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Tyrosine-protein kinase JAK2 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
TofacitinibIC5011.0 [1]
TofacitinibKi0.7 [1], 0.99 [2]
RuxolitinibIC503.0 [1]
RuxolitinibKi0.1 [1], 0.24 [2]
FilgotinibIC503524.0 [1]
BaricitinibIC507.0 [1]
StaurosporineIC502.0 [1]
Pyridone 6IC501.0 [1], 1400.0 [2]
N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamideIC50803.0 [1], 7178.0 [2], 9297.0 [3], 20000.0 [4]
Unii-7N5LJ2Z26CIC502.0 [1], 3.0 [2], 5.0 [3], 30.0 [4], 54.0 [5]
DecernotinibIC5013.0 [1], 24.0 [2], 10000.0 [3]
DecernotinibKi13.0 [1]
N-[4-[2-[(4-Morpholin-4-Ylphenyl)amino]pyrimidin-4-Yl]phenyl]ethanamideIC503.6 [1], 67.0 [2], 795.0 [3], 974.7 [4]
N-[4-[2-(3-Morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]acetamideIC504.2 [1], 19.6 [2], 591.0 [3], 615.0 [4]
N-[4-[2-(3-Piperidin-1-ylanilino)pyrimidin-4-yl]phenyl]acetamideIC506.5 [1], 13.8 [2], 956.1 [3], 1328.0 [4]
N-[4-[5-Methyl-2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]acetamideIC505.1 [1], 28.7 [2], 447.0 [3], 608.9 [4]
6-{[(1R)-2-Methyl-1-(trifluoromethyl)propyl]amino}pyrido[4,3-c]-1,6-naphthyridin-1(2H)-oneIC501.0 [1], 40.0 [2]
2-N-[(1S)-1-(5-Fluoropyrimidin-2-yl)ethyl]-6-N-(5-methyl-1H-pyrazol-3-yl)pyrazine-2,6-diamineIC503.0 [1]
7-(2-Aminopyrimidin-5-yl)-1-[[(1R)-1-cyclopropyl-2,2,2-trifluoroethyl]amino]-5H-pyrido[4,3-b]indole-4-carboxamideIC500.4 [1], 0.8 [2], 11.0 [3], 25.0 [4]
Jak-IN-1IC500.8 [1], 188.0 [2], 190.0 [3]
3-(4-Chlorophenyl)-6-(4-methylpiperazine-1-carbonyl)-9H-carbazole-1-carboxamideIC501.0 [1], 1.2 [2], 71.0 [3]
N-[4-(2-Anilinopyrimidin-4-yl)phenyl]acetamideIC5012.8 [1], 27.4 [2], 1004.3 [3], 1971.0 [4]
1-(Ethylamino)-8-fluoro-5H-pyrido[4,3-b]indole-4-carboxamideIC50230.0 [1], 15000.0 [2]
4-Amino-2-(4-morpholin-4-ylphenyl)thieno[3,2-c]pyridine-7-carboxamideIC5019.0 [1], 761.0 [2], 25000.0 [3]
4-Amino-2-[4-(Tert-Butylsulfamoyl)phenyl]-N-Methylthieno[3,2-C]pyridine-7-CarboxamideIC501.0 [1], 48.0 [2], 1010.0 [3], 1480.0 [4]
4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-[2-(dimethylamino)ethyl]thieno[3,2-c]pyridine-7-carboxamideIC508.0 [1], 515.0 [2], 2400.0 [3], 7830.0 [4]
4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-morpholin-4-ylethyl)thieno[3,2-c]pyridine-7-carboxamideIC502.0 [1], 148.0 [2], 1620.0 [3], 2190.0 [4]
4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-methoxyethyl)thieno[3,2-c]pyridine-7-carboxamideIC503.0 [1], 135.0 [2], 959.0 [3], 3950.0 [4]
1-Cyclopropyl-N-[3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl]methanesulfonamideIC501196.0 [1], 1200.0 [2], 7180.0 [3], 7540.0 [4]
FedratinibIC503.0 [1]
MomelotinibIC5011.0 [1], 18.0 [2], 41.0 [3]
CID 16722832IC506.0 [1]
(16E)-14-Methyl-20-oxa-5,7,14,27-tetrazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2(27),3,5,8,10,12(26),16,21,23-decaeneIC5073.0 [1], 170.0 [2]
CID 57336812IC501.3 [1], 1.8 [2], 61.0 [3]
2,6-Dichloro-N-{2-[(Cyclopropylcarbonyl)amino]pyridin-4-Yl}benzamideKi27.6 [1], 28.0 [2]
3-[5-[4-(2-Hydroxy-2-methylpropanoyl)piperazin-1-yl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)pyrrole-2,5-dioneIC50578.0 [1], 2550.0 [2], 10000.0 [3]
3-Cyclohexyl-4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaeneIC506000.0 [1]
3-Cyclohexyl-4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaeneKi5.0 [1]
1-(2-Aminoethyl)-2-(4-piperidinyl)-1H-benzoimidazole-5-carboxamideIC503150.0 [1], 3200.0 [2], 437300.0 [3]
N-[(2R)-1-(3-Cyanoazetidin-1-yl)-1-oxopropan-2-yl]-2-cyclopropyl-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC5036.8 [1], 37.0 [2], 8900.0 [3]
3-(3,4-Dichlorophenyl)-6-(Morpholin-4-Ylcarbonyl)-9h-Carbazole-1-CarboxamideIC502.4 [1], 200.0 [2]
3-(3-Methoxyphenyl)-6-(morpholine-4-carbonyl)-9H-carbazole-1-carboxamideIC502.8 [1], 16.0 [2]
2-[5-Methyl-2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1-benzofuran-5-carbonitrileIC5010.4 [1], 1052.0 [2], 3088.0 [3]
N-[3-[[4-(4-Acetamidophenyl)pyrimidin-2-yl]amino]phenyl]-2,6-dichlorobenzamideIC5012.6 [1], 505.0 [2], 763.0 [3]
Atropisomer 1IC50270.0 [1], 870.0 [2]
Atropisomer 1Ki0.0 [1]
8-(4-Methylsulfonylphenyl)-N-(4-Morpholin-4-Ylphenyl)-[1,2,4]triazolo[1,5-A]pyridin-2-AmineIC500.9 [1], 61.0 [2]
N-[4-(4-Methylpiperazin-1-yl)phenyl]-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amineIC502.4 [1], 3.0 [2], 64.0 [3]
N-[3-[(1,1-Dioxo-1,4-thiazinan-4-yl)methyl]phenyl]-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amineIC500.64 [1], 0.67 [2], 107.0 [3]
N-(3-Methoxyphenyl)-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amineIC501.0 [1], 1.4 [2], 176.0 [3]
N-[3-(4-Methylpiperazin-1-yl)phenyl]-8-(4-propan-2-ylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amineIC501.27 [1], 1.3 [2], 85.0 [3]
8-(4-Dimethylphosphorylphenyl)-N-[3-(4-methylpiperazin-1-yl)phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-amineIC501.73 [1], 3.0 [2], 318.0 [3]
N-(4-Methoxyphenyl)-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amineIC501.0 [1], 3.0 [2], 209.0 [3]
8-(4-Methylsulfonylphenyl)-N-(3-morpholin-4-ylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amineIC500.4 [1], 0.8 [2], 110.0 [3]
N-[3-[(4-Methylpiperazin-1-yl)methyl]phenyl]-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amineIC503.07 [1], 3.1 [2], 345.0 [3]
N-[3-[4-(4-Methylpiperazin-1-yl)piperidin-1-yl]phenyl]-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amineIC501.4 [1], 1.5 [2], 177.0 [3]
N-[3-(1-Methylpiperidin-4-yl)phenyl]-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amineIC500.7 [1], 50.0 [2]
N-(3-Methylsulfonylphenyl)-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amineIC505.57 [1], 5.6 [2], 490.0 [3]
N,8-Bis(4-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amineIC501.3 [1], 118.0 [2]
N-[3-(4-Methylpiperazin-1-yl)phenyl]-8-[4-(trifluoromethyl)phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-amineIC503.7 [1], 4.0 [2], 476.0 [3]
(2R)-2-Amino-3-hydroxy-N-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]propanamideIC502.7 [1], 621.7 [2], 1391.0 [3]
(2R)-1-Ethyl-N-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]pyrrolidine-2-carboxamideIC509.1 [1], 1431.3 [2], 2166.0 [3]
(2r)-N-[4-[2-[(4-Morpholin-4-Ylphenyl)amino]pyrimidin-4-Yl]phenyl]pyrrolidine-2-CarboxamideIC502.2 [1], 386.4 [2], 695.0 [3]
(2R)-1-Methyl-N-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]pyrrolidine-2-carboxamideIC505.2 [1], 745.7 [2], 1051.0 [3]
(2R)-2-Amino-N-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]propanamideIC501.7 [1], 327.7 [2], 452.0 [3]
(2S)-2-Amino-N-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]propanamideIC508.7 [1], 1052.5 [2], 1510.0 [3]
5-Amino-N-[3-(2,5-dimethylphenyl)-1-methylpyrazol-4-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamideIC5040.4 [1]
5-Amino-N-[3-(2,5-dimethylphenyl)-1-methylpyrazol-4-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamideKi0.3 [1]
5-Amino-N-[3-(2,5-dichlorophenyl)-1-methylpyrazol-4-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamideIC503.9 [1], 7.4 [2]
5-Amino-N-[3-(2,5-dichlorophenyl)-1-methylpyrazol-4-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamideKi0.1 [1]
5-Amino-N-[3-(3-chlorophenyl)-1,2-oxazol-4-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamideIC50158.0 [1]
5-Amino-N-[3-(3-chlorophenyl)-1,2-oxazol-4-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamideKi1.8 [1], 2.0 [2]
N-[4-(4-Methylpiperazin-1-yl)phenyl]-5-(3-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amineIC509.2 [1], 73.1 [2]
N-[4-(4-Methylpiperazin-1-yl)phenyl]-5-(3-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amineKi2.0 [1]
N-[4-(4-Methylpiperazin-1-yl)phenyl]-5-(4-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amineIC506.9 [1], 32.9 [2]
N-[4-(4-Methylpiperazin-1-yl)phenyl]-5-(4-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amineKi0.3 [1]
3-(3-Fluoro-4-methoxyphenyl)-7-(morpholine-4-carbonyl)-9H-carbazole-1-carboxamideIC505.5 [1], 7.0 [2], 110.0 [3]
3-(2,4-Dichlorophenyl)-6-(morpholine-4-carbonyl)-9H-carbazole-1-carboxamideIC506.8 [1], 7.0 [2], 216.0 [3]
3-(6-Methylpyridin-3-yl)-7-morpholino-9H-carbazole-1-carboxamideIC506.0 [1], 6.1 [2], 120.0 [3]
N-[3-(2,5-Dichlorophenyl)-1-methylpyrazol-4-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamideIC5042.3 [1]
N-[3-(2,5-Dichlorophenyl)-1-methylpyrazol-4-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamideKi0.4 [1], 13.7 [2]
4-N-[(1S)-1-(3,5-Difluoropyridin-2-yl)ethyl]-5-fluoro-2-N-(5-methyl-1H-pyrazol-3-yl)-6-morpholin-4-ylpyrimidine-2,4-diamineIC503.0 [1], 7.0 [2]
4-N-[(1S)-1-(3,5-Difluoropyridin-2-yl)ethyl]-5-fluoro-2-N-(5-methyl-1H-pyrazol-3-yl)-6-morpholin-4-ylpyrimidine-2,4-diamineKi1.41 [1]
4-(5-Methylsulfonyl-6,7-dihydro-4H-furo[3,2-c]pyridin-2-yl)-N-[4-(2-pyrrolidin-1-ylethoxy)phenyl]pyrimidin-2-amineIC50164.0 [1], 1258.0 [2], 4311.0 [3]
3-[2-[2-(4-Morpholin-4-ylanilino)pyrimidin-4-yl]-6,7-dihydro-4H-furo[3,2-c]pyridin-5-yl]-3-oxopropanenitrileIC5013.2 [1], 3125.0 [2], 5521.0 [3]
3-[2-[2-[4-(4-Methylpiperazin-1-yl)anilino]pyrimidin-4-yl]-6,7-dihydro-4H-furo[3,2-c]pyridin-5-yl]-3-oxopropanenitrileIC5053.7 [1], 2338.0 [2], 7443.0 [3]
Jak2-IN-4IC500.7 [1], 425.6 [2], 1254.0 [3]
N-Methyl-N-[3-(propylsulfonylmethyl)cyclobutyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amineIC50550.0 [1], 946.0 [2], 20000.0 [3]
N-[3-(Butylsulfonylmethyl)cyclobutyl]-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amineIC50220.0 [1], 4090.0 [2]
2,2,2-Trifluoro-N-[3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl]ethanesulfonamideIC50381.0 [1], 4120.0 [2]
2-Methyl-N-[3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl]propane-1-sulfonamideIC50542.0 [1], 9400.0 [2]
N-[3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl]-1-(oxetan-3-yl)methanesulfonamideIC50933.0 [1], 6810.0 [2]
4-[[3-[[2-Cyanoethyl(methyl)sulfamoyl]amino]cyclobutyl]-methylamino]-7H-pyrrolo[2,3-d]pyrimidineIC50412.0 [1], 4460.0 [2]
3-(4-Cyanoanilino)-1-[(3R,4S)-4-cyanooxan-3-yl]pyrazole-4-carboxamideIC500.7 [1], 1.2 [2], 89.0 [3]
1-[(3R,4S)-4-Cyanooxan-3-yl]-3-[(2-fluoropyridin-4-yl)amino]pyrazole-4-carboxamideIC502.0 [1], 2.8 [2], 414.0 [3]
1-[(3R,4S)-4-Cyanooxan-3-yl]-3-[4-[(1S)-2,2,2-trifluoro-1-hydroxyethyl]anilino]pyrazole-4-carboxamideIC500.47 [1], 0.7 [2], 48.0 [3]
3-(4-Chloroanilino)-1-[(3R,4S)-4-cyanooxan-3-yl]pyrazole-4-carboxamideIC501.5 [1], 3.0 [2], 140.0 [3]
3-Anilino-1-[(3R,4S)-4-cyanooxan-3-yl]pyrazole-4-carboxamideIC503.0 [1], 67.0 [2], 209.0 [3]
3-(4-Chloroanilino)-1-[(1S,2S,4S)-2-cyano-4-(dimethylamino)cyclohexyl]pyrazole-4-carboxamideIC5019.0 [1], 23.0 [2], 692.0 [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]benzonitrileIC5024.0 [1], 42.0 [2], 95.0 [3]



References

This online tool may be cited as follows

MLA

"Quest Database™ Tyrosine-protein kinase JAK2 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.22 Dec2024https://www.aatbio.com/data-sets/tyrosine-protein-kinase-jak2-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 22). Quest Database™ Tyrosine-protein kinase JAK2 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/tyrosine-protein-kinase-jak2-inhibitors-ic50-ki.
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