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Tyrosine-protein kinase JAK3 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
TofacitinibIC502.2 [1]
TofacitinibKi0.24 [1], 0.4 [2], 1.0 [3]
RuxolitinibIC50428.0 [1]
RuxolitinibKi3.2 [1], 3.22 [2]
StaurosporineIC501.0 [1]
1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-oneIC5033.0 [1]
1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-oneKi6310.0 [1]
IbrutinibIC5010.4 [1], 16.1 [2], 100.0 [3], 146.0 [4]
BaricitinibIC5025.0 [1], 400.0 [2], 787.0 [3], 8000.0 [4]
Pyridone 6IC505.0 [1], 10.0 [2], 900.0 [3]
3-[5-[4-(2-Hydroxy-2-methylpropanoyl)piperazin-1-yl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)pyrrole-2,5-dioneIC500.5 [1], 1.0 [2], 8.0 [3], 11.0 [4], 525.0 [5]
FilgotinibIC50194.7 [1], 810.0 [2], 10000.0 [3]
N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamideIC50605.0 [1], 8000.0 [2], 10000.0 [3]
[(1S)-6-(5-Phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC500.7 [1], 49.0 [2], 458.0 [3], 10000.0 [4]
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-oneIC500.4 [1], 47.0 [2], 116.0 [3], 399.0 [4]
1-[(3R)-3-(7H-Pyrrolo[2,3-d]pyrimidin-4-ylamino)piperidin-1-yl]prop-2-en-1-oneIC500.7 [1], 56.0 [2], 107.0 [3], 580.0 [4]
N-[3-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]prop-2-enamideIC500.3 [1], 29.0 [2], 32.0 [3], 2280.0 [4]
[(1S)-1-Methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydroinden-1-yl]cyanamideIC500.7 [1], 56.0 [2], 5480.0 [3]
[(1S)-6-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC503.0 [1], 256.0 [2], 598.0 [3], 10000.0 [4]
[(1S)-6-[5-[3-(Hydroxymethyl)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-2,3-dihydro-1H-inden-1-yl]cyanamideIC500.5 [1], 78.0 [2], 498.0 [3], 10000.0 [4]
N-[3-[5-(2-Methoxyethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]prop-2-enamideIC500.5 [1], 31.0 [2], 63.0 [3], 953.0 [4]
2,2-Difluoro-6-[5-(2-methoxyethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-3H-1,4-benzoxazine-4-carbonitrileIC503.0 [1], 162.0 [2], 456.0 [3], 7252.0 [4]
2-PropenaMide, N-[cis-4-[4-aMino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyriMidin-1-yl]cyclohexyl]-IC508278.0 [1], 10000.0 [2]
DecernotinibIC501.2 [1], 2.5 [2]
DecernotinibKi2.5 [1]
3-(2-Aminoquinazolin-6-Yl)-4-Methyl-N-[3-(Trifluoromethyl)phenyl]benzamideIC5020.0 [1]
JAK3 covalent inhibitor-1IC5011.0 [1], 331.0 [2], 10000.0 [3]
1-(2-Aminoethyl)-2-(4-piperidinyl)-1H-benzoimidazole-5-carboxamideIC501260.0 [1], 1300.0 [2], 232500.0 [3]
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-enamideIC500.13 [1], 2.0 [2], 9.0 [3]
3-[(3R)-3-(4,5-Dimethoxy-8-oxo-9,14,16-triazatetracyclo[8.7.0.02,7.011,15]heptadeca-1(17),2,4,6,10,12,15-heptaen-9-yl)piperidin-1-yl]-3-oxopropanenitrileIC502.55 [1], 15.3 [2], 1550.0 [3]
9-Cyclohexyl-4,5-dimethoxy-9,14,16-triazatetracyclo[8.7.0.02,7.011,15]heptadeca-1(17),2,4,6,10,12,15-heptaen-8-oneIC502.92 [1], 65.9 [2], 3720.0 [3]
N-[(1R,3S)-3-(Cyanoamino)-5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]methanesulfonamideIC500.9 [1], 38.0 [2], 2240.0 [3]
[(1S,3R)-3-Hydroxy-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC501.0 [1], 163.0 [2], 1728.0 [3]
1-Cyclopropyl-N-[3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl]methanesulfonamideIC508000.0 [1], 10000.0 [2]
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]benzonitrileIC50460.0 [1], 660.0 [2], 1000.0 [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-amineIC50870.0 [1], 1000.0 [2]
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]anilineIC50260.0 [1], 420.0 [2], 560.0 [3]
CanertinibIC502000.0 [1], 3880.0 [2]
4-[(3-Bromophenyl)amino]-6-acrylamidoquinazolineIC503140.0 [1], 10000.0 [2]
1-Cyclopropyl-3-(3-(5-(morpholinomethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazol-4-yl)ureaIC501.0 [1], 1.1 [2]
OclacitinibIC5095.1 [1]
CID 57336812IC5084.7 [1], 150.0 [2]
SpebrutinibIC5022.5 [1], 1753.0 [2]
9-(1-Methylpyrazol-4-yl)-1-(1-prop-2-enoyl-2,3-dihydroindol-6-yl)benzo[h][1,6]naphthyridin-2-oneIC503336.0 [1], 5180.0 [2]
2,6-Dichloro-N-{2-[(Cyclopropylcarbonyl)amino]pyridin-4-Yl}benzamideKi253.0 [1]
[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)methanoneIC500.5 [1], 59.9 [2]
9-(Cyclohexylmethyl)-4,5-dimethoxy-9,14,16-triazatetracyclo[8.7.0.02,7.011,15]heptadeca-1(17),2,4,6,10,12,15-heptaen-8-oneIC501.65 [1], 76900.0 [2]
2-Methyl-N-[2-[3-(prop-2-enoylamino)anilino]pyrimidin-5-yl]-5-[[3-(trifluoromethyl)benzoyl]amino]benzamideIC501705.0 [1], 2680.0 [2]
CID 11993785IC505.1 [1]
4-[1-(Oxiran-2-ylmethyl)triazol-4-yl]-7H-pyrrolo[2,3-d]pyrimidineIC5035.0 [1]
Unii-7N5LJ2Z26CIC5035.0 [1], 220.0 [2]
5-Fluoro-2-[[(1S)-1-(5-fluoropyridin-2-yl)ethyl]amino]-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyridine-3-carbonitrileIC507.0 [1], 15.0 [2]
N-[(2R)-1-(3-Cyanoazetidin-1-yl)-1-oxopropan-2-yl]-2-cyclopropyl-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC508.2 [1]
Jak-IN-1IC500.26 [1], 0.3 [2]
6-Anilino-4-(benzylamino)pyridine-3-carboxamideIC504.5 [1], 5.0 [2]
Jak3-IN-6IC500.15 [1], 4.0 [2]
3-((1H-Pyrrol-2-yl)methylene)-5-(pyridin-3-yl)indolin-2-oneIC5027.0 [1], 38.0 [2]
4-Amino-N-methyl-2-phenylthieno[3,2-c]pyridine-7-carboxamideIC50767.0 [1], 25000.0 [2]
1-[(3R,4R)-4-Methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]prop-2-en-1-oneIC5075.0 [1], 1930.0 [2]
(E)-1-[(3R)-3-(7H-Pyrrolo[2,3-d]pyrimidin-4-ylamino)piperidin-1-yl]but-2-en-1-oneIC501610.0 [1], 10000.0 [2]
1-[(3R)-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]prop-2-en-1-oneIC5018.0 [1], 3840.0 [2]
(E)-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-enamideIC5022.0 [1], 51.0 [2]
(E)-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]prop-2-enenitrileIC500.21 [1], 27.0 [2]
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]propanenitrileIC5010.0 [1], 129.0 [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)methanoneIC500.6 [1], 1.7 [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]ethanoneIC50372.0 [1], 10000.0 [2]
9-Cycloheptyl-4,5-dimethoxy-9,14,16-triazatetracyclo[8.7.0.02,7.011,15]heptadeca-1(17),2,4,6,10,12,15-heptaen-8-oneIC501.09 [1], 18340.0 [2]
9-Cyclooctyl-4,5-dimethoxy-9,14,16-triazatetracyclo[8.7.0.02,7.011,15]heptadeca-1(17),2,4,6,10,12,15-heptaen-8-oneIC501.01 [1], 28860.0 [2]
4,5-Dimethoxy-9-(1-methylpiperidin-4-yl)-9,14,16-triazatetracyclo[8.7.0.02,7.011,15]heptadeca-1(17),2,4,6,10,12,15-heptaen-8-oneIC50124.1 [1], 61570.0 [2]
2-[[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]methylidene]propanedinitrileIC500.39 [1], 4.0 [2]
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-dimethylpropanamideIC5048.0 [1], 181.0 [2]
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]-2-(4-methylpiperazine-1-carbonyl)prop-2-enenitrileIC500.74 [1], 14.0 [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-oneIC500.5 [1], 49.0 [2]
[(1R,2R)-2-Methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC5013.0 [1], 1530.0 [2]
Methyl-[6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC50230.0 [1], 10000.0 [2]
[(1R,2S)-2-Methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC506.0 [1], 603.0 [2]
[(1R,2R)-2-Hydroxy-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC502.0 [1], 280.0 [2]
[(4R)-6-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-3,4-dihydro-2H-chromen-4-yl]cyanamideIC5026.0 [1], 6110.0 [2]
[(1R)-6-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC5066.0 [1], 5820.0 [2]
N-[(1R,3S)-3-(Cyanoamino)-5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-4-methoxybenzenesulfonamideIC5016.0 [1], 947.0 [2]
[1-Methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydroinden-1-yl]cyanamideIC501.0 [1], 92.0 [2]
N-[(1R,3S)-3-(Cyanoamino)-5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-2-methoxyethanesulfonamideIC501.0 [1], 111.0 [2]
[6-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC506.0 [1], 711.0 [2]
6-[5-(2-Methoxyethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-2,3-dihydro-1,4-benzoxazine-4-carbonitrileIC5017.0 [1], 1226.0 [2]
[6-[5-(2-Methoxyethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-3,4-dihydro-2H-chromen-4-yl]cyanamideIC5049.0 [1], 5828.0 [2]
[(4S)-6-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-3,4-dihydro-2H-chromen-4-yl]cyanamideIC507.0 [1], 781.0 [2]
[6-[5-(2-Methoxyethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-2,3-dihydro-1H-inden-1-yl]cyanamideIC5012.0 [1], 1592.0 [2]
3-Cyano-N-[(1R,3S)-3-(cyanoamino)-5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]benzenesulfonamideIC5014.0 [1], 468.0 [2]
[6-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-3,4-dihydro-2H-chromen-4-yl]cyanamideIC507.0 [1], 1211.0 [2]
[(1S,3S)-3-Hydroxy-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]cyanamideIC5013.0 [1], 1338.0 [2]
4-Amino-2-(4-morpholin-4-ylphenyl)thieno[3,2-c]pyridine-7-carboxamideIC5018.0 [1], 25000.0 [2]
(R)-3-(6-(1-(4-Chlorophenyl)ethylamino)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amineIC5081.0 [1], 11000.0 [2]
3-(6-(2-(4-Fluorophenyl)pyrrolidin-1-yl)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amineIC5086.0 [1], 3100.0 [2]
(R)-3-(6-(2,3-Dihydro-1H-inden-1-ylamino)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amineIC50200.0 [1], 20000.0 [2]
(R)-3-(6-(1-(4-Fluorophenyl)butylamino)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amineIC5010.0 [1], 2400.0 [2]
(R)-3-(6-(1-(4-Fluorophenyl)-2-methylpropylamino)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amineIC5012.0 [1], 4100.0 [2]
(R)-3-(6-(1-(4-Fluorophenyl)ethylamino)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amineIC507.0 [1], 3200.0 [2]
Atropisomer 1IC501530.0 [1]
Atropisomer 1Ki0.01 [1]
3-[6-[[(1R)-1-(4-Fluorophenyl)propyl]amino]pyrimidin-4-yl]pyrazolo[1,5-a]pyrimidin-2-amineIC5012.0 [1], 1900.0 [2]



References

This online tool may be cited as follows

MLA

"Quest Database™ Tyrosine-protein kinase JAK3 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Dec2024https://www.aatbio.com/data-sets/tyrosine-protein-kinase-jak3-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 21). Quest Database™ Tyrosine-protein kinase JAK3 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/tyrosine-protein-kinase-jak3-inhibitors-ic50-ki.
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