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Tyrosine-protein kinase JAK1 Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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TofacitinibIC503.2 [1]
TofacitinibKi0.68 [1], 0.7 [2]
RuxolitinibIC503.3 [1]
RuxolitinibKi0.09 [1], 0.2 [2]
FilgotinibIC5010.0 [1]
BaricitinibIC500.99 [1], 4.0 [2], 6.0 [3]
StaurosporineIC501.0 [1], 1.01 [2], 3.0 [3], 12.5 [4]
DecernotinibIC5011.0 [1], 13.2 [2], 50.0 [3], 112.0 [4]
1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-oneIC501640.0 [1], 10000.0 [2]
3-(4-Cyanoanilino)-1-[(3R,4S)-4-cyanooxan-3-yl]pyrazole-4-carboxamideIC500.07 [1], 0.15 [2], 13.0 [3], 220.0 [4]
Pyridone 6IC504.0 [1], 15.0 [2], 600.0 [3]
N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamideIC5029.0 [1], 572.0 [2]
3-[5-[4-(2-Hydroxy-2-methylpropanoyl)piperazin-1-yl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)pyrrole-2,5-dioneIC50311.0 [1], 344.0 [2], 1017.0 [3]
3-Cyclohexyl-4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaeneIC5020.0 [1]
3-Cyclohexyl-4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaeneKi1.3 [1]
3-(4-Chloro-3-methoxyanilino)-1-[(3R,4S)-4-cyanooxan-3-yl]pyrazole-4-carboxamideIC500.1 [1], 13.0 [2], 1760.0 [3]
4-[(4-Aminocyclohexyl)amino]-3-(1h-Benzimidazol-2-Yl)-1h-Pyridin-2-OneIC500.1 [1], 0.6 [2], 3.0 [3]
N-[5-[4-(Morpholin-4-ylmethyl)phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamideIC5052.11 [1], 92.0 [2], 5590.0 [3]
N-[5-[4-[(4,4-Difluoropiperidin-1-yl)methyl]phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamideIC507.69 [1], 27.0 [2], 2749.0 [3]
1-Cyclopropyl-N-[3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl]methanesulfonamideIC5042.0 [1], 1030.0 [2]
1-[(3R,4S)-4-Cyanooxan-3-yl]-3-[(2-fluoropyridin-4-yl)amino]pyrazole-4-carboxamideIC500.2 [1], 0.24 [2], 42.0 [3]
1-[(3R,4S)-4-Cyanooxan-3-yl]-3-[4-[(1S)-2,2,2-trifluoro-1-hydroxyethyl]anilino]pyrazole-4-carboxamideIC500.05 [1], 0.09 [2], 14.0 [3]
3-(4-Chloroanilino)-1-[(3R,4S)-4-cyanooxan-3-yl]pyrazole-4-carboxamideIC500.13 [1], 0.2 [2], 14.0 [3]
3-Anilino-1-[(3R,4S)-4-cyanooxan-3-yl]pyrazole-4-carboxamideIC500.4 [1], 10.0 [2], 33.0 [3]
3-(4-Chloroanilino)-1-[(1S,2S,4S)-2-cyano-4-(dimethylamino)cyclohexyl]pyrazole-4-carboxamideIC500.55 [1], 1.5 [2], 64.0 [3]
4-[[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]amino]benzonitrileIC502.2 [1], 3.9 [2], 22.0 [3]
4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)-N-(2-phenylethyl)cyclohexan-1-amineIC506.1 [1], 6.3 [2], 97.0 [3]
4-Fluoro-N-[4-(4,5,6,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]anilineIC505.4 [1], 6.6 [2], 69.0 [3]
Nvp-aew541IC5010000.0 [1]
MomelotinibIC5011.0 [1]
OclacitinibIC509.53 [1]
2,6-Dichloro-N-{2-[(Cyclopropylcarbonyl)amino]pyridin-4-Yl}benzamideKi83.8 [1], 84.0 [2]
[2-[6-(2-Ethyl-5-fluoro-4-hydroxyphenyl)-1H-indazol-3-yl]-3,4,6,7-tetrahydroimidazo[4,5-c]pyridin-5-yl]-(5-piperidin-1-ylpyrazin-2-yl)methanoneIC502.2 [1], 5.4 [2]
[(1S)-6-(5-Phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC50422.0 [1], 3345.0 [2]
1-(Piperidin-4-Yl)-1,6-Dihydroimidazo[4,5-D]pyrrolo[2,3-B]pyridineKi45.0 [1], 46.0 [2]
cis-3-[4-Amino-7-(3-azetidin-1-ylmethyl-cyclobutyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-phenolIC50260.0 [1]
7-[3-(Azetidin-1-ylmethyl)cyclobutyl]-5-[3-[[(2S)-oxolan-2-yl]methoxy]phenyl]pyrrolo[2,3-d]pyrimidin-4-amineIC5010000.0 [1]
CID 11993785IC5047.0 [1]
1-(2-Aminoethyl)-2-(4-piperidinyl)-1H-benzoimidazole-5-carboxamideIC5050.0 [1], 5700.0 [2]
Unii-7N5LJ2Z26CIC502.0 [1], 3.0 [2]
3-[(3r)-3-(Imidazo[4,5-D]pyrrolo[2,3-B]pyridin-1(6h)-Yl)piperidin-1-Yl]-3-OxopropanenitrileKi0.4 [1]
N-[(2R)-1-(3-Cyanoazetidin-1-yl)-1-oxopropan-2-yl]-2-cyclopropyl-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC5047.0 [1]
Jak-IN-1IC503.2 [1]
2-Methyl-1-(Piperidin-4-Yl)-1,6-Dihydroimidazo[4,5-D]pyrrolo[2,3-B]pyridineKi10.0 [1]
3-[4-(3,5,8,10-Tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrileKi0.6 [1]
1-[(3Ar,7aR)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-3,3a,4,5,7,7a-hexahydro-2H-pyrrolo[2,3-c]pyridin-6-yl]prop-2-en-1-oneIC50984.0 [1], 10000.0 [2]
1-[(3R,4R)-4-Methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]prop-2-en-1-oneIC50274.0 [1], 988.0 [2]
(E)-1-[(3R)-3-(7H-Pyrrolo[2,3-d]pyrimidin-4-ylamino)piperidin-1-yl]but-2-en-1-oneIC502290.0 [1], 10000.0 [2]
1-[(3R)-3-(7H-Pyrrolo[2,3-d]pyrimidin-4-ylamino)piperidin-1-yl]prop-2-en-1-oneIC501400.0 [1], 10000.0 [2]
1-[(3R)-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]prop-2-en-1-oneIC501150.0 [1], 7820.0 [2]
N-[5-[4-[[(2,2,2-Trifluoroacetyl)amino]methyl]phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamideIC5016.0 [1], 4467.0 [2]
(2R)-N-[3-[2-[(1,3-Dimethylpyrazol-4-yl)amino]-5-fluoropyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)butanamideIC504.0 [1], 75.1 [2]
(2S)-2-[(2S)-2,4-Dimethylpiperazin-1-yl]-N-[3-[2-[(3-ethoxy-1-methylpyrazol-4-yl)amino]-5-fluoropyrimidin-4-yl]-1H-indol-7-yl]propanamideIC503000.0 [1], 7600.0 [2]
(2R)-N-[3-[2-[(3-Ethoxy-1-methylpyrazol-4-yl)amino]-5-methylpyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)butanamideIC506.0 [1], 104.0 [2]
(2R)-2-[(2S)-2,4-Dimethylpiperazin-1-yl]-N-[3-[2-[(3-methoxy-1-methylpyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]propanamideIC50643.0 [1], 847.0 [2]
(2R)-N-[3-[5-Chloro-2-[(3-methoxy-1-methylpyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propanamideIC507.0 [1], 57.9 [2]
(2R)-N-[3-[2-[(1,3-Dimethylpyrazol-4-yl)amino]-5-fluoropyrimidin-4-yl]-1H-indol-7-yl]-3-methoxy-2-(4-methylpiperazin-1-yl)propanamideIC503.0 [1], 56.6 [2]
6-Chloro-2-(2,5-difluoro-4-methoxyphenyl)-N-(piperidin-4-ylmethyl)-1H-imidazo[4,5-b]pyridin-7-amineIC5071.0 [1], 173.0 [2]
6-Chloro-2-(3,4-dimethoxyphenyl)-N-(piperidin-4-ylmethyl)-1H-imidazo[4,5-b]pyridin-7-amineIC504.9 [1], 87.0 [2]
6-Chloro-2-(2-fluoro-4-methoxyphenyl)-N-(piperidin-4-ylmethyl)-1H-imidazo[4,5-b]pyridin-7-amineIC5034.0 [1], 106.0 [2]
6-Chloro-2-(4-methoxy-2-methylphenyl)-N-(piperidin-4-ylmethyl)-1H-imidazo[4,5-b]pyridin-7-amineIC509.0 [1], 37.0 [2]
6-Chloro-2-(2-fluoro-5-methoxyphenyl)-N-(piperidin-4-ylmethyl)-1H-imidazo[4,5-b]pyridin-7-amineIC5049.0 [1], 76.0 [2]
6-Chloro-2-(4-methoxyphenyl)-N-(piperidin-4-ylmethyl)-1H-imidazo[4,5-b]pyridin-7-amineIC5017.0 [1], 29.0 [2]
N-[3-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]prop-2-enamideIC50966.0 [1], 8710.0 [2]
3-(4-Cyano-3-methoxyanilino)-1-[(3R,4S)-4-cyanooxan-3-yl]pyrazole-4-carboxamideIC500.07 [1], 19.0 [2]
1-[(3R,4S)-4-Cyanooxan-3-yl]-3-[(2-fluoro-6-methoxypyridin-4-yl)amino]pyrazole-4-carboxamideIC500.4 [1], 39.0 [2]
[2-[6-(2-Ethyl-5-fluoro-4-hydroxyphenyl)-1H-indazol-3-yl]-3,4,6,7-tetrahydroimidazo[4,5-c]pyridin-5-yl]-(4-fluorophenyl)methanoneIC500.1 [1], 0.7 [2]
Methyl 2-[4-[(4-aminocyclohexyl)amino]-2-oxo-1H-pyridin-3-yl]-4,5,6,7-tetrahydro-3H-benzimidazole-5-carboxylateIC500.8 [1], 44.0 [2]
[(1S)-1-Methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydroinden-1-yl]cyanamideIC505.0 [1], 57.0 [2]
1-[(3R,4S)-4-Cyanooxan-3-yl]-3-[[(3S)-3-methyl-1,1-dioxo-2,3-dihydro-1,2-benzothiazol-5-yl]amino]pyrazole-4-carboxamideIC500.04 [1], 16.0 [2]
1-[(3R,4S)-4-Cyanooxan-3-yl]-3-(3,4-dicyanoanilino)pyrazole-4-carboxamideIC500.9 [1], 77.0 [2]
3-(3-Chloro-4-cyanoanilino)-1-[(3R,4S)-4-cyanooxan-3-yl]pyrazole-4-carboxamideIC500.4 [1], 26.0 [2]
1-[(3R,4S)-4-Cyanooxan-3-yl]-3-[(8-fluoro-4-methoxyquinolin-6-yl)amino]pyrazole-4-carboxamideIC500.19 [1], 24.0 [2]
3-[(4-Chloro-8-fluoroquinolin-6-yl)amino]-1-[(3R,4S)-4-cyanooxan-3-yl]pyrazole-4-carboxamideIC500.24 [1], 14.0 [2]
1-[(3Ar,7aR)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-3,3a,4,5,7,7a-hexahydro-2H-pyrrolo[2,3-c]pyridin-6-yl]ethanoneIC50863.0 [1], 10000.0 [2]
1-[(3R,4S)-4-Cyanooxan-3-yl]-3-[4-(1-methylpyrazol-4-yl)anilino]pyrazole-4-carboxamideIC500.02 [1], 6.0 [2]
1-[(3R,4S)-4-Cyanooxan-3-yl]-3-(4-cyclopropylanilino)pyrazole-4-carboxamideIC500.5 [1], 37.0 [2]
1-[(3R,4S)-4-Cyanooxan-3-yl]-3-[(4-methylquinazolin-6-yl)amino]pyrazole-4-carboxamideIC500.16 [1], 24.0 [2]
1-[(3R,4S)-4-Cyanooxan-3-yl]-3-[[2-(dimethylamino)-6-fluoropyridin-4-yl]amino]pyrazole-4-carboxamideIC500.18 [1], 28.0 [2]
1-[(3R,4S)-4-Cyanooxan-3-yl]-3-[4-(triazol-1-yl)anilino]pyrazole-4-carboxamideIC500.06 [1], 23.0 [2]
1-[(3R,4S)-4-Cyanooxan-3-yl]-3-(4-fluoroanilino)pyrazole-4-carboxamideIC500.3 [1], 31.0 [2]
3-(4-Cyano-3-cyclopropylanilino)-1-[(3R,4S)-4-cyanooxan-3-yl]pyrazole-4-carboxamideIC501.4 [1], 72.0 [2]
1-[(3R,4S)-4-Cyanooxan-3-yl]-3-[4-(difluoromethoxy)anilino]pyrazole-4-carboxamideIC500.1 [1], 5.0 [2]
2-Cyano-3-[5-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)furan-2-yl]-N,N-dimethylprop-2-enamideIC5052.0 [1], 668.0 [2]
1-[6-[5-(2-Methoxyethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-2,3-dihydro-1,4-benzoxazin-4-yl]prop-2-en-1-oneIC5010000.0 [1]
[(1R,2R)-2-Methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC5094.0 [1], 973.0 [2]
[(1S)-6-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC5082.0 [1], 644.0 [2]
Methyl-[6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC50814.0 [1], 7624.0 [2]
[(1R,2S)-2-Methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC50100.0 [1], 705.0 [2]
[(1R,2R)-2-Hydroxy-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC50105.0 [1], 1266.0 [2]
[(4R)-6-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-3,4-dihydro-2H-chromen-4-yl]cyanamideIC5081.0 [1], 665.0 [2]
[(1R)-6-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC5096.0 [1], 844.0 [2]
N-[(1R,3S)-3-(Cyanoamino)-5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]methanesulfonamideIC5097.0 [1], 1918.0 [2]
[1-Methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydroinden-1-yl]cyanamideIC508.0 [1], 94.0 [2]
[(1S)-6-[5-[3-(Hydroxymethyl)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-2,3-dihydro-1H-inden-1-yl]cyanamideIC50733.0 [1], 9604.0 [2]
N-[(1R,3S)-3-(Cyanoamino)-5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-2-methoxyethanesulfonamideIC50775.0 [1], 8652.0 [2]
[6-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC50113.0 [1], 909.0 [2]
6-[5-(2-Methoxyethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-2,3-dihydro-1,4-benzoxazine-4-carbonitrileIC50991.0 [1], 6501.0 [2]
[6-[5-(2-Methoxyethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-3,4-dihydro-2H-chromen-4-yl]cyanamideIC50369.0 [1], 3776.0 [2]
N-[3-[5-(2-Methoxyethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]prop-2-enamideIC504163.0 [1], 10000.0 [2]
Items per page: 1 - 10 of 100
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References

This online tool may be cited as follows

MLA

"Quest Database™ Tyrosine-protein kinase JAK1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Dec. 2024, https://www.aatbio.com/data-sets/tyrosine-protein-kinase-jak1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, December 21). Quest Database™ Tyrosine-protein kinase JAK1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/tyrosine-protein-kinase-jak1-inhibitors-ic50-ki.
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