 | 1-[(2R)-1-[(4S)-4-(4-Chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl]-3-methyl-1-oxobutan-2-yl]-3-(2-hydroxy-2-methylpropyl)urea | IC50 | 6.0 [1] |
 | 1-[4-(4-Chloro-3-methoxyphenyl)piperazin-1-yl]-2-[4-chloro-5-methyl-3-(trifluoromethyl)pyrazol-1-yl]ethanone | IC50 | 3.9 [1] |
 | (1R,3R)-N-[(2R)-1-[(4S)-4-(4-Chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl]-3-methyl-1-oxobutan-2-yl]-3-hydroxycyclopentane-1-carboxamide | IC50 | 4.0 [1] |
 | BX-471 free base | IC50 | 1.5 [1], 5.5 [2], 18.0 [3], 31.0 [4] |
| BX-471 free base | Ki | 1.0 [1] |
 | N-[(2R)-1-[4-(4-Chlorophenyl)piperidin-1-yl]-3-methyl-1-oxobutan-2-yl]benzamide | IC50 | 15.0 [1], 78.0 [2], 85.0 [3] |
 | BX471 (hydrochloride) | IC50 | 0.4 [1], 2.36 [2], 40.0 [3], 550.0 [4] |
 | 5-[4-(4-Chlorophenyl)-4-hydroxy-1-piperidyl]-2,2-diphenyl-pentanenitrile | IC50 | 48.0 [1], 630.0 [2], 2500.0 [3] |
| 5-[4-(4-Chlorophenyl)-4-hydroxy-1-piperidyl]-2,2-diphenyl-pentanenitrile | Ki | 52.0 [1] |
 | N-[(2S,3S,5R)-1-Cyclohexyl-3-hydroxy-7-methyl-5-(methylcarbamoyl)octan-2-yl]quinoline-3-carboxamide | IC50 | 840.0 [1], 2280.0 [2], 2300.0 [3] |
 | J-113863 Cation, trans- | IC50 | 0.73 [1], 0.9 [2], 47.0 [3] |
 | (2R)-2-N-[(4-Chlorophenyl)methyl]-2-N-methyl-1-N-[4-(trifluoromethyl)phenyl]pyrrolidine-1,2-dicarboxamide | IC50 | 22.0 [1], 140.0 [2] |
 | N-[5-Chloro-2-[(E)-3-[(2R)-4-[(4-fluorophenyl)methyl]-2-methylpiperazin-1-yl]-3-oxoprop-1-enyl]-4-methoxyphenyl]acetamide | IC50 | 1.5 [1], 4.0 [2], 20.0 [3], 69.7 [4] |
 | N-[5-Chloro-2-[(E)-3-[3-[(4-fluorophenyl)methyl]-3,8-diazabicyclo[3.2.1]octan-8-yl]-3-oxoprop-1-enyl]phenyl]-2-(dimethylamino)acetamide | IC50 | 9.0 [1], 10.0 [2], 30.0 [3], 41.0 [4] |
 | N-[5-Chloro-2-[(E)-3-[(2R)-4-[(4-fluorophenyl)methyl]-2-methylpiperazin-1-yl]-3-oxoprop-1-enyl]phenyl]acetamide | IC50 | 1.0 [1], 9.97 [2], 30.0 [3], 320.0 [4] |
 | N-[5-Chloro-2-[(E)-3-[3-[(4-fluorophenyl)methyl]-3,8-diazabicyclo[3.2.1]octan-8-yl]-3-oxoprop-1-enyl]-4-methoxyphenyl]acetamide | IC50 | 0.0 [1], 1.0 [2], 7.0 [3], 7.5 [4] |
 | [5-Chloro-2-[(E)-3-[(2R)-4-[(4-fluorophenyl)methyl]-2-methylpiperazin-1-yl]-3-oxoprop-1-enyl]phenyl]urea | IC50 | 0.9 [1], 16.0 [2], 40.0 [3], 45.0 [4] |
 | N-[(2R)-1-[(4S)-4-(4-Chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl]-3-methyl-1-oxobutan-2-yl]-3-hydroxy-3-methylbutanamide | IC50 | 3.0 [1], 5.2 [2] |
| N-[(2R)-1-[(4S)-4-(4-Chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl]-3-methyl-1-oxobutan-2-yl]-3-hydroxy-3-methylbutanamide | Ki | 3.7 [1] |
 | N-[(2S,3S,5R)-5-Carbamoyl-3-hydroxy-8-methyl-1-phenylnonan-2-yl]quinoxaline-2-carboxamide | IC50 | 2.0 [1], 28.0 [2] |
 | N-[2-[(2S)-3-(5-Fluorospiro[3H-1-benzofuran-2,4'-piperidine]-1'-yl)-2-hydroxypropoxy]-4-hydroxyphenyl]acetamide | IC50 | 0.52 [1], 2.6 [2] |
 | N-[2-[(2S)-3-(5-Chlorospiro[3H-1-benzofuran-2,4'-piperidine]-1'-yl)-2-hydroxypropoxy]-4-hydroxyphenyl]acetamide | IC50 | 0.36 [1], 2.0 [2] |
 | N-(2-(3-(4-(4-Fluorobenzyl)piperazin-1-yl)-3-oxoprop-1-enyl)-5-chlorophenyl)acetamide | IC50 | 58.0 [1], 150.0 [2], 190.0 [3] |
 | N-[5-Chloro-2-[(E)-3-[(2S,5R)-4-[(4-fluorophenyl)methyl]-2,5-dimethylpiperazin-1-yl]-3-oxoprop-1-enyl]phenyl]acetamide | IC50 | 1.0 [1], 100.0 [2], 10500.0 [3] |
 | N-[6-[(E)-3-[(2R)-4-[(4-Fluorophenyl)methyl]-2-methylpiperazin-1-yl]-3-oxoprop-1-enyl]quinolin-7-yl]acetamide | IC50 | 20.0 [1], 30.0 [2], 300.0 [3] |
 | (R)-N-(3-(3-(4-(4-Fluorobenzyl)-2-methylpiperazin-1-yl)-3-oxoprop-1-enyl)naphthalen-2-yl)acetamide | IC50 | 13.0 [1], 80.0 [2], 1500.0 [3] |
 | N-[5-Chloro-2-[(E)-3-[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethylpiperazin-1-yl]-3-oxoprop-1-enyl]phenyl]acetamide | IC50 | 0.1 [1], 9.0 [2], 1350.0 [3] |
 | 2-[4-Chloro-5-methyl-3-(trifluoromethyl)pyrazol-1-yl]-1-[4-(4-fluorophenyl)piperazin-1-yl]ethanone | IC50 | 93.0 [1], 307.0 [2], 310.0 [3] |
 | 3-Amino-4-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methylpiperazin-1-yl]-2-oxoethoxy]anilino]cyclobut-3-ene-1,2-dione | IC50 | 4.0 [1], 7.0 [2], 10.0 [3] |
 | N-[5-Chloro-2-[[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methylpiperazin-1-yl]-2-oxoethyl]amino]phenyl]acetamide | IC50 | 2.4 [1], 50.0 [2], 1700.0 [3] |
 | N-[5-Chloro-2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methylpiperazine-1-carbonyl]-1H-indol-7-yl]acetamide | IC50 | 9.6 [1], 560.0 [2], 1000.0 [3] |
 | N-[5-Chloro-2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methylpiperazine-1-carbonyl]-1-benzofuran-7-yl]acetamide | IC50 | 28.0 [1], 120.0 [2], 1000.0 [3] |
 | 3-[5-Chloro-2-[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methylpiperazin-1-yl]-2-oxoethoxy]anilino]-4-(methylamino)cyclobut-3-ene-1,2-dione | IC50 | 17.0 [1], 18.0 [2], 26.0 [3] |
 | 3-[5-Bromo-2-[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methylpiperazin-1-yl]-2-oxoethoxy]anilino]-4-(methylamino)cyclobut-3-ene-1,2-dione | IC50 | 14.0 [1], 25.0 [2] |
 | 3-[5-Chloro-2-[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methylpiperazin-1-yl]-2-oxoethoxy]anilino]-4-(2-methoxyethylamino)cyclobut-3-ene-1,2-dione | IC50 | 19.0 [1], 54.0 [2], 63.0 [3] |
 | 3-[5-Chloro-2-[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methylpiperazin-1-yl]-2-oxoethoxy]anilino]-4-(2-hydroxyethylamino)cyclobut-3-ene-1,2-dione | IC50 | 13.0 [1], 20.0 [2], 47.0 [3] |
 | 3-(2-Aminoethylamino)-4-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methylpiperazin-1-yl]-2-oxoethoxy]anilino]cyclobut-3-ene-1,2-dione | IC50 | 6.0 [1], 18.0 [2], 23.0 [3] |
 | 3-[5-Chloro-2-[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methylpiperazin-1-yl]-2-oxoethoxy]anilino]-4-(2-morpholin-4-ylethylamino)cyclobut-3-ene-1,2-dione | IC50 | 12.0 [1] |
 | 3-[5-Chloro-2-[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methylpiperazin-1-yl]-2-oxoethoxy]anilino]-4-(2-piperazin-1-ylethylamino)cyclobut-3-ene-1,2-dione | IC50 | 5.0 [1], 39.0 [2], 50.0 [3] |
 | 3-[5-Chloro-2-[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methylpiperazin-1-yl]-2-oxoethoxy]anilino]-4-(pyridin-3-ylmethylamino)cyclobut-3-ene-1,2-dione | IC50 | 8.0 [1], 38.0 [2], 42.0 [3] |
 | 6-[2-(Dimethylamino)ethyl-methylamino]-1,3-dimethyl-N-[(3-propan-2-yloxyphenyl)carbamoyl]pyrazolo[3,4-b]pyridine-5-carboxamide;hydrochloride | IC50 | 10000.0 [1] |
 | 1-[(2R)-Butan-2-yl]-3-[(2R)-1-[(4S)-4-(4-chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl]-3-methyl-1-oxobutan-2-yl]urea | IC50 | 3.0 [1], 6.0 [2] |
| 1-[(2R)-Butan-2-yl]-3-[(2R)-1-[(4S)-4-(4-chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl]-3-methyl-1-oxobutan-2-yl]urea | Ki | 2.1 [1] |
 | N-[(2R)-1-[(4S)-4-(4-Chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl]-3-methyl-1-oxobutan-2-yl]-3-methylbutanamide | IC50 | 1.9 [1], 2.9 [2] |
| N-[(2R)-1-[(4S)-4-(4-Chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl]-3-methyl-1-oxobutan-2-yl]-3-methylbutanamide | Ki | 2.6 [1] |
 | N-[(2R)-1-[(4S)-4-(4-Chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl]-3-methyl-1-oxobutan-2-yl]cyclopentanecarboxamide | IC50 | 1.4 [1], 2.5 [2] |
| N-[(2R)-1-[(4S)-4-(4-Chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl]-3-methyl-1-oxobutan-2-yl]cyclopentanecarboxamide | Ki | 0.7 [1] |
 | N-[(2S,3S,5R)-3-Hydroxy-7-methyl-5-(methylcarbamoyl)-1-phenyloctan-2-yl]quinoline-3-carboxamide | IC50 | 650.0 [1] |
 | 1-(5-Amino-4,4-diphenyl-pentyl)-4-(4-chloro-phenyl)-piperidin-4-ol | IC50 | 760.0 [1] |
| 1-(5-Amino-4,4-diphenyl-pentyl)-4-(4-chloro-phenyl)-piperidin-4-ol | Ki | 244.0 [1] |
 | 2-(Benzothiazol-2-ylsulfanyl)-N-[1-(3,4-dichloro-benzyl)-piperidin-4-yl]-acetamide | IC50 | 450.0 [1] |
 | 5-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-2-phenyl-2-piperidin-1-yl-pentanenitrile | IC50 | 4800.0 [1] |
| 5-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-2-phenyl-2-piperidin-1-yl-pentanenitrile | Ki | 130.0 [1] |
 | 5-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-2-thiophen-2-yl-pentanenitrile | IC50 | 8400.0 [1] |
| 5-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-2-thiophen-2-yl-pentanenitrile | Ki | 128.0 [1] |
 | 2-{4-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-1-cyano-butyl}-benzonitrile | IC50 | 5800.0 [1] |
| 2-{4-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-1-cyano-butyl}-benzonitrile | Ki | 98.0 [1] |
 | 6-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-2,2-diphenyl-hexanenitrile | IC50 | 1600.0 [1] |
| 6-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-2,2-diphenyl-hexanenitrile | Ki | 78.0 [1] |
 | 7-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-2,2-diphenyl-heptanenitrile | IC50 | 5600.0 [1] |
| 7-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-2,2-diphenyl-heptanenitrile | Ki | 99.0 [1] |
 | 11-[3-[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]propyl]-5-methyl-6-oxobenzo[c][1]benzazepine-11-carbonitrile | IC50 | 3300.0 [1] |
| 11-[3-[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]propyl]-5-methyl-6-oxobenzo[c][1]benzazepine-11-carbonitrile | Ki | 32.0 [1] |
 | 5-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-2-thiophen-3-yl-pentanenitrile | IC50 | 9800.0 [1] |
| 5-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-2-thiophen-3-yl-pentanenitrile | Ki | 236.0 [1] |
 | Ethyl 5-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-2-cyano-2-phenylpentanoate | IC50 | 7000.0 [1] |
| Ethyl 5-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-2-cyano-2-phenylpentanoate | Ki | 33.0 [1] |
 | 2-(3-Bromo-4-methoxy-phenyl)-5-[4-(4-chloro-phenyl)-4-hydroxy-piperidin-1-yl]-pentanenitrile | IC50 | 1900.0 [1] |
| 2-(3-Bromo-4-methoxy-phenyl)-5-[4-(4-chloro-phenyl)-4-hydroxy-piperidin-1-yl]-pentanenitrile | Ki | 74.0 [1] |
 | 4-[1-(4-Cyano-4,4-diphenylbutyl)-4-hydroxypiperidin-4-yl]benzonitrile | IC50 | 10900.0 [1] |
| 4-[1-(4-Cyano-4,4-diphenylbutyl)-4-hydroxypiperidin-4-yl]benzonitrile | Ki | 92.0 [1] |
 | 5-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-2-(3-chloro-propyl)-2-phenyl-pentanenitrile | IC50 | 8300.0 [1] |
| 5-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-2-(3-chloro-propyl)-2-phenyl-pentanenitrile | Ki | 51.0 [1] |
 | 2-{3-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-propyl}-2-phenyl-succinonitrile | IC50 | 3200.0 [1] |
| 2-{3-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-propyl}-2-phenyl-succinonitrile | Ki | 125.0 [1] |
 | 5-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-2-(3-hydroxy-phenyl)-pentanenitrile | IC50 | 9000.0 [1] |
| 5-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-2-(3-hydroxy-phenyl)-pentanenitrile | Ki | 156.0 [1] |
 | 1-[(2R)-1-[(4S)-4-(4-Chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl]-3-methyl-1-oxobutan-2-yl]-3-[(1R,3S)-3-hydroxycyclopentyl]urea | IC50 | 2.0 [1], 4.0 [2] |
 | 1-[(2R)-1-[(4S)-4-(4-Chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl]-3-methyl-1-oxobutan-2-yl]-3-[(2S)-2-hydroxypropyl]urea | IC50 | 2.0 [1], 7.0 [2] |
 | 1-[(2R)-1-[(4S)-4-(4-Chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl]-3-methyl-1-oxobutan-2-yl]-3-[(2R)-2-hydroxypropyl]urea | IC50 | 2.0 [1], 6.0 [2] |
 | N-[(2R)-1-[(4S)-4-(4-Chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl]-3-methyl-1-oxobutan-2-yl]-4-hydroxy-4-methylpentanamide | IC50 | 2.0 [1], 22.0 [2] |
 | N-[(2R)-1-[4-(4-Chlorophenyl)-3,3-dimethylpiperazin-1-yl]-3-methyl-1-oxobutan-2-yl]cyclopentanecarboxamide | IC50 | 4.1 [1], 18.0 [2] |
 | (2R)-2-N-[(4-Chlorophenyl)methyl]-2-N-methyl-1-N-[2-methyl-4-(trifluoromethyl)phenyl]pyrrolidine-1,2-dicarboxamide | IC50 | 16.0 [1], 50.0 [2] |
 | 1-[1-(2-Bromophenyl)sulfonylpiperidin-4-yl]-4-(4-chlorophenyl)piperidin-4-ol | IC50 | 90.0 [1] |
 | (2R)-2-N-[(4-Chlorophenyl)methyl]-1-N-(4-methoxyphenyl)-2-N-methylpyrrolidine-1,2-dicarboxamide | IC50 | 290.0 [1], 440.0 [2] |
 | (2R)-2-N-[(4-Chlorophenyl)methyl]-1-N-[2-chloro-4-(trifluoromethyl)phenyl]-2-N-methylpyrrolidine-1,2-dicarboxamide | IC50 | 35.0 [1], 120.0 [2] |
 | (2R)-2-N-[(4-Chlorophenyl)methyl]-1-N-[2-fluoro-4-(trifluoromethyl)phenyl]-2-N-methylpyrrolidine-1,2-dicarboxamide | IC50 | 22.0 [1], 23.0 [2] |
 | (2R)-2-N-[(4-Chlorophenyl)methyl]-1-N-[2,6-dimethyl-4-(trifluoromethyl)phenyl]-2-N-methylpyrrolidine-1,2-dicarboxamide | IC50 | 6.0 [1], 11.0 [2] |
 | (2R)-2-[4-[(4-Chlorophenyl)methyl]-1,2,4-triazol-3-yl]-N-[4-(trifluoromethyl)phenyl]pyrrolidine-1-carboxamide | IC50 | 4.0 [1], 17.0 [2] |
 | (2R)-2-[1-[(4-Chlorophenyl)methyl]tetrazol-5-yl]-N-[4-(trifluoromethyl)phenyl]pyrrolidine-1-carboxamide | IC50 | 6.5 [1], 20.0 [2] |
 | (2R)-2-[2-[(4-Chlorophenyl)methyl]-1,2,4-triazol-3-yl]-N-[4-(trifluoromethyl)phenyl]pyrrolidine-1-carboxamide | IC50 | 22.0 [1], 32.0 [2] |
 | N-[(2S,3S)-8-Fluoro-3-hydroxy-8-methyl-5-(4-methylpiperazine-1-carbonyl)-1-phenylnonan-2-yl]quinoxaline-2-carboxamide | IC50 | 5600.0 [1], 7050.0 [2] |
 | N-[(2S,3S)-8-Fluoro-3-hydroxy-5-(hydroxycarbamoyl)-8-methyl-1-phenylnonan-2-yl]quinoxaline-2-carboxamide | IC50 | 27.0 [1], 31.0 [2] |
 | N-[(2S,3S)-8-Fluoro-3-hydroxy-8-methyl-1-phenyl-5-(pyrrolidine-1-carbonyl)nonan-2-yl]quinoxaline-2-carboxamide | IC50 | 740.0 [1], 2320.0 [2] |
 | N-[(2S,3S)-8-Fluoro-5-(hydrazinecarbonyl)-3-hydroxy-8-methyl-1-phenylnonan-2-yl]quinoxaline-2-carboxamide | IC50 | 1.0 [1], 7.0 [2] |
 | N-[(2S,3S)-6-Amino-3-hydroxy-5-(oxan-4-yl)-6-oxo-1-phenylhexan-2-yl]quinoxaline-2-carboxamide | IC50 | 3460.0 [1], 12500.0 [2] |
 | N-[(2S,3S,5R)-5-Carbamoyl-3,8-dihydroxy-8-methyl-1-phenylnonan-2-yl]quinoxaline-2-carboxamide | IC50 | 580.0 [1], 1180.0 [2] |
 | N-[(2S,3S)-6-Amino-5-(4,4-difluorocyclohexyl)-3-hydroxy-6-oxo-1-phenylhexan-2-yl]quinoxaline-2-carboxamide | IC50 | 20.0 [1], 220.0 [2] |
 | N-[(2S,3S)-6-Amino-5-(4,4-difluoro-1-hydroxycyclohexyl)-3-hydroxy-6-oxo-1-phenylhexan-2-yl]quinoxaline-2-carboxamide | IC50 | 68.0 [1], 560.0 [2] |
 | N-[(2S,3S)-5-(Benzylcarbamoyl)-8-fluoro-3-hydroxy-8-methyl-1-phenylnonan-2-yl]quinoxaline-2-carboxamide | IC50 | 440.0 [1], 850.0 [2] |
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