| 1-[2-[(1R,3S,5R)-3-[[(1S)-1-(3-Chloro-2-fluorophenyl)ethyl]carbamoyl]-2-azabicyclo[3.1.0]hexan-2-yl]-2-oxoethyl]pyrazolo[3,4-c]pyridine-3-carboxamide | IC50 | 29.0 [1], 30.0 [2], 70.0 [3], 144.0 [4] |
| Methyl (S)-2-((2-((3-(trifluoromethoxy)phenyl)carbamoyl)pyrrolidine-1-carboxamido)-methyl)benzoate | IC50 | 14000.0 [1] |
| Danicopan | IC50 | 4.0 [1], 15.0 [2] |
| (1R,3S,5R)-3-N-(6-Bromopyridin-2-yl)-2-N-(1-carbamoylindol-3-yl)-2-azabicyclo[3.1.0]hexane-2,3-dicarboxamide | IC50 | 5.0 [1], 6.0 [2], 9.0 [3] |
| (2S)-N-(6-Bromopyridin-2-yl)-3-[2-(3-carbamoylpyrazolo[3,4-b]pyridin-1-yl)acetyl]-1,3-thiazolidine-2-carboxamide | IC50 | 19.0 [1], 27.31 [2], 205.0 [3] |
| (2S)-1-N-(1-Carbamoylindol-3-yl)-2-N-[3-(trifluoromethoxy)phenyl]pyrrolidine-1,2-dicarboxamide | IC50 | 500.0 [1], 800.0 [2] |
| 1-[2-[(1R,3S,5R)-3-[(3-Bromo-2-fluorophenyl)carbamoyl]-2-azabicyclo[3.1.0]hexan-2-yl]-2-oxoethyl]indazole-3-carboxamide | IC50 | 10.0 [1], 150.0 [2] |
| (1R,3S,5R)-2-N-(1-Carbamoylindol-3-yl)-3-N-[3-(trifluoromethoxy)phenyl]-2-azabicyclo[3.1.0]hexane-2,3-dicarboxamide | IC50 | 50.0 [1], 210.0 [2], 1250.0 [3] |
| 1-[2-[(1R,3S,5R)-3-[(6-Bromopyridin-2-yl)carbamoyl]-2-azabicyclo[3.1.0]hexan-2-yl]-2-oxoethyl]indazole-3-carboxamide | IC50 | 5.0 [1], 9.0 [2], 11.0 [3] |
| 1-[2-[(1R,3S,5R)-3-[(6-Bromopyridin-2-yl)carbamoyl]-2-azabicyclo[3.1.0]hexan-2-yl]-2-oxoethyl]indole-3-carboxamide | IC50 | 66.0 [1], 1860.0 [2] |
| (2-Carbamimidoyl-1-benzothiophen-6-yl) thiophene-2-carboxylate | IC50 | 96.0 [1], 98.0 [2] |
| Example 373 [WO2012093101] | IC50 | 1.0 [1] |
| (1R,3S,5R)-2-N-(1-Carbamoylindol-3-yl)-3-N-[6-(trifluoromethyl)pyridin-2-yl]-2-azabicyclo[3.1.0]hexane-2,3-dicarboxamide | IC50 | 14.0 [1], 22.0 [2] |
| (2s)-N-(6-Bromopyridin-2-Yl)-3-[(1h-Indazol-1-Yl)acetyl]-1,3-Thiazolidine-2-Carboxamide | IC50 | 77.0 [1], 2180.0 [2] |
| (1R,3S,5R)-2-N-(1-Carbamoylindol-3-yl)-3-N-[2-fluoro-3-(trifluoromethyl)phenyl]-2-azabicyclo[3.1.0]hexane-2,3-dicarboxamide | IC50 | 23.0 [1], 587.0 [2] |
| 1-[2-[(1R,3S,5R)-3-[(6-Bromopyridin-2-yl)carbamoyl]-2-azabicyclo[3.1.0]hexan-2-yl]-2-oxoethyl]pyrazolo[3,4-b]pyridine-3-carboxamide | IC50 | 31.95 [1], 47.0 [2] |
| (1R,3S,5R)-N-(6-Bromopyridin-2-yl)-2-(2-indazol-1-ylacetyl)-2-azabicyclo[3.1.0]hexane-3-carboxamide | IC50 | 19.0 [1], 6600.0 [2] |
| (1R,3S,5R)-2-[2-(3-Acetylindazol-1-yl)acetyl]-N-(6-bromopyridin-2-yl)-2-azabicyclo[3.1.0]hexane-3-carboxamide | IC50 | 15.0 [1], 35.0 [2] |
| 3-[3-(Aminomethyl)phenyl]-5-(3-methylbutanoylamino)-N-[(1S)-1,2,3,4-tetrahydronaphthalen-1-yl]benzamide | IC50 | 3400.0 [1], 11000.0 [2] |
| Tert-butyl 2-[1-carbamoyl-3-[[(1R,3S,5R)-3-[(3-chloro-2-fluorophenyl)methylcarbamoyl]-2-azabicyclo[3.1.0]hexane-2-carbonyl]amino]indol-6-yl]acetate | IC50 | 3.0 [1] |
| (2R)-1-N-(1-Carbamoylindol-3-yl)-2-N-[3-(trifluoromethoxy)phenyl]pyrrolidine-1,2-dicarboxamide | IC50 | 18300.0 [1], 30000.0 [2] |
| 2-[1-Carbamoyl-3-[[(2S,4R)-2-[(3-chloro-2-fluorophenyl)methylcarbamoyl]-4-fluoro-4-methylpyrrolidine-1-carbonyl]amino]indol-5-yl]oxyacetic acid | IC50 | 2.0 [1] |
| (2S,4S)-1-N-(1-Carbamoylindol-3-yl)-4-fluoro-2-N-[3-(trifluoromethoxy)phenyl]pyrrolidine-1,2-dicarboxamide | IC50 | 700.0 [1] |
| (2S)-1-N-(1-Carbamoylindol-3-yl)-4,4-difluoro-2-N-[3-(trifluoromethoxy)phenyl]pyrrolidine-1,2-dicarboxamide | IC50 | 450.0 [1] |
| (2S)-1-N-(1-Carbamoylindol-3-yl)-2-N-[3-(trifluoromethoxy)phenyl]piperidine-1,2-dicarboxamide | IC50 | 22000.0 [1], 22200.0 [2] |
| (2S,4R)-1-N-(1-Carbamoylindol-3-yl)-4-fluoro-2-N-[3-(trifluoromethoxy)phenyl]pyrrolidine-1,2-dicarboxamide | IC50 | 48.0 [1], 50.0 [2] |
| (2S,4S)-1-N-(1-Carbamoylindol-3-yl)-4-hydroxy-2-N-[3-(trifluoromethoxy)phenyl]pyrrolidine-1,2-dicarboxamide | IC50 | 1400.0 [1], 1425.0 [2] |
| (2S,4S)-4-Amino-1-N-(1-carbamoylindol-3-yl)-2-N-[3-(trifluoromethoxy)phenyl]pyrrolidine-1,2-dicarboxamide | IC50 | 500.0 [1], 667.0 [2] |
| (2S,4R)-1-N-(1-Carbamoylindol-3-yl)-4-methyl-2-N-[3-(trifluoromethoxy)phenyl]pyrrolidine-1,2-dicarboxamide | IC50 | 850.0 [1] |
| (2S,4S)-4-Amino-1-N-(1-carbamoylindol-3-yl)-2-N-(2-hydroxy-2-phenylethyl)pyrrolidine-1,2-dicarboxamide | IC50 | 24750.0 [1] |
| (1R,3S,5R)-2-N-(1-Carbamoylindol-3-yl)-3-N-[2-fluoro-3-(trifluoromethoxy)phenyl]-2-azabicyclo[3.1.0]hexane-2,3-dicarboxamide | IC50 | 12.0 [1], 250.0 [2] |
| (2S,4S)-1-N-(1-Carbamoylindol-3-yl)-4-methyl-2-N-[3-(trifluoromethoxy)phenyl]pyrrolidine-1,2-dicarboxamide | IC50 | 300.0 [1] |
| Isatoic anhydride | IC50 | 2900.0 [1] |
| 5-Methylsulfanyl-4-[4-(5-propyl-1-pyridin-2-ylpyrazol-4-yl)-1,3-thiazol-2-yl]thiophene-2-carboximidamide | IC50 | 3700.0 [1] |
| 2-[2-[[3-[3-[(1S)-1-Amino-2-hydroxyethyl]phenyl]-5-(hydroxymethyl)phenyl]methoxy]phenyl]acetic acid | IC50 | 4.0 [1] |
| 4-[(1R)-3-[4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-1-(ethylamino)-3-oxopropyl]benzonitrile | IC50 | 1.0 [1] |
| 2-Acetyloxy-5-(4-acetyloxy-3-carboxyphenyl)benzoic acid | IC50 | 100.0 [1] |
| 2-[2-[[3-[3-(2-Amino-2-oxoethyl)-2-fluorophenyl]-5-(1-methylpyrazol-4-yl)phenyl]methoxy]phenyl]acetic acid | IC50 | 23.0 [1] |
| (S)-N2-Benzhydryl-N1-(1-methyl-1H-indol-3-yl)pyrrolidine-1,2-dicarboxamide | IC50 | 5800.0 [1] |
| (1R,3S,5R)-2-N-(1-Carbamoylindol-3-yl)-3-N-(3-chlorophenyl)-2-azabicyclo[3.1.0]hexane-2,3-dicarboxamide | IC50 | 150.0 [1] |
| (2S)-1-N-(1-Methylindol-3-yl)-2-N-[3-(trifluoromethoxy)phenyl]pyrrolidine-1,2-dicarboxamide | IC50 | 20000.0 [1] |
| 3-[[3-[3-(Aminomethyl)anilino]-2H-pyrazolo[3,4-d]pyrimidin-4-yl]amino]phenol | IC50 | 20000.0 [1] |
| (2S)-2-[[4-[3-(Aminomethyl)anilino]quinazolin-2-yl]amino]-3-methylbutanoic acid | IC50 | 75000.0 [1] |
| (1R,2S)-2-[[4-[3-(Aminomethyl)anilino]quinazolin-2-yl]amino]cyclohexane-1-carboxylic acid | IC50 | 84000.0 [1] |
| N-[3-[3-(Aminomethyl)phenyl]phenyl]-3-methylbutanamide | IC50 | 120000.0 [1] |
| 3-[3-(Aminomethyl)phenyl]-N-[(1S)-1,2,3,4-tetrahydronaphthalen-1-yl]benzamide | IC50 | 54000.0 [1] |
| Methyl 3-[[(2S)-2-[[3-(trifluoromethoxy)phenyl]carbamoyl]pyrrolidine-1-carbonyl]amino]benzoate | IC50 | 30000.0 [1] |
| 3-[2-[(1R,3S,5R)-3-[[2-Fluoro-3-(trifluoromethoxy)phenyl]carbamoyl]-2-azabicyclo[3.1.0]hexan-2-yl]-2-oxoethyl]indole-1-carboxamide | IC50 | 370.0 [1] |
| Methyl 4-methyl-3-[[(2S)-2-[[3-(trifluoromethoxy)phenyl]carbamoyl]pyrrolidine-1-carbonyl]amino]benzoate | IC50 | 17000.0 [1] |
| (2S)-2-[[4-[3-(Aminomethyl)anilino]pyrimidin-2-yl]amino]-3-methylbutanoic acid | IC50 | 44000.0 [1] |
| N-[3-[3-(Aminomethyl)phenyl]phenyl]-2-phenylacetamide | IC50 | 43000.0 [1] |
| 3-[3-(Aminomethyl)phenyl]-N-benzylbenzamide | IC50 | 310000.0 [1] |
| N-[3-[3-(Aminomethyl)phenyl]phenyl]benzamide | IC50 | 257000.0 [1] |
| 3-[3-(Aminomethyl)phenyl]-N-[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]benzamide | IC50 | 98000.0 [1] |
| N-[3-[3-(Aminomethyl)phenyl]phenyl]acetamide | IC50 | 690000.0 [1] |
| N-[3-[3-(Aminomethyl)phenyl]phenyl]-3-phenylpropanamide | IC50 | 140000.0 [1] |
| (1R,3S,5R)-3-N-(3-Bromophenyl)-2-N-(1-carbamoylindol-3-yl)-2-azabicyclo[3.1.0]hexane-2,3-dicarboxamide | IC50 | 45.0 [1] |
| (1S,2S,5R)-3-N-(1-Carbamoylindol-3-yl)-2-N-[3-(trifluoromethoxy)phenyl]-3-azabicyclo[3.1.0]hexane-2,3-dicarboxamide | IC50 | 650.0 [1] |
| (1R,3S,5R)-2-N-(1-Carbamoylindol-3-yl)-3-N-[3-(difluoromethoxy)phenyl]-2-azabicyclo[3.1.0]hexane-2,3-dicarboxamide | IC50 | 150.0 [1] |
| (1R,3S,5R)-2-N-(1-Carbamoylindol-3-yl)-3-N-(3-methoxyphenyl)-2-azabicyclo[3.1.0]hexane-2,3-dicarboxamide | IC50 | 320.0 [1] |
| 1-[2-[(1R,3S,5R)-3-[(6-Bromopyridin-2-yl)carbamoyl]-2-azabicyclo[3.1.0]hexan-2-yl]-2-oxoethyl]-5-(fluoromethyl)pyrazolo[3,4-c]pyridine-3-carboxamide | IC50 | 2.0 [1] |
| 1-[2-[(1R,3S,5R)-3-[(6-Iodopyridin-2-yl)carbamoyl]-2-azabicyclo[3.1.0]hexan-2-yl]-2-oxoethyl]indazole-3-carboxamide | IC50 | 3.0 [1] |
| 5,7-Dimethyl-1-[2-oxo-2-[(1R,3S,5R)-3-[[6-(trifluoromethyl)pyridin-2-yl]carbamoyl]-2-azabicyclo[3.1.0]hexan-2-yl]ethyl]pyrazolo[3,4-c]pyridine-3-carboxamide | IC50 | 6.0 [1] |
| 2-Acetyloxy-5-[(4-acetyloxy-3-carboxyphenyl)methyl]benzoic acid | IC50 | 100.0 [1] |
| [(3S)-4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-ethylpiperazin-1-yl]-[(1R,2R)-1-amino-1,2,3,4-tetrahydronaphthalen-2-yl]methanone | IC50 | 2660.0 [1] |
| (3R)-3-Amino-1-[(3S)-4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-methylpiperazin-1-yl]-3-[4-(trifluoromethyl)phenyl]propan-1-one | IC50 | 40.0 [1] |
| 2-[(3S)-4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-methylpiperazine-1-carbonyl]-1H-indole-5-carbonitrile | IC50 | 15.0 [1] |
| (3R)-3-Amino-1-[4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-3-(4-methylphenyl)propan-1-one | IC50 | 70.0 [1] |
| 2-[(3S)-4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-propylpiperazine-1-carbonyl]-1H-indole-5-carbonitrile | IC50 | 11.0 [1] |
| (3R)-1-[4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-3-cyclohexyl-3-(methylamino)propan-1-one | IC50 | 80.0 [1] |
| 4-[(1R)-1-Amino-3-[(3S)-4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-propylpiperazin-1-yl]-3-oxopropyl]benzonitrile | IC50 | 10.0 [1] |
| (3R)-3-Amino-1-[(3S)-4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-phenylpiperazin-1-yl]-3-(4-fluorophenyl)propan-1-one | IC50 | 7.0 [1] |
| 4-[(1R)-3-[(3R,5S)-4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3,5-dimethylpiperazin-1-yl]-3-oxo-1-(propan-2-ylamino)propyl]benzonitrile | IC50 | 11.0 [1] |
| 4-[(1R)-1-Amino-3-[(3S)-4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-ethylpiperazin-1-yl]-3-oxopropyl]benzonitrile | IC50 | 7.0 [1] |
| 4-[(1R)-3-[4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-3-oxo-1-(propan-2-ylamino)propyl]benzonitrile | IC50 | 3.0 [1] |
| (3R)-3-Amino-1-[(3S)-4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-ethylpiperazin-1-yl]-3-[4-(trifluoromethyl)phenyl]propan-1-one | IC50 | 90.0 [1] |
| (3R)-3-Amino-1-[4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-3-cyclopentylpropan-1-one | IC50 | 100.0 [1] |
| 4-[(1R)-1-Amino-3-[(3S)-4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-methylpiperazin-1-yl]-3-oxopropyl]benzonitrile | IC50 | 9.0 [1] |
| (3R)-3-Amino-1-[(2R,5S)-4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-2,5-dimethylpiperazin-1-yl]-3-(4-fluorophenyl)propan-1-one | IC50 | 50.0 [1] |
| 3-[(1R)-1-Amino-3-[4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-3-oxopropyl]benzonitrile | IC50 | 40.0 [1] |
| 4-[(1R)-1-Amino-3-[4-[4-amino-8-fluoro-6-methoxy-7-(2-methoxyethoxy)quinazolin-2-yl]piperazin-1-yl]-3-oxopropyl]benzonitrile | IC50 | 110.0 [1] |
| 1-[4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-2-[(2S)-1-(2-methylpropyl)pyrrolidin-2-yl]ethanone | IC50 | 170.0 [1] |
| 4-[(E)-3-[(3S)-4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-methylpiperazin-1-yl]-3-oxoprop-1-enyl]benzonitrile | IC50 | 20.0 [1] |
| (3S)-3-Amino-1-[(3S)-4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-methylpiperazin-1-yl]-4-phenylbutan-1-one | IC50 | 2250.0 [1] |
| 4-[(1R)-1-Amino-3-[4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-3-oxopropyl]benzonitrile | IC50 | 10.0 [1] |
| 4-[(1R)-3-[4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-1-(methylamino)-3-oxopropyl]benzonitrile | IC50 | 4.0 [1] |
| (3R)-3-Amino-1-[4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-3-(2,4-difluorophenyl)propan-1-one | IC50 | 450.0 [1] |
| (3R)-3-Amino-1-[4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-3-(4-chlorophenyl)propan-1-one | IC50 | 90.0 [1] |
| (E)-1-[4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-3-cyclopropylprop-2-en-1-one | IC50 | 500.0 [1] |
| (3S)-3-Amino-1-[(3S)-4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-methylpiperazin-1-yl]-5-methylhexan-1-one | IC50 | 240.0 [1] |
| 1-[(3S)-4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-phenylpiperazin-1-yl]-2-[(2S)-piperidin-2-yl]ethanone | IC50 | 20.0 [1] |
| 1-[(3S)-4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-phenylpiperazin-1-yl]-2-[(2S)-azetidin-2-yl]ethanone | IC50 | 610.0 [1] |
| (3R)-3-Amino-1-[4-(4-amino-5-fluoro-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-3-(4-fluorophenyl)propan-1-one | IC50 | 30.0 [1] |
| (3R)-3-Amino-1-[4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-3-(furan-2-yl)propan-1-one | IC50 | 90.0 [1] |
| (3R)-1-[4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-3-(methylamino)-3-phenylpropan-1-one | IC50 | 50.0 [1] |
| (3R)-3-Amino-1-[(3S)-4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-propylpiperazin-1-yl]-3-[4-(trifluoromethyl)phenyl]propan-1-one | IC50 | 60.0 [1] |
| 1-[4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-2-[(3S)-piperidin-3-yl]ethanone | IC50 | 3870.0 [1] |
| [(3S)-4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-methylpiperazin-1-yl]-[(1R,2R)-1-amino-1,2,3,4-tetrahydronaphthalen-2-yl]methanone | IC50 | 1070.0 [1] |
| [(3S)-4-(4-Amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-methylpiperazin-1-yl]-(5-fluoro-1H-indol-2-yl)methanone | IC50 | 90.0 [1] |
| (3R)-3-Amino-1-[(3S)-4-(4-amino-8-fluoro-6,7-dimethoxyquinazolin-2-yl)-3-ethylpiperazin-1-yl]-3-(4-fluorophenyl)propan-1-one | IC50 | 30.0 [1] |