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Mitogen-activated protein kinase kinase kinase 12 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
Dlk-IN-1IC50129.0 [1], 195.0 [2]
Dlk-IN-1Ki1.9 [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-amineIC50144.0 [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-amineKi0.17 [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-amineIC50180.0 [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-amineKi1.6 [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]pyridineIC50485.0 [1]
5-[5-[1-(Oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-3-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridineKi2.3 [1]
3-Methyl-5-[5-[1-(oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-1H-pyrrolo[2,3-b]pyridineIC50303.0 [1]
3-Methyl-5-[5-[1-(oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-1H-pyrrolo[2,3-b]pyridineKi3.7 [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]pyridineIC502800.0 [1]
3-Fluoro-5-[5-[1-(oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-1H-pyrrolo[2,3-b]pyridineKi96.0 [1]
5-[5-[1-(Oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amineIC501900.0 [1]
5-[5-[1-(Oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amineKi150.0 [1], 154.0 [2]
3-Chloro-5-[5-[1-(oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]pyridin-2-amineIC501700.0 [1]
3-Chloro-5-[5-[1-(oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]pyridin-2-amineKi1000.0 [1]
3-Chloro-5-[5-[1-(oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-1H-pyrrolo[2,3-b]pyridineIC50574.0 [1]
3-Chloro-5-[5-[1-(oxetan-3-yl)piperidin-4-yl]-1-propan-2-ylpyrazol-3-yl]-1H-pyrrolo[2,3-b]pyridineKi15.0 [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-amineIC50611.0 [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-amineKi1.0 [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]ethanoneIC50302.0 [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]ethanoneKi5.6 [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-amineIC50265.0 [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-amineKi9.0 [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-amineIC50250.0 [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-amineKi2.7 [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-amineIC50873.0 [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-amineKi7.0 [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-amineIC501200.0 [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-amineKi35.0 [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-amineIC50210.0 [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-amineKi8.1 [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-amineIC50328.0 [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-amineKi8.0 [1]
CID 72547959IC5030.0 [1]
CID 72547959Ki0.5 [1]
2-[[1-Cyclopentyl-5-[1-(Oxetan-3-Yl)piperidin-4-Yl]pyrazol-3-Yl]amino]pyridine-4-CarbonitrileIC50536.0 [1]
2-[[1-Cyclopentyl-5-[1-(Oxetan-3-Yl)piperidin-4-Yl]pyrazol-3-Yl]amino]pyridine-4-CarbonitrileKi42.0 [1]
2-(3,3-Difluoropyrrolidin-1-yl)-6-piperidin-4-yl-N-[4-(trifluoromethyl)pyridin-2-yl]pyrimidin-4-amineIC50410.0 [1]
2-(3,3-Difluoropyrrolidin-1-yl)-6-piperidin-4-yl-N-[4-(trifluoromethyl)pyridin-2-yl]pyrimidin-4-amineKi2.0 [1]
[3-[2-Methyl-6-[[4-(trifluoromethyl)pyridin-2-yl]amino]pyrimidin-4-yl]piperidin-1-yl]-phenylmethanoneIC50229.0 [1]
[3-[2-Methyl-6-[[4-(trifluoromethyl)pyridin-2-yl]amino]pyrimidin-4-yl]piperidin-1-yl]-phenylmethanoneKi24.0 [1]
1-[4-[2-(3,3-Difluoropyrrolidin-1-yl)-6-[[4-(trifluoromethyl)pyridin-2-yl]amino]pyrimidin-4-yl]piperidin-1-yl]ethanoneIC50300.0 [1]
1-[4-[2-(3,3-Difluoropyrrolidin-1-yl)-6-[[4-(trifluoromethyl)pyridin-2-yl]amino]pyrimidin-4-yl]piperidin-1-yl]ethanoneKi33.0 [1]
2-(3,3-Difluoropyrrolidin-1-yl)-6-(oxan-4-yl)-N-[4-(trifluoromethyl)pyridin-2-yl]pyrimidin-4-amineIC50440.0 [1]
2-(3,3-Difluoropyrrolidin-1-yl)-6-(oxan-4-yl)-N-[4-(trifluoromethyl)pyridin-2-yl]pyrimidin-4-amineKi41.0 [1]
2-[[6-Ethyl-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrileIC50213.0 [1]
2-[[6-Ethyl-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrileKi18.0 [1]
2-[[6-(3,3-Difluoropyrrolidin-1-yl)-4-[1-(oxetan-3-yl)azetidin-3-yl]pyridin-2-yl]amino]pyridine-4-carbonitrileIC5057.0 [1]
2-[[6-(3,3-Difluoropyrrolidin-1-yl)-4-[1-(oxetan-3-yl)azetidin-3-yl]pyridin-2-yl]amino]pyridine-4-carbonitrileKi0.7 [1]
2-[[6-Cyclopropyl-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrileIC5062.0 [1]
2-[[6-Cyclopropyl-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrileKi1.0 [1]
[3-[2-Methyl-6-[(5-methyl-1,3-thiazol-2-yl)amino]pyrimidin-4-yl]piperidin-1-yl]-phenylmethanoneIC50641.0 [1]
[3-[2-Methyl-6-[(5-methyl-1,3-thiazol-2-yl)amino]pyrimidin-4-yl]piperidin-1-yl]-phenylmethanoneKi35.0 [1]
[3-[2-Methyl-6-[(4-propan-2-ylpyridin-2-yl)amino]pyrimidin-4-yl]piperidin-1-yl]-phenylmethanoneIC501300.0 [1]
[3-[2-Methyl-6-[(4-propan-2-ylpyridin-2-yl)amino]pyrimidin-4-yl]piperidin-1-yl]-phenylmethanoneKi4.0 [1]
[3-[6-[(4-Cyclopropylpyridin-2-yl)amino]-2-methylpyrimidin-4-yl]piperidin-1-yl]-phenylmethanoneIC50486.0 [1]
[3-[6-[(4-Cyclopropylpyridin-2-yl)amino]-2-methylpyrimidin-4-yl]piperidin-1-yl]-phenylmethanoneKi18.0 [1]
2-[[6-(1-Benzoylpiperidin-3-yl)-2-methylpyrimidin-4-yl]amino]pyridine-4-carbonitrileIC501000.0 [1]
2-[[6-(1-Benzoylpiperidin-3-yl)-2-methylpyrimidin-4-yl]amino]pyridine-4-carbonitrileKi90.0 [1]
[3-[6-[(4-Methoxypyridin-2-yl)amino]-2-methylpyrimidin-4-yl]piperidin-1-yl]-phenylmethanoneIC501000.0 [1]
[3-[6-[(4-Methoxypyridin-2-yl)amino]-2-methylpyrimidin-4-yl]piperidin-1-yl]-phenylmethanoneKi57.0 [1]
2-[[4-(2-Cyanopropan-2-yl)-6-(3,3-difluoropyrrolidin-1-yl)pyridin-2-yl]amino]pyridine-4-carbonitrileIC50193.0 [1]
2-[[4-(2-Cyanopropan-2-yl)-6-(3,3-difluoropyrrolidin-1-yl)pyridin-2-yl]amino]pyridine-4-carbonitrileKi14.0 [1]
2-[[6-(3,3-Difluoropyrrolidin-1-yl)-4-(2-hydroxypropan-2-yl)pyridin-2-yl]amino]pyridine-4-carbonitrileIC50125.0 [1]
2-[[6-(3,3-Difluoropyrrolidin-1-yl)-4-(2-hydroxypropan-2-yl)pyridin-2-yl]amino]pyridine-4-carbonitrileKi5.0 [1]
2-[[6-Cyclobutyloxy-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrileIC5064.0 [1]
2-[[6-Cyclobutyloxy-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrileKi0.2 [1]
2-[[1-(3,3-Difluorocyclopentyl)-5-[1-(oxetan-3-yl)piperidin-4-yl]pyrazol-3-yl]amino]pyridine-4-carbonitrileIC50721.0 [1]
2-[[1-(3,3-Difluorocyclopentyl)-5-[1-(oxetan-3-yl)piperidin-4-yl]pyrazol-3-yl]amino]pyridine-4-carbonitrileKi48.0 [1]
2-[[1-(Cyclobutylmethyl)-5-[1-(oxetan-3-yl)piperidin-4-yl]pyrazol-3-yl]amino]pyridine-4-carbonitrileIC501400.0 [1]
2-[[1-(Cyclobutylmethyl)-5-[1-(oxetan-3-yl)piperidin-4-yl]pyrazol-3-yl]amino]pyridine-4-carbonitrileKi133.0 [1]
2-[[1-Cyclopentyl-5-[1-(oxetan-3-yl)azetidin-3-yl]pyrazol-3-yl]amino]pyridine-4-carbonitrileIC50459.0 [1]
2-[[1-Cyclopentyl-5-[1-(oxetan-3-yl)azetidin-3-yl]pyrazol-3-yl]amino]pyridine-4-carbonitrileKi48.0 [1]
2-[[1-Cyclopentyl-5-[1-(oxetan-3-yl)pyrrolidin-3-yl]pyrazol-3-yl]amino]pyridine-4-carbonitrileIC50632.0 [1]
2-[[1-Cyclopentyl-5-[1-(oxetan-3-yl)pyrrolidin-3-yl]pyrazol-3-yl]amino]pyridine-4-carbonitrileKi25.0 [1]
2-[[1-Cyclopentyl-5-(oxolan-3-yl)pyrazol-3-yl]amino]pyridine-4-carbonitrileIC50698.0 [1]
2-[[1-Cyclopentyl-5-(oxolan-3-yl)pyrazol-3-yl]amino]pyridine-4-carbonitrileKi54.0 [1]
2-[[4-Cyclopropyl-5-[1-(oxetan-3-yl)piperidin-4-yl]-1,3-thiazol-2-yl]amino]pyridine-4-carbonitrileIC508600.0 [1]
2-[[4-Cyclopropyl-5-[1-(oxetan-3-yl)piperidin-4-yl]-1,3-thiazol-2-yl]amino]pyridine-4-carbonitrileKi569.0 [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-amineIC50304.0 [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-amineKi3.0 [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-amineIC50202.0 [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-amineKi9.0 [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-amineIC501300.0 [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-amineKi67.0 [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-amineIC50406.0 [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-amineKi3.0 [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-amineIC50274.0 [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-amineKi5.0 [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-olIC50208.0 [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-olKi4.0 [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-amineIC5099.0 [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-amineKi3.0 [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-amineIC501800.0 [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-amineKi82.0 [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-olIC50829.0 [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-olKi23.0 [1]
2-[[6-(Azetidin-1-yl)-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrileIC50141.0 [1]
2-[[6-(Azetidin-1-yl)-4-[1-(oxetan-3-yl)piperidin-4-yl]pyridin-2-yl]amino]pyridine-4-carbonitrileKi8.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Mitogen-activated protein kinase kinase kinase 12 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.10 May2024https://www.aatbio.com/data-sets/mitogen-activated-protein-kinase-kinase-kinase-12-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 10). Quest Database™ Mitogen-activated protein kinase kinase kinase 12 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/mitogen-activated-protein-kinase-kinase-kinase-12-inhibitors-ic50-ki.
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