 | 4-(2-Benzyl-2,7-diazaspiro[3.4]octan-7-yl)-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidine | IC50 | 56.0 [1], 144.0 [2] |
 | 4-[2-(2-Methyl-4,5,6,7-tetrahydroindazol-4-yl)-2,7-diazaspiro[3.4]octan-7-yl]-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidine | IC50 | 120.0 [1], 385.0 [2] |
 | 4-(2-Benzyl-2,7-diazaspiro[4.5]decan-7-yl)-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidine | IC50 | 140.0 [1], 227.0 [2] |
 | [(6S)-5-Azaspiro[2.4]heptan-6-yl]-[7-[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]-2,7-diazaspiro[3.4]octan-2-yl]methanone | IC50 | 92.0 [1], 102.0 [2] |
 | 4-[2-[(1R)-1-(Azetidin-3-yl)-2-methylpropyl]-2,7-diazaspiro[3.4]octan-7-yl]-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidine | IC50 | 8.0 [1], 21.0 [2] |
 | 4-[2-[(1S)-1-(Azetidin-3-yl)-2-methylpropyl]-2,7-diazaspiro[3.4]octan-7-yl]-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidine | IC50 | 110.0 [1], 190.0 [2] |
 | 4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-propylthieno[2,3-d]pyrimidine | IC50 | 450.0 [1] |
 | CID 91667931 | IC50 | 14.0 [1] |
 | 6-Hydroxy-1-(1H-pyrazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 21.0 [1] |
 | CID 72201086 | IC50 | 46.0 [1] |
 | CID 90455046 | IC50 | 15.0 [1] |
 | 4-(3-(4-(Hydroxy(phenyl)cyclopentylmethyl)piperidine-1-yl)propyloxy)benzonitrile | IC50 | 390.0 [1] |
 | 4-[3-[4-(Cyclopentyl-hydroxy-pyridin-2-ylmethyl)piperidin-1-yl]propoxy]benzenesulfonamide | IC50 | 114.0 [1] |
 | 4-[3-[4-[Cyclopentyl-(3,5-difluorophenyl)-hydroxymethyl]piperidin-1-yl]propoxy]benzonitrile | IC50 | 437.0 [1] |
 | 4-[3-[4-(Cyclopentyl-hydroxy-pyridin-2-ylmethyl)piperidin-1-yl]propoxy]benzonitrile | IC50 | 302.0 [1] |
 | 4-[3-[4-[Cyclopentyl-(3-fluorophenyl)-hydroxymethyl]piperidin-1-yl]propoxy]benzonitrile | IC50 | 197.0 [1] |
 | 4-[3-[4-[(3-Chlorophenyl)-cyclopentyl-hydroxymethyl]piperidin-1-yl]propoxy]benzonitrile | IC50 | 226.0 [1] |
 | 4-[3-[4-[Cyclopentyl-hydroxy-(1,3-thiazol-2-yl)methyl]piperidin-1-yl]propoxy]benzonitrile | IC50 | 242.0 [1] |
 | 5-[[4-[[6-(2,2,2-Trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrile | IC50 | 31.0 [1] |
 | 4-Methyl-1-(2H-triazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 23.0 [1] |
 | 1-(3-Hydroxy-2-propan-2-yloxypropyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 23.0 [1] |
 | 1-(2-Hydroxyethyl)-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 44.0 [1] |
 | 2-[2-Cyano-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indol-1-yl]acetamide | IC50 | 27.0 [1] |
 | 6-Methoxy-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrile | IC50 | 40.0 [1] |
 | 6-Hydroxy-1-(2-hydroxyethyl)-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 27.0 [1] |
 | 6-Hydroxy-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrile | IC50 | 27.0 [1] |
 | 2-[2-Cyano-6-methoxy-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indol-1-yl]acetamide | IC50 | 37.0 [1] |
 | 1-(2-Hydroxyethyl)-6-methoxy-4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 16.0 [1] |
 | 6-Methoxy-1-(1H-pyrazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 24.0 [1] |
 | 6-Hydroxy-4-methyl-1-(1H-pyrazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 18.0 [1] |
 | 6-Methoxy-4-methyl-1-(1H-pyrazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 12.0 [1] |
 | 6-Hydroxy-4-methyl-1-(2H-triazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 17.0 [1] |
 | 6-Methoxy-4-methyl-1-(2H-triazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 16.0 [1] |
 | 3-Methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrile | IC50 | 111.0 [1] |
 | 4-[3-[4-[Hydroxy-pyridin-2-yl-(1,3-thiazol-2-yl)methyl]piperidin-1-yl]propoxy]benzonitrile | IC50 | 90.0 [1] |
 | 4-[3-[4-[Hydroxy-pyridin-2-yl-(1,3-thiazol-2-yl)methyl]piperidin-1-yl]propoxy]benzenesulfonamide | IC50 | 246.0 [1] |
 | 1-(2,3-Dihydroxypropyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 37.0 [1] |
 | (2S)-2-Acetamido-N-[(2S)-1-[[(3S,6S,9S,15R,28S)-15-benzyl-3-[3-(diaminomethylideneamino)propyl]-6-methyl-2,5,8,14,17,27-hexaoxo-1,4,7,13,16,26-hexazatricyclo[26.3.0.09,13]hentriacontan-18-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-5-(diaminomethylideneamino)pentanamide | Ki | 23.8 [1] |
 | 4-(4-(4-Chlorobenzyl)piperazin-1-yl)-6-ethylthieno[2,3-d]pyrimidine | IC50 | 14000.0 [1] |
 | 6-Ethyl-4-(4-(thiazol-2-yl)piperazin-1-yl)thieno[2,3-d]pyrimidine | IC50 | 46000.0 [1] |
 | 6-Butyl-4-(4-(5,5-dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)thieno[2,3-d]pyrimidine | IC50 | 750.0 [1] |
 | 4-(4-(1,3,4-Thiadiazol-2-yl)piperazin-1-yl)-6-ethylthieno[2,3-d]pyrimidine | IC50 | 193000.0 [1] |
 | 4-[3-[4-[(3-Fluorophenyl)-hydroxy-(1,3-thiazol-2-yl)methyl]piperidin-1-yl]propoxy]benzenesulfonamide | IC50 | 354.0 [1] |
 | 4-[3-[4-[(3-Fluorophenyl)-hydroxy-(1,3-thiazol-2-yl)methyl]piperidin-1-yl]propoxy]benzonitrile | IC50 | 460.0 [1] |
 | 6-Ethyl-4-(4-pyridin-2-ylpiperazin-1-yl)thieno[2,3-d]pyrimidine | IC50 | 58000.0 [1] |
 | 4-(4-Benzylpiperazin-1-yl)-6-ethylthieno[2,3-d]pyrimidine | IC50 | 52000.0 [1] |
 | 6-Ethyl-4-(4-(pyrimidin-2-yl)piperazin-1-yl)thieno[2,3-d]pyrimidine | IC50 | 87000.0 [1] |
 | 3-Fluoro-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrile | IC50 | 96.0 [1] |
 | 1-(2-Hydroxyethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 35.0 [1] |
 | 6-Hydroxy-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrile | IC50 | 20.0 [1] |
 | 4-[3-[4-(Cyclopentyl-hydroxy-piperidin-2-ylmethyl)piperidin-1-yl]propoxy]benzonitrile | IC50 | 28000.0 [1] |
 | 4-[3-[4-[Cyclopentyl-hydroxy-(3-methoxyphenyl)methyl]piperidin-1-yl]propoxy]benzonitrile | IC50 | 1100.0 [1] |
 | 2-[2-Cyano-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indol-1-yl]acetamide | IC50 | 25.0 [1] |
 | 6-Methoxy-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrile | IC50 | 22.0 [1] |
 | 1-[(2R)-2,3-Dihydroxypropyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 46.0 [1] |
 | 1-[(2S)-3-Hydroxy-2-methoxypropyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 37.0 [1] |
 | 1-(2H-Triazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 27.0 [1] |
 | 6-Ethoxy-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrile | IC50 | 47.0 [1] |
 | 4-Chloro-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrile | IC50 | 22.0 [1] |
 | 1-[(2S)-2,3-Dihydroxypropyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 42.0 [1] |
 | 1-(2-Hydroxy-3-methoxypropyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 101.0 [1] |
 | 1-[(2R)-3-Hydroxy-2-methoxypropyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 40.0 [1] |
 | 2-[2-Cyano-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indol-1-yl]propanamide | IC50 | 244.0 [1] |
 | 1-(1H-Pyrazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile | IC50 | 23.0 [1] |
 | 6-Fluoro-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrile | IC50 | 109.0 [1] |
 | 3-Amino-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2-carbonitrile | IC50 | 124.0 [1] |
 | 6-Methylsulfanyl-4-[4-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]piperazin-1-yl]thieno[2,3-d]pyrimidine | IC50 | 20000.0 [1] |
 | 6-Propyl-4-[4-[5-(trifluoromethyl)-1H-1,2,4-triazol-3-yl]piperazin-1-yl]thieno[2,3-d]pyrimidine | IC50 | 200000.0 [1] |
 | 6-(2-Chloroethyl)-4-[4-(5,5-dimethyl-4H-1,3-thiazol-2-yl)piperazin-1-yl]thieno[2,3-d]pyrimidine | IC50 | 193.0 [1] |
 | 6-Ethyl-4-[4-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]piperazin-1-yl]thieno[2,3-d]pyrimidine | IC50 | 1300.0 [1] |
 | 2-[4-[6-(2,2,2-Trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]piperazin-1-yl]-5-(trifluoromethyl)-1,3,4-oxadiazole | IC50 | 1400.0 [1] |
 | 6-Cyclopropyl-4-[4-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]piperazin-1-yl]thieno[2,3-d]pyrimidine | IC50 | 2000.0 [1] |
 | 6-Propyl-4-[4-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]piperazin-1-yl]thieno[2,3-d]pyrimidine | IC50 | 650.0 [1] |
 | 4-[4-(5,5-Dimethyl-4H-1,3-thiazol-2-yl)piperazin-1-yl]-6-(1,1,1-trifluoropropan-2-yl)thieno[2,3-d]pyrimidine | IC50 | 765.0 [1] |