 | Dlk-IN-1 | IC50 | 129.0 [1], 195.0 [2] |
 | Dlk-IN-1 | Ki | 1.9 [1], 3.0 [2] |
 | 5-[1-(Cyclopropylmethyl)-5-[(1R,5S)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | IC50 | 144.0 [1] |
 | 5-[1-(Cyclopropylmethyl)-5-[(1R,5S)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | Ki | 0.17 [1], 4.0 [2] |
 | 5-[5-[(1S,5R)-3-(Oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]-1-(2,2,2-trifluoroethyl)pyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | IC50 | 180.0 [1] |
 | 5-[5-[(1S,5R)-3-(Oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]-1-(2,2,2-trifluoroethyl)pyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | Ki | 1.6 [1], 16.0 [2] |
 | 5-[5-[1-(Oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-3-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridine | IC50 | 485.0 [1] |
 | 5-[5-[1-(Oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-3-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridine | Ki | 2.3 [1] |
 | 3-Methyl-5-[5-[1-(oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-1H-pyrrolo[2,3-b]pyridine | IC50 | 303.0 [1] |
 | 3-Methyl-5-[5-[1-(oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-1H-pyrrolo[2,3-b]pyridine | Ki | 3.7 [1], 4.0 [2] |
 | 3-Fluoro-5-[5-[1-(oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-1H-pyrrolo[2,3-b]pyridine | IC50 | 2800.0 [1] |
 | 3-Fluoro-5-[5-[1-(oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-1H-pyrrolo[2,3-b]pyridine | Ki | 96.0 [1] |
 | 5-[5-[1-(Oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | IC50 | 1900.0 [1] |
 | 5-[5-[1-(Oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | Ki | 150.0 [1], 154.0 [2] |
 | 3-Chloro-5-[5-[1-(oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]pyridin-2-amine | IC50 | 1700.0 [1] |
 | 3-Chloro-5-[5-[1-(oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]pyridin-2-amine | Ki | 1000.0 [1] |
 | 3-Chloro-5-[5-[1-(oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-1H-pyrrolo[2,3-b]pyridine | IC50 | 574.0 [1] |
 | 3-Chloro-5-[5-[1-(oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-1H-pyrrolo[2,3-b]pyridine | Ki | 15.0 [1] |
 | 5-[5-[(1S,5R)-3-(2,2-Difluoroethyl)-3-azabicyclo[3.1.0]hexan-6-yl]-1-propan-2-ylpyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | IC50 | 611.0 [1] |
 | 5-[5-[(1S,5R)-3-(2,2-Difluoroethyl)-3-azabicyclo[3.1.0]hexan-6-yl]-1-propan-2-ylpyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | Ki | 1.0 [1] |
 | 1-[(1R,5S)-6-[5-[6-Amino-5-(trifluoromethyl)pyridin-3-yl]-2-propan-2-ylpyrazol-3-yl]-3-azabicyclo[3.1.0]hexan-3-yl]ethanone | IC50 | 302.0 [1] |
 | 1-[(1R,5S)-6-[5-[6-Amino-5-(trifluoromethyl)pyridin-3-yl]-2-propan-2-ylpyrazol-3-yl]-3-azabicyclo[3.1.0]hexan-3-yl]ethanone | Ki | 5.6 [1], 6.0 [2] |
 | 5-[5-[(1S,5R)-3-(2-Methoxyethyl)-3-azabicyclo[3.1.0]hexan-6-yl]-1-propan-2-ylpyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | IC50 | 265.0 [1] |
 | 5-[5-[(1S,5R)-3-(2-Methoxyethyl)-3-azabicyclo[3.1.0]hexan-6-yl]-1-propan-2-ylpyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | Ki | 9.0 [1], 9.4 [2] |
 | 5-[5-[(1S,5R)-3-(Oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]-1-propan-2-ylpyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | IC50 | 250.0 [1] |
 | 5-[5-[(1S,5R)-3-(Oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]-1-propan-2-ylpyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | Ki | 2.7 [1], 7.0 [2] |
 | 3-Methoxy-5-[5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]-1-propan-2-ylpyrazol-3-yl]pyridin-2-amine | IC50 | 873.0 [1] |
 | 3-Methoxy-5-[5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]-1-propan-2-ylpyrazol-3-yl]pyridin-2-amine | Ki | 7.0 [1], 7.4 [2] |
 | 3-(Difluoromethyl)-5-[5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]-1-propan-2-ylpyrazol-3-yl]pyridin-2-amine | IC50 | 1200.0 [1] |
 | 3-(Difluoromethyl)-5-[5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]-1-propan-2-ylpyrazol-3-yl]pyridin-2-amine | Ki | 35.0 [1] |
 | 5-[1-(Cyclobutylmethyl)-5-[(1R,5S)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | IC50 | 210.0 [1] |
 | 5-[1-(Cyclobutylmethyl)-5-[(1R,5S)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | Ki | 8.1 [1], 11.0 [2] |
 | 3-(Difluoromethoxy)-5-[5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]-1-propan-2-ylpyrazol-3-yl]pyridin-2-amine | IC50 | 328.0 [1] |
 | 3-(Difluoromethoxy)-5-[5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]-1-propan-2-ylpyrazol-3-yl]pyridin-2-amine | Ki | 8.0 [1] |
 | CID 72547959 | IC50 | 30.0 [1] |
 | CID 72547959 | Ki | 0.5 [1] |
 | 2-[[1-Cyclopentyl-5-[1-(Oxetan-3-Yl)piperidin-4-Yl]pyrazol-3-Yl]amino]pyridine-4-Carbonitrile | IC50 | 536.0 [1] |
 | 2-[[1-Cyclopentyl-5-[1-(Oxetan-3-Yl)piperidin-4-Yl]pyrazol-3-Yl]amino]pyridine-4-Carbonitrile | Ki | 42.0 [1] |
 | 2-(3,3-Difluoropyrrolidin-1-yl)-6-piperidin-4-yl-N-[4-(trifluoromethyl)pyridin-2-yl]pyrimidin-4-amine | IC50 | 410.0 [1] |
 | 2-(3,3-Difluoropyrrolidin-1-yl)-6-piperidin-4-yl-N-[4-(trifluoromethyl)pyridin-2-yl]pyrimidin-4-amine | Ki | 2.0 [1] |
 | [3-[2-Methyl-6-[[4-(trifluoromethyl)pyridin-2-yl]amino]pyrimidin-4-yl]piperidin-1-yl]-phenylmethanone | IC50 | 229.0 [1] |
 | [3-[2-Methyl-6-[[4-(trifluoromethyl)pyridin-2-yl]amino]pyrimidin-4-yl]piperidin-1-yl]-phenylmethanone | Ki | 24.0 [1] |
 | 1-[4-[2-(3,3-Difluoropyrrolidin-1-yl)-6-[[4-(trifluoromethyl)pyridin-2-yl]amino]pyrimidin-4-yl]piperidin-1-yl]ethanone | IC50 | 300.0 [1] |
 | 1-[4-[2-(3,3-Difluoropyrrolidin-1-yl)-6-[[4-(trifluoromethyl)pyridin-2-yl]amino]pyrimidin-4-yl]piperidin-1-yl]ethanone | Ki | 33.0 [1] |
 | 2-(3,3-Difluoropyrrolidin-1-yl)-6-(oxan-4-yl)-N-[4-(trifluoromethyl)pyridin-2-yl]pyrimidin-4-amine | IC50 | 440.0 [1] |
 | 2-(3,3-Difluoropyrrolidin-1-yl)-6-(oxan-4-yl)-N-[4-(trifluoromethyl)pyridin-2-yl]pyrimidin-4-amine | Ki | 41.0 [1] |
 | 2-[[6-Ethyl-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrile | IC50 | 213.0 [1] |
 | 2-[[6-Ethyl-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrile | Ki | 18.0 [1] |
 | 2-[[6-(3,3-Difluoropyrrolidin-1-yl)-4-[1-(oxetan-3-yl)azetidin-3-yl]pyridin-2-yl]amino]pyridine-4-carbonitrile | IC50 | 57.0 [1] |
 | 2-[[6-(3,3-Difluoropyrrolidin-1-yl)-4-[1-(oxetan-3-yl)azetidin-3-yl]pyridin-2-yl]amino]pyridine-4-carbonitrile | Ki | 0.7 [1] |
 | 2-[[6-Cyclopropyl-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrile | IC50 | 62.0 [1] |
 | 2-[[6-Cyclopropyl-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrile | Ki | 1.0 [1] |
 | [3-[2-Methyl-6-[(5-methyl-1,3-thiazol-2-yl)amino]pyrimidin-4-yl]piperidin-1-yl]-phenylmethanone | IC50 | 641.0 [1] |
 | [3-[2-Methyl-6-[(5-methyl-1,3-thiazol-2-yl)amino]pyrimidin-4-yl]piperidin-1-yl]-phenylmethanone | Ki | 35.0 [1] |
 | [3-[2-Methyl-6-[(4-propan-2-ylpyridin-2-yl)amino]pyrimidin-4-yl]piperidin-1-yl]-phenylmethanone | IC50 | 1300.0 [1] |
 | [3-[2-Methyl-6-[(4-propan-2-ylpyridin-2-yl)amino]pyrimidin-4-yl]piperidin-1-yl]-phenylmethanone | Ki | 4.0 [1] |
 | [3-[6-[(4-Cyclopropylpyridin-2-yl)amino]-2-methylpyrimidin-4-yl]piperidin-1-yl]-phenylmethanone | IC50 | 486.0 [1] |
 | [3-[6-[(4-Cyclopropylpyridin-2-yl)amino]-2-methylpyrimidin-4-yl]piperidin-1-yl]-phenylmethanone | Ki | 18.0 [1] |
 | 2-[[6-(1-Benzoylpiperidin-3-yl)-2-methylpyrimidin-4-yl]amino]pyridine-4-carbonitrile | IC50 | 1000.0 [1] |
 | 2-[[6-(1-Benzoylpiperidin-3-yl)-2-methylpyrimidin-4-yl]amino]pyridine-4-carbonitrile | Ki | 90.0 [1] |
 | [3-[6-[(4-Methoxypyridin-2-yl)amino]-2-methylpyrimidin-4-yl]piperidin-1-yl]-phenylmethanone | IC50 | 1000.0 [1] |
 | [3-[6-[(4-Methoxypyridin-2-yl)amino]-2-methylpyrimidin-4-yl]piperidin-1-yl]-phenylmethanone | Ki | 57.0 [1] |
 | 2-[[4-(2-Cyanopropan-2-yl)-6-(3,3-difluoropyrrolidin-1-yl)pyridin-2-yl]amino]pyridine-4-carbonitrile | IC50 | 193.0 [1] |
 | 2-[[4-(2-Cyanopropan-2-yl)-6-(3,3-difluoropyrrolidin-1-yl)pyridin-2-yl]amino]pyridine-4-carbonitrile | Ki | 14.0 [1] |
 | 2-[[6-(3,3-Difluoropyrrolidin-1-yl)-4-(2-hydroxypropan-2-yl)pyridin-2-yl]amino]pyridine-4-carbonitrile | IC50 | 125.0 [1] |
 | 2-[[6-(3,3-Difluoropyrrolidin-1-yl)-4-(2-hydroxypropan-2-yl)pyridin-2-yl]amino]pyridine-4-carbonitrile | Ki | 5.0 [1] |
 | 2-[[6-Cyclobutyloxy-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrile | IC50 | 64.0 [1] |
 | 2-[[6-Cyclobutyloxy-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrile | Ki | 0.2 [1] |
 | 2-[[1-(3,3-Difluorocyclopentyl)-5-[1-(oxetan-3-yl)piperidin-4-yl]pyrazol-3-yl]amino]pyridine-4-carbonitrile | IC50 | 721.0 [1] |
 | 2-[[1-(3,3-Difluorocyclopentyl)-5-[1-(oxetan-3-yl)piperidin-4-yl]pyrazol-3-yl]amino]pyridine-4-carbonitrile | Ki | 48.0 [1] |
 | 2-[[1-(Cyclobutylmethyl)-5-[1-(oxetan-3-yl)piperidin-4-yl]pyrazol-3-yl]amino]pyridine-4-carbonitrile | IC50 | 1400.0 [1] |
 | 2-[[1-(Cyclobutylmethyl)-5-[1-(oxetan-3-yl)piperidin-4-yl]pyrazol-3-yl]amino]pyridine-4-carbonitrile | Ki | 133.0 [1] |
 | 2-[[1-Cyclopentyl-5-[1-(oxetan-3-yl)azetidin-3-yl]pyrazol-3-yl]amino]pyridine-4-carbonitrile | IC50 | 459.0 [1] |
 | 2-[[1-Cyclopentyl-5-[1-(oxetan-3-yl)azetidin-3-yl]pyrazol-3-yl]amino]pyridine-4-carbonitrile | Ki | 48.0 [1] |
 | 2-[[1-Cyclopentyl-5-[1-(oxetan-3-yl)pyrrolidin-3-yl]pyrazol-3-yl]amino]pyridine-4-carbonitrile | IC50 | 632.0 [1] |
 | 2-[[1-Cyclopentyl-5-[1-(oxetan-3-yl)pyrrolidin-3-yl]pyrazol-3-yl]amino]pyridine-4-carbonitrile | Ki | 25.0 [1] |
 | 2-[[1-Cyclopentyl-5-(oxolan-3-yl)pyrazol-3-yl]amino]pyridine-4-carbonitrile | IC50 | 698.0 [1] |
 | 2-[[1-Cyclopentyl-5-(oxolan-3-yl)pyrazol-3-yl]amino]pyridine-4-carbonitrile | Ki | 54.0 [1] |
 | 2-[[4-Cyclopropyl-5-[1-(oxetan-3-yl)piperidin-4-yl]-1,3-thiazol-2-yl]amino]pyridine-4-carbonitrile | IC50 | 8600.0 [1] |
 | 2-[[4-Cyclopropyl-5-[1-(oxetan-3-yl)piperidin-4-yl]-1,3-thiazol-2-yl]amino]pyridine-4-carbonitrile | Ki | 569.0 [1] |
 | 5-[1-(Cyclopropylmethyl)-5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethoxy)pyridin-2-amine | IC50 | 304.0 [1] |
 | 5-[1-(Cyclopropylmethyl)-5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethoxy)pyridin-2-amine | Ki | 3.0 [1] |
 | 5-[1-(Cyclopentylmethyl)-5-[(1R,5S)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | IC50 | 202.0 [1] |
 | 5-[1-(Cyclopentylmethyl)-5-[(1R,5S)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | Ki | 9.0 [1] |
 | 5-[1-Methyl-5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethoxy)pyridin-2-amine | IC50 | 1300.0 [1] |
 | 5-[1-Methyl-5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethoxy)pyridin-2-amine | Ki | 67.0 [1] |
 | 5-[1-Ethyl-5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | IC50 | 406.0 [1] |
 | 5-[1-Ethyl-5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | Ki | 3.0 [1] |
 | 5-[5-[(1S,5R)-3-(Oxetan-3-ylmethyl)-3-azabicyclo[3.1.0]hexan-6-yl]-1-propan-2-ylpyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | IC50 | 274.0 [1] |
 | 5-[5-[(1S,5R)-3-(Oxetan-3-ylmethyl)-3-azabicyclo[3.1.0]hexan-6-yl]-1-propan-2-ylpyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | Ki | 5.0 [1] |
 | 1-[(1R,5S)-6-[5-[6-Amino-5-(trifluoromethyl)pyridin-3-yl]-2-propan-2-ylpyrazol-3-yl]-3-azabicyclo[3.1.0]hexan-3-yl]propan-2-ol | IC50 | 208.0 [1] |
 | 1-[(1R,5S)-6-[5-[6-Amino-5-(trifluoromethyl)pyridin-3-yl]-2-propan-2-ylpyrazol-3-yl]-3-azabicyclo[3.1.0]hexan-3-yl]propan-2-ol | Ki | 4.0 [1] |
 | 5-[1-(2-Methylpropyl)-5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | IC50 | 99.0 [1] |
 | 5-[1-(2-Methylpropyl)-5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | Ki | 3.0 [1] |
 | 5-[1-Methyl-5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | IC50 | 1800.0 [1] |
 | 5-[1-Methyl-5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | Ki | 82.0 [1] |
 | 1-[3-[6-Amino-5-(trifluoromethyl)pyridin-3-yl]-5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-1-yl]-2-methylpropan-2-ol | IC50 | 829.0 [1] |
 | 1-[3-[6-Amino-5-(trifluoromethyl)pyridin-3-yl]-5-[(1S,5R)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-1-yl]-2-methylpropan-2-ol | Ki | 23.0 [1] |
 | 2-[[6-(Azetidin-1-yl)-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrile | IC50 | 141.0 [1] |
 | 2-[[6-(Azetidin-1-yl)-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrile | Ki | 8.0 [1] |