-yl)methyl)piperidin-1-yl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C35H45ClN4O4
 1
1
IC50 = 4.5 nM
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CP0382075
(R)-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-cyclohexyl-4-(5-oxo-6-oxa-4-aza-spiro[2.4]hept-4-ylmethyl)-piperidin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C36H45ClN4O4
 1
1
IC50 = 4.6 nM
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CP0390506
(4R,5S)-4-(4-Fluoro-phenyl)-1-methyl-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C34H36ClFN4O3S
 1
1
IC50 = 4.7 nM
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CP0487182
(4R,5S)-4-p-Tolyl-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C34H37ClN4O3S
 1
1
IC50 = 4.7 nM
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CP0495900
(R)-N-((R)-3-(4-chlorophenyl)-1-(4-cyclohexyl-4-((2-oxoimidazolidin-1-yl)methyl)piperidin-1-yl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C34H44ClN5O3
 1
1
IC50 = 4.8 nM
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CP0849385
(2S,5S)-5-tert-Butyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide dihydrochloride
   Show/Hide
C34H56Cl2FN5O3
 1
1
IC50 = 5 nM
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CP0855524
(2S,5S)-5-(1-Methyl-cyclopropyl)-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide dihydrochloride
   Show/Hide
C34H54Cl2FN5O3
 1
1
IC50 = 5 nM
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CP0378159
(3R,5R)-N-[(2R)-1-[4-(tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-3,5-diethylpiperazine-1-carboxamide
   Show/Hide
C34H54FN5O3
 1
1
IC50 = 5.1 nM
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CP0507025
3-[6-(4-Chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-N-(2-phenoxy-ethyl)-propionamide
   Show/Hide
C28H26ClN3O4S
 1
1
IC50 = 5.598 nM
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CP0871300
(2S,5S)-5-Methyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide dihydrochloride
   Show/Hide
C31H50Cl2FN5O3
 1
1
IC50 = 6 nM
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CP0202448
N-[(1S)-1-[2-[1-[(3R,4S)-1-tert-butyl-4-[4-(trifluoromethyl)phenyl]pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C32H41ClF3N3O2
 1
1
IC50 = 7.8 nM
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CP0497207
(R)-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid {(R)-1-(4-chloro-benzyl)-2-[4-cyclohexyl-4-(6-oxo-7-oxa-5-aza-spiro[3.4]oct-5-ylmethyl)-piperidin-1-yl]-2-oxo-ethyl}-amide
   Show/Hide
C37H47ClN4O4
 1
1
IC50 = 7.9 nM
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CP0914841
(2S,5S)-5-Cyclopropyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide dihydrochloride
   Show/Hide
C33H52Cl2FN5O3
 1
1
IC50 = 8 nM
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CP0376348
ethyl N-[[1-[(2R)-3-(4-chlorophenyl)-2-[[(3R)-1,2,3,4-tetrahydroisoquinoline-3-carbonyl]amino]propanoyl]-4-cyclohexylpiperidin-4-yl]methyl]-N-propan-2-ylcarbamate
   Show/Hide
C37H51ClN4O4
 1
1
IC50 = 8.1 nM
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CP0452758
N-[(1S)-1-[2-[1-[(3R,4S)-1-tert-butyl-4-[2-fluoro-4-(trifluoromethyl)phenyl]pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C32H40ClF4N3O2
 1
1
IC50 = 9.8 nM
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CP0445633
(4R,5S)-4-(4-Fluoro-phenyl)-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C33H34ClFN4O3S
 1
1
IC50 = 11 nM
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CP0920216
(S)-6-Isopropyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide; compound with ditrifluoroacetic acid
   Show/Hide
C37H54F7N5O7
 1
1
IC50 = 11 nM
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CP0449079
(4R,5S)-4-(2-Fluoro-phenyl)-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C33H34ClFN4O3S
 1
1
IC50 = 13 nM
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CP0541585
(4R,5S)-4-Naphthalen-2-yl-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C37H37ClN4O3S
 1
1
IC50 = 17 nM
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CP0847598
(S)-4,7-Diaza-spiro[2.5]octane-6-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide; compound with ditrifluoroacetic acid
   Show/Hide
C36H50F7N5O7
 1
1
IC50 = 17 nM
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CP0480658
(4R,5S)-4-(4-Methoxy-phenyl)-pyrrolidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C33H35ClN4O4S
 1
1
IC50 = 19 nM
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CP0926680
(2S,5R)-5-Isopropyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide; compound with ditrifluoroacetic acid
   Show/Hide
C37H54F7N5O7
 1
1
IC50 = 20 nM
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CP0922716
(2S,5R)-5-(1-Methyl-cyclopropyl)-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide; compound with ditrifluoroacetic acid
   Show/Hide
C38H54F7N5O7
 1
1
IC50 = 24 nM
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CP0845644
(2S,5R)-5-Cyclopropyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide; compound with ditrifluoroacetic acid
   Show/Hide
C38H55F6N5O7
 1
1
IC50 = 25 nM
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CP0404631
6-(4-Chloro-phenylsulfanyl)-4-((R)-3-{[(4R,5S)-4-(4-fluoro-phenyl)-piperidin-3-ylmethyl]-amino}-butyl)-2-(4-methoxy-phenyl)-2H-pyridazin-3-one
   Show/Hide
C33H36ClFN4O2S
 1
1
IC50 = 28 nM
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CP0461509
(4R,5S)-4-p-Tolyl-pyrrolidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C33H35ClN4O3S
 1
1
IC50 = 28 nM
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CP0509648
(S)-1-(4-Fluoro-phenyl)-piperazine-2-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C32H33ClFN5O3S
 1
1
IC50 = 28 nM
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CP0874930
(2S,5R)-5-tert-Butyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide; compound with ditrifluoroacetic acid
   Show/Hide
C38H56F7N5O7
 1
1
IC50 = 29 nM
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CP0897048
(3R,4S)-4-Phenyl-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide hydrochloride
   Show/Hide
C33H36Cl2N4O3S
 1
1
IC50 = 33 nM
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CP0508757
(3R,4S)-4-Phenyl-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide; hydrochloride
   Show/Hide
C33H35ClN4O3S
 1
1
IC50 = 33 nM
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CP0058988
1-{2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine
   Show/Hide
C30H43ClN4O2
 1
1
IC50 = 35 nM
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CP0508758
(2S,3S)-3-(2,4-Dichloro-phenyl)-piperidine-4-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C33H33Cl3N4O3S
 1
1
IC50 = 36 nM
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CP0845645
(2S,5R)-5-Ethyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide; compound with ditrifluoroacetic acid
   Show/Hide
C36H52F7N5O7
 1
1
IC50 = 40 nM
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CP0376520
(3R,4S)-4-Phenyl-piperidine-3-carboxylic acid {3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C33H35ClN4O3S
 1
1
IC50 = 41 nM
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CP0374140
1-{2-[(1S)-(3-Azetidinylcarboxamido)-2-methylpropyl]-6-fluorophenyl}-4-[(2R)-methyl-3-(2-methoxy-4-chlorophenyl)propionyl]piperazine
   Show/Hide
C29H38ClFN4O3
 1
1
IC50 = 42 nM
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CP0508759
(4R,5S)-4-(3-Chloro-phenyl)-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C33H34Cl2N4O3S
 1
1
IC50 = 43 nM
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CP0445477
(4R,5S)-4-(4-Chloro-phenyl)-pyrrolidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C32H32Cl2N4O3S
 1
1
IC50 = 45 nM
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CP0445643
(2S,3S)-3-(4-Cyano-phenyl)-piperidine-4-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C34H34ClN5O3S
 1
1
IC50 = 45 nM
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CP0947432
(2S,5R)-5-Ethyl-4-methyl-piperazine-2-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide dihydrochloride
   Show/Hide
C33H54Cl2FN5O3
 1
1
IC50 = 46 nM
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CP0509671
(2S,3S)-3-(4-Chloro-phenyl)-piperidine-4-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C33H34Cl2N4O3S
 1
1
IC50 = 58 nM
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CP0541751
(4R,5S)-4-(2,4-Difluoro-phenyl)-pyrrolidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C32H31ClF2N4O3S
 1
1
IC50 = 60 nM
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CP0059383
N-[(1S)-1-[2-[4-[(3R,4S)-4-(4-chlorophenyl)-1-(oxan-4-yl)pyrrolidine-3-carbonyl]piperazin-1-yl]-5-methylphenyl]-2-methylpropyl]-3-(dimethylamino)propanamide
   Show/Hide
C36H52ClN5O3
 1
1
IC50 = 64 nM
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CP0145641
(4-(2-((S)-1-amino-2-methylpropyl)-4-methylphenyl)piperazin-1-yl)((3R,4S)-4-(4-chlorophenyl)-1-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl)methanone
   Show/Hide
C31H43ClN4O2
 1
1
IC50 = 65 nM
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CP0466535
(2S,3S)-3-(4-Fluoro-phenyl)-piperidine-4-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C33H34ClFN4O3S
 1
1
IC50 = 66 nM
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CP0390508
(4R,5S)-4-(4-Fluoro-phenyl)-pyrrolidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C32H32ClFN4O3S
 1
1
IC50 = 70 nM
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CP0876124
Ac-Nle4-cyclo(Asp5-His6-D-4-Dip-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C55H68N12O9
 1
1
IC50 = 74 nM
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CP0437356
N-[(1S)-1-[2-[1-[(3R,4S)-1-tert-butyl-4-(2-chloro-4-fluorophenyl)pyrrolidine-3-carbonyl]piperidin-4-yl]-5-chlorophenyl]propyl]acetamide
   Show/Hide
C31H40Cl2FN3O2
 1
1
IC50 = 82.2 nM
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CP0296428
1-{2-[(1S)-(methylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine
   Show/Hide
C29H41ClN4O2
 1
1
IC50 = 87 nM
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CP0541596
(4R,5S)-4-Naphthalen-1-yl-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C37H37ClN4O3S
 1
1
IC50 = 89 nM
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CP0358667
1-{2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl}-4-[(2R)-methyl-3-(2-methyl-4-chlorophenyl)propionyl]piperazine
   Show/Hide
C31H45ClN4O2
 1
1
IC50 = 92 nM
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CP0541732
N-[(2R)-4-[6-(4-chlorophenyl)sulfanyl-2-(4-methoxyphenyl)-3-oxopyridazin-4-yl]butan-2-yl]-4-(4-fluorophenyl)-N-methylpiperidine-3-carboxamide
   Show/Hide
C34H36ClFN4O3S
 1
1
IC50 = 93 nM
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CP0392706
(3R,4S)-4-Phenyl-pyrrolidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide; hydrochloride
   Show/Hide
C32H33ClN4O3S
 2
1
IC50 = 98 nM
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2
IC50 = 380 nM
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CP0390507
(4R,5S)-4-(3-Trifluoromethyl-phenyl)-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C34H34ClF3N4O3S
 1
1
IC50 = 100 nM
   TI
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CP0504921
(2S,3S)-3-(2-Fluoro-phenyl)-piperidine-4-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C33H34ClFN4O3S
 1
1
IC50 = 100 nM
   TI
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   LO
   TS
CP0373760
(2S)-2-amino-3-(1H-imidazol-4-yl)-N-[(2R)-1-{1-methanesulfonyl-1,2-dihydrospiro[indole-3,4'-piperidine]-1'-yl}-3-(naphthalen-2-yl)-1-oxopropan-2-yl]propanamide
   Show/Hide
C32H36N6O4S
 1
1
IC50 = 108 nM
   TI
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   LO
   TS
CP0461048
1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-amide
   Show/Hide
C33H41ClN6O2
 1
1
IC50 = 127 nM
   TI
   LI
   LO
   TS
CP0965108
(3S,4S)-3-Phenyl-piperidine-4-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide hydrochloride
   Show/Hide
C33H36Cl2N4O3S
 1
1
IC50 = 130 nM
   TI
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   TS
CP0445470
(3S,4S)-3-Phenyl-piperidine-4-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide; hydrochloride
   Show/Hide
C33H35ClN4O3S
 1
1
IC50 = 130 nM
   TI
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CP0480670
(4R,5S)-4-Thiophen-3-yl-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C31H33ClN4O3S2
 1
1
IC50 = 130 nM
   TI
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   TS
CP0448539
3-[6-(4-Chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-N-((R)-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-3-yl)-propionamide
   Show/Hide
C30H27ClN4O4S
 1
1
IC50 = 144 nM
   TI
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CP0386368
1-{2-[(1S)-(3-Dimethylaminopropionamino)-2-methylpropyl]-4-chlorophenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine
   Show/Hide
C29H40Cl2N4O2
 1
1
IC50 = 150 nM
   TI
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   TS
CP0442623
1-{2-[(1S)-((2R)-Aminopropionamido)-2-methylpropyl]-4-chlorophenyl}-4-[(2R)-methyl-3-(2-methoxy-4-dichlorophenyl)propionyl]piperazine
   Show/Hide
C28H38Cl2N4O3
 1
1
IC50 = 150 nM
   TI
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   LO
   TS
CP0876125
Ac-Nle4-cyclo(Asp5-Pro6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C55H70N10O9
 1
1
IC50 = 160 nM
   TI
   LI
   LO
   TS
CP0514396
(4R,5S)-4-(2-Fluoro-phenyl)-pyrrolidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C32H32ClFN4O3S
 1
1
IC50 = 160 nM
   TI
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   TS
CP0503293
1-{2-[(1S)-(1-Methyl-3-azetadinylcarbonyl)-amino-2-methylpropyl]-4-chlorophenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine
   Show/Hide
C29H38Cl2N4O2
 1
1
IC50 = 160 nM
   TI
   LI
   LO
   TS
CP0925920
(3R,4S)-4-Phenyl-pyrrolidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide hydrochloride
   Show/Hide
C32H34Cl2N4O3S
 1
1
IC50 = 190 nM
   TI
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   TS
CP0270338
1-{2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl}-4-[(2R)-methyl-3-(2-fluoro-4-chlorophenyl)propionyl]piperazine
   Show/Hide
C30H42ClFN4O2
 1
1
IC50 = 190 nM
   TI
   LI
   LO
   TS
CP0509676
(2S,3S)-3-(4-Trifluoromethyl-phenyl)-piperidine-4-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C34H34ClF3N4O3S
 1
1
IC50 = 200 nM
   TI
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   LO
   TS
CP0442055
(R)-N-((R)-1-(4-((1H-tetrazol-5-yl)methyl)-4-cyclohexylpiperidin-1-yl)-3-(4-chlorophenyl)-1-oxopropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
   Show/Hide
C32H40ClN7O2
 1
1
IC50 = 238 nM
   TI
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   LO
   TS
CP0173276
1-{2-[(1S)-(3-Dimethylaminopropionamino)-2-methylpropyl]-6-fluorophenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine
   Show/Hide
C29H40ClFN4O2
 1
1
IC50 = 270 nM
   TI
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   LO
   TS
CP0136197
1-{2-[(1S)-(aminopropionyl)amino-2-methylpropyl]-4-methylphenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine
   Show/Hide
C28H39ClN4O2
 1
1
IC50 = 280 nM
   TI
   LI
   LO
   TS
CP0541731
6-(4-Chloro-phenylsulfanyl)-4-((R)-3-{[(4S,5R)-4-(4-fluoro-phenyl)-piperidin-3-ylmethyl]-amino}-butyl)-2-(4-methoxy-phenyl)-2H-pyridazin-3-one
   Show/Hide
C33H36ClFN4O2S
 1
1
IC50 = 290 nM
   TI
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   LO
   TS
CP0433388
1-{2-[(1S)-(Methylaminoacetamido)-2-methylpropyl]-4-chlorophenyl}-4-[(2R)-methyl-3-(2-methoxy-4-dichlorophenyl)propionyl]piperazine
   Show/Hide
C28H38Cl2N4O3
 1
1
IC50 = 290 nM
   TI
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   LO
   TS
CP0442631
1-{2-[(1S)-(Methylaminoacetamido)-2-methylpropyl]-4-chlorophenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine
   Show/Hide
C27H36Cl2N4O2
 1
1
IC50 = 300 nM
   TI
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   LO
   TS
CP0496469
(3S,4S)-3-Phenyl-piperidine-4-carboxylic acid {3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C33H35ClN4O3S
 1
1
IC50 = 339 nM
   TI
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   TS
CP0415761
1-{2-[(1S)-(Methylaminoacetamido)-2-methylpropyl]-6-fluorophenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine
   Show/Hide
C27H36ClFN4O2
 1
1
IC50 = 340 nM
   TI
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   TS
CP0435301
(2R,3S)-3-(4-Fluoro-benzyl)-piperidine-4-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C34H36ClFN4O3S
 1
1
IC50 = 390 nM
   TI
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   TS
CP0415759
1-{2-[(1S)-(Methylaminoacetamido)-2-methylpropyl]-6-fluorophenyl}-4-[(2R)-methyl-3-(2-methoxy-4-chlorophenyl)propionyl]piperazine
   Show/Hide
C28H38ClFN4O3
 1
1
IC50 = 390 nM
   TI
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   TS
CP0058986
1-{2-[(1S)-(methylaminoacetamido)-2-methylpropyl]-4-methylphenyl}-4-[(2R)-methyl-3-(2-fluoro-4-chlorophenyl)propionyl]piperazine
   Show/Hide
C28H38ClFN4O2
 1
1
IC50 = 410 nM
   TI
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   TS
CP0374139
1-{2-[(1S)-(Methylaminoethyl)amino-2-methylpropyl]-6-fluorophenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine
   Show/Hide
C27H38ClFN4O
 1
1
IC50 = 480 nM
   TI
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   LO
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CP0484592
1-{2-[(1S)-(3-Dimethylaminopropionyl) amino-2-methylpropyl]phenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine
   Show/Hide
C29H41ClN4O2
 1
1
IC50 = 480 nM
   TI
   LI
   LO
   TS
CP0483601
(4R,5S)-4-(3-Fluoro-phenyl)-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C33H34ClFN4O3S
 1
1
IC50 = 490 nM
   TI
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   LO
   TS
CP0510887
N-[(1S)-1-[2-[4-[(3S,4R)-4-(2,4-dichlorophenyl)-1-propan-2-ylpyrrolidine-3-carbonyl]piperazin-1-yl]-3-fluorophenyl]-2-methylpropyl]-3-(dimethylamino)propanamide
   Show/Hide
C33H46Cl2FN5O2
 1
1
IC50 = 560 nM
   TI
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   LO
   TS
CP0844893
Ac-Nle4-cyclo(Asp5-His6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C56H70N12O9
 1
1
IC50 = 570 nM
   TI
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   LO
   TS
CP0422262
Ac-Nle4-cyclo(Asp5-His6-D-Phe-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C49H64N12O9
 1
1
IC50 = 590 nM
   TI
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CP0212906
(R)-3-(4-chloro-2-fluorophenyl)-2-methyl-1-(4-(4-methyl-2-((S)-2-methyl-1-(2-(methylamino)ethylamino)propyl)phenyl)piperazin-1-yl)propan-1-one
   Show/Hide
C28H40ClFN4O
 1
1
IC50 = 660 nM
   TI
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   TS
CP0876424
c-Nle4-cyclo(Asp5-Tic6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C60H72N10O9
 1
1
IC50 = 720 nM
   TI
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   LO
   TS
CP0480669
(2R,3S)-3-Benzyl-piperidine-4-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C34H37ClN4O3S
 1
1
IC50 = 750 nM
   TI
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   TS
CP0519865
1-{2-[(1S)-Amino-2-methylpropyl]-4-chlorophenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]-piperazine
   Show/Hide
C24H31Cl2N3O
 1
1
IC50 = 750 nM
   TI
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   TS
CP0399828
(R)-1-(4-Fluoro-phenyl)-piperazine-2-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C32H33ClFN5O3S
 1
1
IC50 = 950 nM
   TI
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   LO
   TS
CP0466853
(3R,4S)-4-Phenyl-pyrrolidine-3-carboxylic acid {(S)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C32H33ClN4O3S
 1
1
IC50 = 975 nM
   TI
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   TS
CP0878527
Ac-Nle4-cyclo(Asp5-Phg6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C58H70N10O9
 1
1
IC50 = 990 nM
   TI
   LI
   LO
   TS
CP0878544
Ac-Nle4-cyclo(Asp5-Pro6-D-4,4'-Bip7-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C54H68N10O9
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0485836
(S)-1-(4-Fluoro-phenyl)-piperazine-2-carboxylic acid {(S)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C32H33ClFN5O3S
 1
1
IC50 = 1000 nM
   TI
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   TS
CP0391977
(R)-1-(4-Fluoro-phenyl)-piperazine-2-carboxylic acid {(S)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide
   Show/Hide
C32H33ClFN5O3S
 1
1
IC50 = 1100 nM
   TI
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   LO
   TS
CP0922153
(3R,4S)-4-Phenyl-piperidine-3-carboxylic acid {(S)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide hydrochloride
   Show/Hide
C33H36Cl2N4O3S
 1
1
IC50 = 1197 nM
   TI
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   LO
   TS
CP0394757
Ac-Nle4-cyclo(Asp5-His6-D-4,4'-Bip-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C56H69N11O9
 1
1
IC50 = 1200 nM
   TI
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   TS
CP0505125
(3R,4S)-4-Phenyl-pyrrolidine-3-carboxylic acid {3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-propyl}-amide
   Show/Hide
C31H31ClN4O3S
 1
1
IC50 = 1245 nM
   TI
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   TS
CP0432989
Ac-Nle4-cyclo(Asp5-His6-L-Phe-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C49H64N12O9
 1
1
IC50 = 1600 nM
   TI
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   LO
   TS
CP0879920
Ac-Nle4-cyclo(Asp5-Oic6-D-D-pBzlPhe7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C60H78N10O9
 1
1
IC50 = 1600 nM
   TI
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CP0505607
(4-(2-((S)-1-amino-2-methylpropyl)-4-methylphenyl)piperazin-1-yl)((3S,4R)-4-(4-chlorophenyl)-1-(1-isobutylpiperidin-4-yl)pyrrolidin-3-yl)methanone
   Show/Hide
C35H52ClN5O
 1
1
IC50 = 1800 nM
   TI
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CP0486433
(3R,4S)-4-Phenyl-piperidine-3-carboxylic acid {3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-propyl}-amide
   Show/Hide
C32H33ClN4O3S
 1
1
IC50 = 1970 nM
   TI
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   TS
CP0919241
(3S,4R)-4-Phenyl-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide hydrochloride
   Show/Hide
C33H36Cl2N4O3S
 1
1
IC50 = 2055 nM
   TI
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   TS
CP0967345
(3R,4S)-4-Phenyl-piperidine-3-carboxylic acid {3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-2-methyl-propyl}-amide hydrochloride
   Show/Hide
C33H36Cl2N4O3S
 1
1
IC50 = 2170 nM
   TI
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   TS
CP0919118
(3R,4R)-4-Phenyl-piperidine-3-carboxylic acid {(R)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide hydrochloride
   Show/Hide
C33H36Cl2N4O3S
 1
1
IC50 = 2240 nM
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CP0270336
(R)-1-(4-(2-((S)-1-amino-2-methylpropyl)-4-methylphenyl)piperazin-1-yl)-3-(4-chlorophenyl)-2-methylpropan-1-one
   Show/Hide
C25H34ClN3O
 1
1
IC50 = 2400 nM
   TI
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   LO
   TS
CP0497218
(3S,4S)-3-Phenyl-piperidine-4-carboxylic acid {3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-propyl}-amide
   Show/Hide
C32H33ClN4O3S
 1
1
IC50 = 2755 nM
   TI
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   TS
CP0947547
(3S,4R)-4-Phenyl-piperidine-3-carboxylic acid {(S)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide hydrochloride
   Show/Hide
C33H36Cl2N4O3S
 1
1
IC50 = 2990 nM
   TI
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   TS
CP0541671
1,2,3,4-Tetrahydro-isoquinoline-3-carboxylic acid [1-(4-chloro-benzyl)-2-(4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidin-1-yl)-2-oxo-ethyl]-amide
   Show/Hide
C33H41ClN6O2
 1
1
IC50 = 3050 nM
   TI
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   TS
CP0394113
Ac-Nle4-cyclo(Asp5-His6-D-Bth-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C53H68N12O9S
 1
1
IC50 = 3600 nM
   TI
   LI
   LO
   TS
CP0895117
(3R,4S)-4-Phenyl-piperidine-3-carboxylic acid {3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-butyl}-amide hydrochloride
   Show/Hide
C33H36Cl2N4O3S
 1
1
IC50 = 3930 nM
   TI
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   TS
CP0394150
Ac-Nle4-cyclo(Asp5-His6-D-Phe(4-Cl)-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C49H63ClN12O9
 1
1
IC50 = 4500 nM
   TI
   LI
   LO
   TS
CP0855549
Ac-Nle4-cyclo(Asp5-Oic6-D-4,4'-Bip7-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C58H74N10O9
 1
1
IC50 = 4700 nM
   TI
   LI
   LO
   TS
CP0882669
Ac-Nle4-cyclo(Asp5-Val6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
   Show/Hide
C55H72N10O9
 1
1
IC50 = 4700 nM
   TI
   LI
   LO
   TS
CP0425206
Ac-Nle4-cyclo(Asp5-His6-D-Nal(2)-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C53H66N12O9
 1
1
IC50 = 4800 nM
   TI
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   LO
   TS
CP0877821
(S)-4-Methyl-piperazine-2-carboxylic acid [(S)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide dihydrochloride
   Show/Hide
C31H50Cl2FN5O3
 1
1
IC50 = 6500 nM
   TI
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   TS
CP0377912
(1R,4S,6R)-2-Methyl-2-aza-bicyclo[2.2.2]octane-6-carboxylic acid [(R)-2-(4-tert-butylcarbamoyl-4-cyclohexyl-piperidin-1-yl)-1-(4-fluoro-benzyl)-2-oxo-ethyl]-amide
   Show/Hide
C34H51FN4O3
 1
1
IC50 = 7000 nM
   TI
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   LO
   TS
CP0934284
(3R,4R)-4-Phenyl-piperidine-3-carboxylic acid {(S)-3-[6-(4-chloro-phenylsulfanyl)-2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-pyridazin-4-yl]-1-methyl-propyl}-amide hydrochloride
   Show/Hide
C33H36Cl2N4O3S
 1
1
IC50 = 9020 nM
   TI
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   LO
   TS
CP0394108
Ac-Nle4-cyclo(Asp5-His6-D-Tyr(Me)-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C50H66N12O10
 1
1
IC50 > 10000 nM
   TI
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CP0394112
Ac-Nle4-cyclo(Asp5-His6-D-Cha-Pro8-Trp9-Lys10)-NH2
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C49H70N12O9
 1
1
IC50 > 10000 nM
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CP0394115
Ac-Nle4-cyclo(Asp5-His6-D-Nle-Pro8-Trp9-Lys10)-NH2
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C46H66N12O9
 1
1
IC50 > 10000 nM
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CP0394119
Ac-Nle4-cyclo(Asp5-His6-D-Glu-Pro8-Trp9-Lys10)-NH2
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C45H62N12O11
 1
1
IC50 > 10000 nM
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CP0432988
Ac-Nle4-cyclo(Asp5-His6-D-Tyr-Pro8-Trp9-Lys10)-NH2
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C49H64N12O10
 1
1
IC50 > 10000 nM
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CP0433726
Ac-Nle4-cyclo(Asp5-His6-D-Gln-Pro8-Trp9-Lys10)-NH2
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C45H63N13O10
 1
1
IC50 > 10000 nM
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CP0434012
Ac-Nle4-cyclo(Asp5-His6-D-His-Pro8-Trp9-Lys10)-NH2
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C46H62N14O9
 1
1
IC50 > 10000 nM
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CP0855105
Ac-Nle4-cyclo(Asp5-Chg6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
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C58H76N10O9
 1
1
IC50 > 10000 nM
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CP0795225
1-(3-Thiophen-2-yl-phenyl)-ethanone, O-(phenylaminocarbonyl)oxime
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C19H16N2O2S
 1
1
IC50 > 10000 nM
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CP0425204
Ac-Nle4-cyclo(Asp5-His6-D-Tyr-Pro8-Trp9-Lys10)-NH2
   Show/Hide
C51H65N13O9
 1
1
IC50 > 5000 nM
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CP0844894
Ac-Nle4-cyclo(Asp5-Oic6-D-4,4'-Bip7-Pip8-Trp9-Lys10)-NH2
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C59H76N10O9
 1
1
IC50 > 5000 nM
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CP0544214
(2R)-2-(3,5-dimethoxyphenyl)-1-[(2S)-7-methyl-6-(1-methylpyrazol-4-yl)spiro[3,4-dihydro-1H-1,8-naphthyridine-2,3'-pyrrolidine]-1'-yl]propan-1-one
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C27H33N5O3
 1
1
Ki = 0.044 nM
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CP0568988
(2R)-2-(5-chloro-2-methoxypyridin-4-yl)-1-[(2S)-7-methyl-6-(2-methyltetrazol-5-yl)spiro[3,4-dihydro-1H-1,8-naphthyridine-2,3'-pyrrolidine]-1'-yl]propan-1-one
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C23H27ClN8O2
 1
1
Ki = 0.21 nM
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CP0568735
(2R)-2-(5-chloro-2-methoxypyridin-4-yl)-1-[(2S)-7-methyl-6-pyrimidin-2-ylspiro[3,4-dihydro-1H-1,8-naphthyridine-2,3'-pyrrolidine]-1'-yl]propan-1-one
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C25H27ClN6O2
 1
1
Ki = 0.25 nM
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CP0577051
(2R)-2-(5-chloro-2-methoxypyridin-4-yl)-1-[(2S)-7-methyl-6-([1,2,4]triazolo[1,5-a]pyridin-2-yl)spiro[3,4-dihydro-1H-1,8-naphthyridine-2,3'-pyrrolidine]-1'-yl]propan-1-one
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C27H28ClN7O2
 1
1
Ki = 0.28 nM
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CP0576660
(2R)-2-(5-chloro-2-methoxypyridin-4-yl)-1-[(2S)-6-[5-(difluoromethyl)-1-methyl-1,2,4-triazol-3-yl]-7-methylspiro[3,4-dihydro-1H-1,8-naphthyridine-2,3'-pyrrolidine]-1'-yl]propan-1-one
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C25H28ClF2N7O2
 1
1
Ki = 0.4 nM
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CP0568734
(2S)-2-[6-(difluoromethoxy)pyridin-3-yl]-1-[(2S)-7-methyl-6-pyrimidin-2-ylspiro[3,4-dihydro-1H-1,8-naphthyridine-2,3'-pyrrolidine]-1'-yl]propan-1-one
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C25H26F2N6O2
 1
1
Ki = 0.44 nM
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CP0544213
(2R)-2-(5-fluoro-2-methoxypyridin-4-yl)-1-[(2S)-7-methyl-6-pyrimidin-2-ylspiro[3,4-dihydro-1H-1,8-naphthyridine-2,3'-pyrrolidine]-1'-yl]propan-1-one
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C25H27FN6O2
 1
1
Ki = 0.46 nM
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CP0568985
(2R)-2-(6-methoxy-2-methylpyrimidin-4-yl)-1-[(2S)-7-methyl-6-(2-methyltetrazol-5-yl)spiro[3,4-dihydro-1H-1,8-naphthyridine-2,3'-pyrrolidine]-1'-yl]propan-1-one
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C23H29N9O2
 1
1
Ki = 0.54 nM
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CP0579377
2-[5-chloro-2-(difluoromethoxy)pyridin-4-yl]-1-[(2S)-7-methyl-6-pyrimidin-2-ylspiro[3,4-dihydro-1H-1,8-naphthyridine-2,3'-pyrrolidine]-1'-yl]propan-1-one
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C25H25ClF2N6O2
 1
1
Ki = 0.54 nM
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CP0574481
(2R)-2-(5-chloro-2-methoxypyridin-4-yl)-1-[(2R)-7-methyl-6-(2-methyltetrazol-5-yl)spiro[3,4-dihydro-1H-1,8-naphthyridine-2,3'-pyrrolidine]-1'-yl]propan-1-one
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C23H27ClN8O2
 1
1
Ki = 4.5 nM
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CP0964966
(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-5-oxo-2-[[(3S,9S,12S,15S,18S,21R,26R,29S,32S,38S,41S,47S)-9,15,32,38-tetrakis(4-aminobutyl)-21-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-12,18-bis(3-amino-3-oxopropyl)-29,41-dibenzyl-2,8,11,14,17,20,28,31,34,37,40,43,46-tridecaoxo-23,24-dithia-1,7,10,13,16,19,27,30,33,36,39,42,45-tridecazatricyclo[45.3.0.03,7]pentacontane-26-carbonyl]amino]pentanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid
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C144H214N38O30S2
 1
1
Ki = 6.918 nM
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CP0961058
(S)-1-((S)-1-((6S,9S,15S,18S,21R,24S,27S,30S,33S,36S)-1-((S)-1-((S)-1-((2S,5S,8S,11S,14R,17S,20S,23S,26S)-20-((1H-imidazol-5-yl)methyl)-26-amino-5,11-bis(3-amino-3-oxopropyl)-2,8-bis(4-aminobutyl)-23-benzyl-14-(carbamoylthiomethyl)-17-(4-hydroxybenzyl)-28-methyl-4,7,10,13,16,19,22,25-octaoxo-3,6,9,12,15,18,21,24-octaazanonacosane)pyrrolidine-2-carbonyl)pyrrolidin-2-yl)-24-(3-amino-3-oxopropyl)-9,15,30-tris(4-aminobutyl)-6,18,27-tribenzyl-21-(carbamoylthiomethyl)-36-(3-guanidinopropyl)-33-isobutyl-1,4,7,10,13,16,19,22,25,28,31,34-dodecaoxo-2,5,8,11,14,17,20,23,26,29,32,35-dodecaazaheptatriacontane)pyrrolidine-2-carbonyl)pyrrolidine-2-carboxylic acid
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C146H218N40O32S2
 1
1
Ki = 12.59 nM
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CP0568986
(2S)-2-(6-methoxy-2-methylpyrimidin-4-yl)-1-[(2S)-7-methyl-6-(2-methyltetrazol-5-yl)spiro[3,4-dihydro-1H-1,8-naphthyridine-2,3'-pyrrolidine]-1'-yl]propan-1-one
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C23H29N9O2
 1
1
Ki = 30 nM
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CP0574482
2-[6-(difluoromethoxy)pyridin-3-yl]-1-[(2S)-7-methyl-6-(1-methylpyrazol-4-yl)spiro[3,4-dihydro-1H-1,8-naphthyridine-2,3'-pyrrolidine]-1'-yl]propan-1-one
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C25H28F2N6O2
 1
1
Ki = 57 nM
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CP0944118
(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(3S,9S,12S,15S,18S,21R,26R,29S,32S,38S,41S,47S)-32,38-bis(4-aminobutyl)-21-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-12,18-bis(3-amino-3-oxopropyl)-29,41-dibenzyl-2,8,11,14,17,20,28,31,34,37,40,43,46-tridecaoxo-9,15-di(propan-2-yl)-23,24-dithia-1,7,10,13,16,19,27,30,33,36,39,42,45-tridecazatricyclo[45.3.0.03,7]pentacontane-26-carbonyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid
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C142H208N36O30S2
 1
1
Ki = 60.26 nM
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CP0944134
(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(3S,9S,12S,15S,18S,21R,26R,29S,32S,38S,41S,47S)-32,38-bis(4-aminobutyl)-21-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-12,18-bis(3-amino-3-oxopropyl)-29,41-dibenzyl-9,15-bis(hydroxymethyl)-2,8,11,14,17,20,28,31,34,37,40,43,46-tridecaoxo-23,24-dithia-1,7,10,13,16,19,27,30,33,36,39,42,45-tridecazatricyclo[45.3.0.03,7]pentacontane-26-carbonyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid
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C138H200N36O32S2
 1
1
Ki = 67.61 nM
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CP0574483
2-(2,4-dichlorophenyl)-1-[(2S)-7-methyl-6-pyrimidin-2-ylspiro[3,4-dihydro-1H-1,8-naphthyridine-2,3'-pyrrolidine]-1'-yl]propan-1-one
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C25H25Cl2N5O
 1
1
Ki = 82 nM
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CP0961059
(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(3S,9S,12S,15S,18S,21R,26R,29S,32S,38S,41S,47S)-32,38-bis(4-aminobutyl)-21-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-12,18-bis(3-amino-3-oxopropyl)-29,41-dibenzyl-9,15-bis(2-methylpropyl)-2,8,11,14,17,20,28,31,34,37,40,43,46-tridecaoxo-23,24-dithia-1,7,10,13,16,19,27,30,33,36,39,42,45-tridecazatricyclo[45.3.0.03,7]pentacontane-26-carbonyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid
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C144H212N36O30S2
 1
1
Ki = 93.33 nM
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CP0964152
(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(3S,9S,12S,15S,18S,21R,26R,29S,32S,38S,41S,47S)-32,38-bis(4-aminobutyl)-21-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-12,18-bis(3-amino-3-oxopropyl)-29,41-dibenzyl-9,15-dimethyl-2,8,11,14,17,20,28,31,34,37,40,43,46-tridecaoxo-23,24-dithia-1,7,10,13,16,19,27,30,33,36,39,42,45-tridecazatricyclo[45.3.0.03,7]pentacontane-26-carbonyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid
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C138H200N36O30S2
 1
1
Ki = 117.49 nM
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CP0944119
(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(3S,9S,12S,15R,20R,23S,26S,32S,35S,41S)-15-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]-5-oxopentanoyl]amino]-26,32-bis(4-aminobutyl)-12-(3-amino-3-oxopropyl)-23,35-dibenzyl-9-methyl-2,8,11,14,22,25,28,31,34,37,40-undecaoxo-17,18-dithia-1,7,10,13,21,24,27,30,33,36,39-undecazatricyclo[39.3.0.03,7]tetratetracontane-20-carbonyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid
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C138H200N36O30S2
 1
1
Ki = 245.47 nM
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CP0969533
(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(3S,9R,14R,17S,20S,26S,29S,35S)-9-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]-5-oxopentanoyl]amino]-20,26-bis(4-aminobutyl)-17,29-dibenzyl-2,8,16,19,22,25,28,31,34-nonaoxo-11,12-dithia-1,7,15,18,21,24,27,30,33-nonazatricyclo[33.3.0.03,7]octatriacontane-14-carbonyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid
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C138H200N36O30S2
 1
1
Ki = 245.47 nM
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CP0544212
(2R)-2-[6-(difluoromethoxy)pyridin-3-yl]-1-[(2S)-7-methyl-6-pyrimidin-2-ylspiro[3,4-dihydro-1H-1,8-naphthyridine-2,3'-pyrrolidine]-1'-yl]propan-1-one
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C25H26F2N6O2
 1
1
Ki > 200 nM
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