| CID 68379135 | IC50 | 67.0 [1], 70.0 [2], 74.0 [3] |
| GPR4 antagonist 1 | IC50 | 55.0 [1], 110.0 [2], 114.0 [3] |
| 4-[2,2-Dimethylpropyl-[[4-[3-(4-propan-2-ylpiperazin-1-yl)prop-1-ynyl]phenyl]methyl]amino]pyrimidine-2-carbonitrile | IC50 | 1930.0 [1], 23000.0 [2] |
| 4-[2,2-Dimethylpropyl-[[4-[(E)-3-(4-piperidin-1-ylpiperidin-1-yl)prop-1-enyl]phenyl]methyl]amino]pyrimidine-2-carbonitrile | IC50 | 490.0 [1], 23000.0 [2] |
| 4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-2-one | IC50 | 27.0 [1], 890.0 [2] |
| (2R)-3-[4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-1-yl]propane-1,2-diol | IC50 | 21.0 [1], 67.0 [2] |
| 2-Ethyl-5,7-dimethyl-3-[[4-[3-(4-propan-2-ylpiperazin-1-yl)propyl]phenyl]methyl]pyrazolo[1,5-a]pyrimidine | IC50 | 13.0 [1], 20.0 [2] |
| 3-[(2-Ethyl-5,7-dimethylimidazo[4,5-b]pyridin-3-yl)methyl]-8-(piperidin-1-ylmethyl)-6,11-dihydro-5H-benzo[b][1]benzazepine | IC50 | 67.0 [1] |
| 3-[(2-Ethylbenzimidazol-1-yl)methyl]-6,11-dihydro-5H-benzo[b][1]benzazepine | IC50 | 10000.0 [1] |
| 3-(Benzimidazol-1-ylmethyl)-6,11-dihydro-5H-benzo[b][1]benzazepine | IC50 | 10000.0 [1] |
| 3-[(2-Ethyl-5,7-dimethylimidazo[4,5-b]pyridin-3-yl)methyl]-10H-phenothiazine | IC50 | 910.0 [1] |
| N-[4-(Dimethylamino)butyl]-4-[[2,2-dimethylpropyl-(2,6-dimethylpyrimidin-4-yl)amino]methyl]benzamide | IC50 | 160.0 [1] |
| 1-[2-[1-[4-[[2,2-Dimethylpropyl-(2,6-dimethylpyrimidin-4-yl)amino]methyl]phenyl]triazol-4-yl]ethyl]piperidin-4-ol | IC50 | 50.0 [1] |
| 2-Chloro-N-(2,2-dimethylpropyl)-N-[[4-[(E)-3-(4-piperidin-1-ylpiperidin-1-yl)prop-1-enyl]phenyl]methyl]pyrimidin-4-amine | IC50 | 360.0 [1] |
| N-(2,2-Dimethylpropyl)-2-methoxy-N-[[4-[3-(4-propan-2-ylpiperazin-1-yl)prop-1-ynyl]phenyl]methyl]pyrimidin-4-amine | IC50 | 140.0 [1] |
| 4-N-(2,2-Dimethylpropyl)-2-N,2-N-dimethyl-4-N-[[4-[(E)-3-(4-piperidin-1-ylpiperidin-1-yl)prop-1-enyl]phenyl]methyl]pyrimidine-2,4-diamine | IC50 | 4800.0 [1] |
| 2-Chloro-N-(2,2-dimethylpropyl)-N-[[4-[3-(4-propan-2-ylpiperazin-1-yl)prop-1-ynyl]phenyl]methyl]pyrimidin-4-amine | IC50 | 300.0 [1] |
| 6-Ethyl-2,4-dimethyl-7-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]pyrrolo[2,3-d]pyrimidine | IC50 | 11600.0 [1] |
| 5,7-Dimethyl-2-propan-2-yl-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]imidazo[4,5-b]pyridine | IC50 | 2440.0 [1] |
| N-(2,2-Dimethylpropyl)-2,6-dimethyl-N-[[4-[3-(4-propan-2-ylpiperazin-1-yl)prop-1-ynyl]phenyl]methyl]pyrimidin-4-amine | IC50 | 800.0 [1] |
| N-(2,2-Dimethylpropyl)-2-methyl-N-[[4-[(E)-3-(4-piperidin-1-ylpiperidin-1-yl)prop-1-enyl]phenyl]methyl]pyrimidin-4-amine | IC50 | 380.0 [1] |
| 2-Ethyl-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]imidazo[4,5-b]pyridine | IC50 | 9100.0 [1] |
| N-(2,2-Dimethylpropyl)-2,6-dimethyl-N-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]pyrimidin-4-amine | IC50 | 330.0 [1] |
| 5-(Dimethylamino)-N-[4-[[2,2-dimethylpropyl-(2,6-dimethylpyrimidin-4-yl)amino]methyl]phenyl]pentanamide | IC50 | 200.0 [1] |
| N-(2,2-Dimethylpropyl)-N-[[4-[(E)-3-(4-piperidin-1-ylpiperidin-1-yl)prop-1-enyl]phenyl]methyl]-6-(trifluoromethyl)pyrimidin-4-amine | IC50 | 2970.0 [1] |
| N-(2,2-Dimethylpropyl)-2-methoxy-N-[[4-[(E)-3-(4-piperidin-1-ylpiperidin-1-yl)prop-1-enyl]phenyl]methyl]pyrimidin-4-amine | IC50 | 700.0 [1] |
| 5,7-Dimethyl-2-(2-methylpropyl)-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]imidazo[4,5-b]pyridine | IC50 | 7310.0 [1] |
| N-(2,2-Dimethylpropyl)-2,6-dimethyl-N-[[4-[(E)-3-(4-piperidin-1-ylpiperidin-1-yl)prop-1-enyl]phenyl]methyl]pyrimidin-4-amine | IC50 | 410.0 [1] |
| 4-[3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]propyl]-1-propan-2-ylpiperidin-4-ol | IC50 | 63.0 [1] |
| 2-Ethyl-6,8-dimethyl-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]imidazo[1,2-b]pyridazine | IC50 | 74.0 [1] |
| 3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]-1-piperidin-4-ylpropan-1-ol | IC50 | 24.0 [1] |
| 2-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]-5-piperazin-1-yl-1,3,4-oxadiazole | IC50 | 368.0 [1] |
| 3-[(2-Ethyl-5,7-dimethylimidazo[4,5-b]pyridin-3-yl)methyl]-6,11-dihydro-5H-benzo[b][1]benzazepine | IC50 | 900.0 [1] |
| 4-[(2-Ethyl-5,7-dimethylimidazo[4,5-b]pyridin-3-yl)methyl]-N-phenylaniline | IC50 | 10000.0 [1] |
| 5,7-Dimethyl-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]-2-propylimidazo[4,5-b]pyridine | IC50 | 760.0 [1] |
| 2,5,7-Trimethyl-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]imidazo[4,5-b]pyridine | IC50 | 410.0 [1] |
| 1-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-2-one | IC50 | 73.0 [1] |
| 4-[3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]propyl]piperidin-4-ol | IC50 | 50.0 [1] |
| 3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]-1-piperazin-1-ylpropan-1-one | IC50 | 53.0 [1] |
| 2-Ethyl-5,7-dimethyl-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]pyrazolo[1,5-a]pyrimidine | IC50 | 43.0 [1] |
| 3-[(2-Ethyl-5,7-dimethylimidazo[4,5-b]pyridin-3-yl)methyl]-8-[(4-methylpiperazin-1-yl)methyl]-6,11-dihydro-5H-benzo[b][1]benzazepine | IC50 | 130.0 [1] |
| 4-[5-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]-1,3,4-oxadiazol-2-yl]cyclohexan-1-amine | IC50 | 5.0 [1] |
| [4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-1-yl]-[(2S,3R)-3-hydroxypyrrolidin-2-yl]methanone | IC50 | 35.0 [1] |
| 2-Ethyl-5,7-dimethyl-3-[[4-[4-(piperazin-1-ylmethyl)triazol-1-yl]phenyl]methyl]pyrazolo[1,5-a]pyrimidine | IC50 | 38.0 [1] |
| 2-Ethyl-3-[[4-[(E)-3-[(3S)-3-(methoxymethyl)piperazin-1-yl]prop-1-enyl]phenyl]methyl]-5,7-dimethylpyrazolo[1,5-a]pyrimidine | IC50 | 33.0 [1] |
| 2-Ethyl-5,7-dimethyl-3-[[4-[(E)-3-piperazin-1-ylprop-1-enyl]phenyl]methyl]pyrazolo[1,5-a]pyrimidine | IC50 | 10.0 [1] |
| 2-Amino-1-[4-[(E)-3-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-1-yl]ethanone | IC50 | 38.0 [1] |
| (2S)-1-[4-[5-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]-1,3,4-oxadiazol-2-yl]piperidin-1-yl]-3-hydroxy-2-(methylamino)propan-1-one | IC50 | 15.0 [1] |
| Tert-butyl 4-[3-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]propanoyl]piperazine-1-carboxylate | IC50 | 54.0 [1] |
| 1-[[1-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]pyrazol-4-yl]methyl]azetidin-3-ol | IC50 | 118.0 [1] |
| 2-Ethyl-5,7-dimethyl-3-[[4-[4-(piperazin-1-ylmethyl)pyrazol-1-yl]phenyl]methyl]pyrazolo[1,5-a]pyrimidine | IC50 | 43.0 [1] |
| Tert-butyl 4-[(E)-2-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]ethenyl]-4-hydroxypiperidine-1-carboxylate | IC50 | 45.0 [1] |
| 2-Ethyl-5,7-dimethyl-3-[[4-[(E)-3-[(3S)-3-methylpiperazin-1-yl]prop-1-enyl]phenyl]methyl]pyrazolo[1,5-a]pyrimidine | IC50 | 19.0 [1] |
| 2-Ethyl-5,7-dimethyl-3-[[4-[(E)-3-[4-(1-methyltetrazol-5-yl)piperidin-1-yl]prop-1-enyl]phenyl]methyl]pyrazolo[1,5-a]pyrimidine | IC50 | 33.0 [1] |
| Tert-butyl 4-[3-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]propyl]-4-hydroxypiperidine-1-carboxylate | IC50 | 47.0 [1] |
| 4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperidin-4-ol | IC50 | 44.0 [1] |
| Tert-butyl N-[2-[4-[(E)-3-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]-4-hydroxypiperidin-1-yl]-2-oxoethyl]-N-methylcarbamate | IC50 | 34.0 [1] |
| [(2S)-4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-2-yl]methanol | IC50 | 28.0 [1] |
| 4-[[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenoxy]methyl]cyclohexan-1-amine | IC50 | 35.0 [1] |
| Tert-butyl 4-[2-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenoxy]ethyl]piperazine-1-carboxylate | IC50 | 44.0 [1] |
| 1-[[1-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]pyrazol-4-yl]methyl]piperidin-4-amine | IC50 | 26.0 [1] |
| Tert-butyl 3-[(E)-3-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]-3-hydroxyazetidine-1-carboxylate | IC50 | 34.0 [1] |
| 4-[2-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenoxy]ethyl]piperidin-4-ol | IC50 | 110.0 [1] |
| 2-Ethyl-3-[[4-[2-[(3R)-3-(methoxymethyl)piperazin-1-yl]ethoxy]phenyl]methyl]-5,7-dimethylpyrazolo[1,5-a]pyrimidine | IC50 | 59.0 [1] |
| 2-Ethyl-5,7-dimethyl-3-[[4-(piperidin-4-ylmethoxy)phenyl]methyl]pyrazolo[1,5-a]pyrimidine | IC50 | 22.0 [1] |
| (2S)-1-[4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-1-yl]-3-hydroxy-2-(methylamino)propan-1-one | IC50 | 51.0 [1] |
| [4-[[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenoxy]methyl]piperidin-1-yl]-[(2S,3R)-3-hydroxypyrrolidin-2-yl]methanone | IC50 | 19.0 [1] |
| (2S,4S)-4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]-2-methylpiperidin-4-ol | IC50 | 15.0 [1] |
| (2R)-3-[4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]-4-hydroxypiperidin-1-yl]propane-1,2-diol | IC50 | 24.0 [1] |
| Tert-butyl 4-[[1-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]triazol-4-yl]methyl]-4-hydroxypiperidine-1-carboxylate | IC50 | 77.0 [1] |
| 1-[[1-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]pyrazol-4-yl]methyl]azetidin-3-amine | IC50 | 21.0 [1] |
| (2S,3R)-N-[4-[[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenoxy]methyl]cyclohexyl]-3-hydroxypyrrolidine-2-carboxamide | IC50 | 54.0 [1] |
| 1-[(2S)-4-[(E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]-1-methylpiperazin-2-yl]-N,N-dimethylmethanamine | IC50 | 7.0 [1] |
| (2R)-1-[Tert-butyl(dimethyl)silyl]oxy-3-[4-[(E)-3-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-1-yl]propan-2-ol | IC50 | 30.0 [1] |
| (E)-3-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]-1-(4-methylpiperazin-1-yl)prop-2-en-1-one | IC50 | 81.0 [1] |