 | Telcagepant | IC50 | 2.4 [1] |
 | N-[(2R)-1'-Methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]-2-(2-oxo-3-pyridin-2-ylbenzimidazol-1-yl)acetamide | IC50 | 78.0 [1] |
 | N-[(2R)-1'-Methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]-2-(2-oxo-3-pyridin-2-ylbenzimidazol-1-yl)acetamide | Ki | 20.0 [1], 21.0 [2] |
 | 2-(2,10-Dioxo-1,3,9-triazatricyclo[6.3.1.04,12]dodeca-4,6,8(12)-trien-3-yl)-N-[(2S)-2'-oxospiro[1,3-dihydroindene-2,3'-1H-pyrrolo[2,3-b]pyridine]-5-yl]acetamide | IC50 | 0.28 [1] |
 | 2-(2,10-Dioxo-1,3,9-triazatricyclo[6.3.1.04,12]dodeca-4,6,8(12)-trien-3-yl)-N-[(2S)-2'-oxospiro[1,3-dihydroindene-2,3'-1H-pyrrolo[2,3-b]pyridine]-5-yl]acetamide | Ki | 0.04 [1] |
 | Olcegepant | IC50 | 0.02 [1], 0.03 [2], 4.0 [3] |
 | Olcegepant | Ki | 0.01 [1] |
 | 2-[3-[2-(Dimethylamino)-2-oxoethyl]-4,6-dimethyl-2-oxobenzimidazol-1-yl]-N-[(2R)-1'-methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]acetamide | IC50 | 12.0 [1], 14.0 [2], 23.0 [3] |
 | 2-[3-[2-(Dimethylamino)-2-oxoethyl]-4,6-dimethyl-2-oxobenzimidazol-1-yl]-N-[(2R)-1'-methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]acetamide | Ki | 1.7 [1] |
 | 2-(2,10-Dioxo-1,3,9-triazatricyclo[6.3.1.04,12]dodeca-4,6,8(12)-trien-3-yl)-N-[(2R)-1'-methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]acetamide | IC50 | 2.4 [1], 5.4 [2] |
 | 2-(2,10-Dioxo-1,3,9-triazatricyclo[6.3.1.04,12]dodeca-4,6,8(12)-trien-3-yl)-N-[(2R)-1'-methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]acetamide | Ki | 0.51 [1] |
 | 2-(6,9-Dimethyl-2,10-dioxo-1,3,9-triazatricyclo[6.3.1.04,12]dodeca-4(12),5,7-trien-3-yl)-N-[(2R)-1'-methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]acetamide | IC50 | 0.88 [1], 13.0 [2], 31.0 [3], 220.0 [4] |
 | 2-(6,9-Dimethyl-2,10-dioxo-1,3,9-triazatricyclo[6.3.1.04,12]dodeca-4(12),5,7-trien-3-yl)-N-[(2R)-1'-methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]acetamide | Ki | 0.23 [1], 7.1 [2] |
 | 4-(8-Fluoro-2-oxo-1,4-dihydroquinazolin-3-yl)-N-[(2R)-3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-piperidin-1-ylpiperidin-1-yl)propan-2-yl]piperidine-1-carboxamide | IC50 | 0.03 [1] |
 | 4-(8-Fluoro-2-oxo-1,4-dihydroquinazolin-3-yl)-N-[(2R)-3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-piperidin-1-ylpiperidin-1-yl)propan-2-yl]piperidine-1-carboxamide | Ki | 0.01 [1] |
 | 4-(2-Oxo-3H-imidazo[4,5-b]pyridin-1-yl)-N-[(3R)-2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepin-3-yl]piperidine-1-carboxamide | IC50 | 49.0 [1], 730.0 [2] |
 | 4-(2-Oxo-3H-imidazo[4,5-b]pyridin-1-yl)-N-[(3R)-2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepin-3-yl]piperidine-1-carboxamide | Ki | 22.0 [1], 23.0 [2] |
 | N-[(2R)-1'-Methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]-2-(2-oxo-3H-benzimidazol-1-yl)acetamide | IC50 | 110.0 [1], 120.0 [2], 1200.0 [3] |
 | N-[(2R)-1'-Methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]-2-(2-oxo-3H-benzimidazol-1-yl)acetamide | Ki | 38.0 [1], 43.0 [2] |
 | N-[(2R)-1'-Methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]-2-[2-oxo-3-(oxolan-3-yl)benzimidazol-1-yl]acetamide | IC50 | 61.0 [1], 170.0 [2] |
 | N-[(2R)-1'-Methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]-2-[2-oxo-3-(oxolan-3-yl)benzimidazol-1-yl]acetamide | Ki | 20.0 [1] |
 | N-[(2R)-1'-Methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]-2-(3,4,6-trimethyl-2-oxobenzimidazol-1-yl)acetamide | IC50 | 10.0 [1], 370.0 [2], 1200.0 [3] |
 | N-[(2R)-1'-Methyl-2',4'-dioxospiro[1,3-dihydroindene-2,5'-imidazolidine]-5-yl]-2-(3,4,6-trimethyl-2-oxobenzimidazol-1-yl)acetamide | Ki | 2.7 [1] |
 | 2-[(8R)-8-(3,5-Difluorophenyl)-8-methyl-10-oxo-6,9-diazaspiro[4.5]decan-9-yl]-N-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6'-5,7-dihydrocyclopenta[b]pyridine]-3'-yl]acetamide | IC50 | 0.23 [1], 0.34 [2] |
 | 2-[(8R)-8-(3,5-Difluorophenyl)-8-methyl-10-oxo-6,9-diazaspiro[4.5]decan-9-yl]-N-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6'-5,7-dihydrocyclopenta[b]pyridine]-3'-yl]acetamide | Ki | 0.05 [1] |
 | 4-(2-Oxo-3H-benzimidazol-1-yl)-N-[(3R)-2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepin-3-yl]piperidine-1-carboxamide | IC50 | 1583.0 [1] |
 | 4-(2-Oxo-3H-benzimidazol-1-yl)-N-[(3R)-2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepin-3-yl]piperidine-1-carboxamide | Ki | 2200.0 [1], 2250.0 [2] |
 | 4-(2,4-Dioxoimidazolidin-1-yl)-N-[(3R)-2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepin-3-yl]piperidine-1-carboxamide | IC50 | 100.0 [1] |
 | 4-(2,4-Dioxoimidazolidin-1-yl)-N-[(3R)-2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepin-3-yl]piperidine-1-carboxamide | Ki | 29.0 [1], 520.0 [2] |
 | 2-[(8R)-8-(3,5-Difluorophenyl)-6,8-dimethyl-10-oxo-6,9-diazaspiro[4.5]decan-9-yl]-N-[(2R)-2'-oxospiro[1,3-dihydroindene-2,3'-1H-pyrrolo[2,3-b]pyridine]-5-yl]acetamide | IC50 | 0.1 [1], 0.39 [2] |
 | 2-[(8R)-8-(3,5-Difluorophenyl)-6,8-dimethyl-10-oxo-6,9-diazaspiro[4.5]decan-9-yl]-N-[(2R)-2'-oxospiro[1,3-dihydroindene-2,3'-1H-pyrrolo[2,3-b]pyridine]-5-yl]acetamide | Ki | 0.05 [1] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-3-(2-methoxypropan-2-yl)-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-2-oxospiro[1H-pyrido[2,3-d][1,3]oxazine-4,4'-piperidine]-1'-carboxamide | IC50 | 0.24 [1], 0.63 [2] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-3-(2-methoxypropan-2-yl)-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-2-oxospiro[1H-pyrido[2,3-d][1,3]oxazine-4,4'-piperidine]-1'-carboxamide | Ki | 0.05 [1] |
 | [1-[6-Chloro-4-(dimethylcarbamoyl)pyridin-2-yl]-2-(7-methyl-1H-indazol-5-yl)ethyl] 4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate | IC50 | 0.07 [1] |
 | [1-[6-Chloro-4-(dimethylcarbamoyl)pyridin-2-yl]-2-(7-methyl-1H-indazol-5-yl)ethyl] 4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate | Ki | 0.07 [1], 0.18 [2] |
 | CID 73352948 | IC50 | 1.7 [1], 2.0 [2] |
 | CID 73352948 | Ki | 0.03 [1] |
 | N-[(3R,6S)-1-(Cyclopropylmethyl)-2-oxo-6-phenylazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 38.0 [1], 340.0 [2] |
 | N-[(3R,6S)-1-(Cyclopropylmethyl)-2-oxo-6-phenylazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 11.0 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-1-(2-methylsulfinylethyl)-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 5.0 [1], 8.0 [2] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-1-(2-methylsulfinylethyl)-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 1.7 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-1-(2-methylsulfonylethyl)-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 2.0 [1], 3.0 [2] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-1-(2-methylsulfonylethyl)-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 0.5 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-1-methyl-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 8.0 [1], 22.0 [2] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-1-methyl-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 2.7 [1] |
 | N-[(3R,6S)-1-(2,2-Difluoroethyl)-6-(2,3-difluorophenyl)-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 5.0 [1], 15.0 [2] |
 | N-[(3R,6S)-1-(2,2-Difluoroethyl)-6-(2,3-difluorophenyl)-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 0.9 [1] |
 | N-[(3R,6S)-6-(2-Fluorophenyl)-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 65.0 [1], 120.0 [2] |
 | N-[(3R,6S)-6-(2-Fluorophenyl)-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 22.0 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-1-(2-methoxyethyl)-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 2.0 [1], 3.0 [2] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-1-(2-methoxyethyl)-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 0.3 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-1-ethyl-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 6.0 [1], 30.0 [2] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-1-ethyl-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 2.4 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(pyridin-2-ylmethyl)azepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 2.0 [1], 10.0 [2] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(pyridin-2-ylmethyl)azepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 0.9 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 14.0 [1], 22.0 [2] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 3.6 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(6-oxo-1H-pyridazin-5-yl)piperidine-1-carboxamide | IC50 | 44.0 [1], 112.0 [2] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(6-oxo-1H-pyridazin-5-yl)piperidine-1-carboxamide | Ki | 10.0 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-1-(2-methylsulfanylethyl)-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 2.0 [1], 8.0 [2] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-1-(2-methylsulfanylethyl)-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 0.7 [1] |
 | 4-(2-Oxo-3H-imidazo[4,5-b]pyridin-1-yl)-N-[(3R,6S)-2-oxo-6-phenylazepan-3-yl]piperidine-1-carboxamide | IC50 | 520.0 [1], 700.0 [2] |
 | 4-(2-Oxo-3H-imidazo[4,5-b]pyridin-1-yl)-N-[(3R,6S)-2-oxo-6-phenylazepan-3-yl]piperidine-1-carboxamide | Ki | 83.0 [1] |
 | N-[(3R,6S)-6-(3-Fluorophenyl)-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 220.0 [1], 250.0 [2] |
 | N-[(3R,6S)-6-(3-Fluorophenyl)-2-oxoazepan-3-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 51.0 [1] |
 | N-(1-Methyl-2-oxo-5-phenylpyridin-3-yl)-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 495.0 [1], 10900.0 [2] |
 | N-(1-Methyl-2-oxo-5-phenylpyridin-3-yl)-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 498.0 [1] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-3-[1-(trifluoromethyl)cyclopropyl]-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,4'-piperidine]-1'-carboxamide | IC50 | 1.4 [1], 8.6 [2] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-3-[1-(trifluoromethyl)cyclopropyl]-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,4'-piperidine]-1'-carboxamide | Ki | 0.63 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-2-oxospiro[1,3-dihydro-1,8-naphthyridine-4,4'-piperidine]-1'-carboxamide | IC50 | 11.0 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-2-oxospiro[1,3-dihydro-1,8-naphthyridine-4,4'-piperidine]-1'-carboxamide | Ki | 3.5 [1] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-3-phenyl-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 2.6 [1], 34.0 [2] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-3-phenyl-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 1.1 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-oxo-2-phenyl-1,3,8-triazaspiro[4.5]dec-1-ene-8-carboxamide | IC50 | 23.0 [1], 871.0 [2] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-oxo-2-phenyl-1,3,8-triazaspiro[4.5]dec-1-ene-8-carboxamide | Ki | 30.0 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-2-oxospiro[1H-3,1-benzoxazine-4,4'-piperidine]-1'-carboxamide | IC50 | 60.0 [1], 792.0 [2] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-2-oxospiro[1H-3,1-benzoxazine-4,4'-piperidine]-1'-carboxamide | Ki | 46.0 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,4'-piperidine]-1'-carboxamide | IC50 | 3.3 [1], 11.0 [2] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,4'-piperidine]-1'-carboxamide | Ki | 1.7 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-1-oxo-3-phenyl-2,8-diazaspiro[4.5]decane-8-carboxamide | IC50 | 120.0 [1], 692.0 [2] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-1-oxo-3-phenyl-2,8-diazaspiro[4.5]decane-8-carboxamide | Ki | 380.0 [1] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-3-propan-2-yl-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 0.62 [1], 3.2 [2] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-3-propan-2-yl-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 0.69 [1] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-2-(hydroxymethyl)-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 12.0 [1], 26.0 [2] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-2-(hydroxymethyl)-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 3.2 [1] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 6.7 [1], 19.0 [2] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 3.1 [1] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-2-methyl-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 8.7 [1], 28.0 [2] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-2-methyl-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 4.0 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-2-oxospiro[1H-pyrido[2,3-d][1,3]oxazine-4,4'-piperidine]-1'-carboxamide | IC50 | 2.7 [1], 13.0 [2] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-2-oxospiro[1H-pyrido[2,3-d][1,3]oxazine-4,4'-piperidine]-1'-carboxamide | Ki | 1.1 [1] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-2-(2,2,2-trifluoroethyl)-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 7.2 [1], 33.0 [2] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-2-(2,2,2-trifluoroethyl)-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 3.9 [1] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-2,4-dioxo-1,3,8-triazaspiro[4.5]decane-8-carboxamide | IC50 | 94.0 [1], 122.0 [2] |
 | N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-2,4-dioxo-1,3,8-triazaspiro[4.5]decane-8-carboxamide | Ki | 46.0 [1] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-3-(2,2,2-trifluoroethyl)-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-2-oxospiro[1H-pyrido[2,3-d][1,3]oxazine-4,4'-piperidine]-1'-carboxamide | IC50 | 0.41 [1], 2.0 [2] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-3-(2,2,2-trifluoroethyl)-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-2-oxospiro[1H-pyrido[2,3-d][1,3]oxazine-4,4'-piperidine]-1'-carboxamide | Ki | 0.07 [1] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-3-(1,3-thiazol-2-yl)-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | IC50 | 3.6 [1], 64.0 [2] |
 | N-[(6S,9R)-6-(2,3-Difluorophenyl)-3-(1,3-thiazol-2-yl)-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Ki | 1.1 [1] |