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Tyrosine-protein kinase TYK2 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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▼
TofacitinibIC5034.0 [1]
TofacitinibKi4.39 [1], 7.3 [2], 7.8 [3]
RuxolitinibIC5019.0 [1]
RuxolitinibKi0.5 [1], 0.55 [2]
Pyridone 6IC501.0 [1], 5.0 [2], 1700.0 [3]
BaricitinibIC508.7 [1], 53.0 [2], 61.0 [3], 200000.0 [4]
FilgotinibIC5086.77 [1], 116.0 [2], 2600.0 [3]
N-[(1R)-1-[3-[12-Methyl-8-(methylamino)-5-thia-3,7,10,12-tetrazatricyclo[7.3.0.02,6]dodeca-1(9),2(6),3,7,10-pentaen-4-yl]phenyl]ethyl]-2-methylsulfonylbenzamideIC5027.0 [1], 970.0 [2], 1000.0 [3], 2000.0 [4]
6-Anilino-8-(cyclopropylamino)imidazo[1,2-b]pyridazine-3-carboxamideIC5032.0 [1], 1100.0 [2], 1500.0 [3], 2000.0 [4]
6-(Cyclohexylamino)-8-(cyclopropylamino)imidazo[1,2-b]pyridazine-3-carboxamideIC50220.0 [1], 2000.0 [2], 3200.0 [3], 3400.0 [4]
6-(3,5-Difluoro-2-methoxyanilino)-N-[(2S)-2,3-dihydroxy-2-methylpropyl]-8-(methylamino)imidazo[1,2-b]pyridazine-3-carboxamideIC504.0 [1], 160.0 [2], 240.0 [3], 370.0 [4]
8-[[(2R)-2,3-Dihydroxy-2-methylpropyl]amino]-6-[3-[2-fluoro-4-(trifluoromethyl)phenyl]anilino]imidazo[1,2-b]pyridazine-3-carboxamideIC508.0 [1], 750.0 [2], 780.0 [3], 4200.0 [4]
6-[3-Cyano-5-(trifluoromethyl)anilino]-8-(cyclopropylamino)imidazo[1,2-b]pyridazine-3-carboxamideIC50480.0 [1], 8200.0 [2], 12600.0 [3], 50000.0 [4]
8-[[(1S,2R)-2-Fluorocyclopropyl]amino]-6-[3-[2-fluoro-4-(trifluoromethyl)phenyl]anilino]imidazo[1,2-b]pyridazine-3-carboxamideIC5025.0 [1], 320.0 [2], 410.0 [3], 10000.0 [4]
8-(Cyclopropylamino)-6-(3-fluoro-5-methylanilino)imidazo[1,2-b]pyridazine-3-carboxamideIC5024.0 [1], 1400.0 [2], 1700.0 [3], 2000.0 [4]
8-(Cyclopropylamino)-6-(3,5-dimethylanilino)imidazo[1,2-b]pyridazine-3-carboxamideIC5022.0 [1], 700.0 [2], 1400.0 [3], 50000.0 [4]
N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamideIC501250.0 [1], 200000.0 [2]
2,6-Dichloro-N-{2-[(Cyclopropylcarbonyl)amino]pyridin-4-Yl}benzamideKi4.8 [1]
3-[5-[4-(2-Hydroxy-2-methylpropanoyl)piperazin-1-yl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)pyrrole-2,5-dioneIC501691.0 [1], 2110.0 [2], 8055.0 [3]
1-(2-Aminoethyl)-2-(4-piperidinyl)-1H-benzoimidazole-5-carboxamideIC503700.0 [1], 759500.0 [2]
1-Cyclopropyl-N-[3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl]methanesulfonamideIC501870.0 [1], 10000.0 [2], 200000.0 [3]
Tyk2-IN-2IC507.0 [1], 50.0 [2], 100.0 [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]benzonitrileIC5056.0 [1], 140.0 [2], 370.0 [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-amineIC50180.0 [1], 230.0 [2], 1000.0 [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]anilineIC50130.0 [1], 240.0 [2], 1000.0 [3]
8-(Cyclobutylamino)-6-(3,5-dimethylanilino)imidazo[1,2-b]pyridazine-3-carboxamideIC50110.0 [1], 4100.0 [2], 6200.0 [3]
6-(3,5-Dimethylanilino)-8-(ethylamino)imidazo[1,2-b]pyridazine-3-carboxamideIC5017.0 [1], 600.0 [2]
8-Anilino-6-(3,5-dimethylanilino)imidazo[1,2-b]pyridazine-3-carboxamideIC5050.0 [1], 3700.0 [2], 4900.0 [3]
8-(Methylamino)-6-(3-phenylanilino)imidazo[1,2-b]pyridazine-3-carboxamideIC504.0 [1], 200.0 [2], 330.0 [3]
8-(Cyclopropylamino)-6-[3-[2-fluoro-4-(trifluoromethyl)phenyl]anilino]imidazo[1,2-b]pyridazine-3-carboxamideIC5066.0 [1], 1100.0 [2], 1200.0 [3]
6-(3,5-Dimethylanilino)-N-[3-hydroxy-2-(hydroxymethyl)-2-methylpropyl]-8-(methylamino)imidazo[1,2-b]pyridazine-3-carboxamideIC5015.0 [1], 330.0 [2], 480.0 [3]
6-(3-Tert-butylanilino)-8-(methylamino)imidazo[1,2-b]pyridazine-3-carboxamideIC5013.0 [1], 410.0 [2], 510.0 [3]
N-[(2S)-2,3-Dihydroxy-2-methylpropyl]-8-(methylamino)-6-(2,3,5,6-tetrafluoroanilino)imidazo[1,2-b]pyridazine-3-carboxamideIC508.0 [1], 300.0 [2], 450.0 [3]
6-(3,5-Dimethylanilino)-N-(3-hydroxy-2,2-dimethylpropyl)-8-(methylamino)imidazo[1,2-b]pyridazine-3-carboxamideIC502.0 [1], 110.0 [2], 300.0 [3]
N-Cyclopropyl-6-(3,5-dimethylanilino)-8-(methylamino)imidazo[1,2-b]pyridazine-3-carboxamideIC508.0 [1], 100.0 [2], 110.0 [3]
8-(Cyclopentylamino)-6-(3,5-dimethylanilino)imidazo[1,2-b]pyridazine-3-carboxamideIC50500.0 [1], 4800.0 [2], 7300.0 [3]
6-(3,5-Difluoro-2-methoxyanilino)-N-(3-hydroxy-2,2-dimethylpropyl)-8-(methylamino)imidazo[1,2-b]pyridazine-3-carboxamideIC506.0 [1], 30.0 [2], 70.0 [3]
N-Cyclopropyl-6-(2,3-dihydro-1,4-benzodioxin-5-ylamino)-8-(methylamino)imidazo[1,2-b]pyridazine-3-carboxamideIC506.0 [1], 10.0 [2], 20.0 [3]
N-(3-Hydroxy-2,2-dimethylpropyl)-6-(2-methoxyanilino)-8-(methylamino)imidazo[1,2-b]pyridazine-3-carboxamideIC505.0 [1], 120.0 [2], 150.0 [3]
StaurosporineIC500.35 [1], 0.6 [2]
OclacitinibIC5075.1 [1]
DecernotinibIC5011.0 [1], 10000.0 [2]
1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-oneIC5010000.0 [1]
2-Chloro-4-cyano-6-fluoro-N-[2-[[(1R,2R)-2-fluorocyclopropanecarbonyl]amino]pyridin-4-yl]benzamideKi1.6 [1]
4-Amino-N-methyl-2-phenylthieno[3,2-c]pyridine-7-carboxamideIC50937.0 [1], 25000.0 [2]
3-Amino-5-[(2S)-3-methylbutan-2-yl]-7-(1-methyl-5-morpholin-4-ylpyrazol-3-yl)-1H-pyrazolo[4,3-c]pyridin-4-oneIC500.55 [1], 200.0 [2]
3-Amino-5-[(2S)-3-methylbutan-2-yl]-7-(5-morpholin-4-ylpyridin-2-yl)-1H-pyrazolo[4,3-c]pyridin-4-oneIC500.92 [1], 48.0 [2]
3-Amino-5-(2-methylpropyl)-7-(1-methylpyrazol-3-yl)-1H-pyrazolo[4,3-c]pyridin-4-oneIC5072.0 [1], 1100.0 [2]
3-Amino-5-[(2R)-3-methylbutan-2-yl]-7-(5-morpholin-4-ylpyridin-2-yl)-1H-pyrazolo[4,3-c]pyridin-4-oneIC509.7 [1], 440.0 [2]
3-Amino-5-(3-methylbutan-2-yl)-7-(5-morpholin-4-ylpyridin-2-yl)-1H-pyrazolo[4,3-c]pyridin-4-oneIC501.5 [1], 54.0 [2]
3-Amino-5-(3-methylbutan-2-yl)-7-(1-methylpyrazol-3-yl)-1H-pyrazolo[4,3-c]pyridin-4-oneIC506.3 [1], 310.0 [2]
3-Amino-5-(2-methylpentan-3-yl)-7-(1-methylpyrazol-3-yl)-1H-pyrazolo[4,3-c]pyridin-4-oneIC5091.0 [1], 6900.0 [2]
3-Amino-7-[5-(2-hydroxypropan-2-yl)-1-methylpyrazol-3-yl]-5-[(2R)-3-methylbutan-2-yl]-1H-pyrazolo[4,3-c]pyridin-4-oneIC502.1 [1], 190.0 [2]
3-Amino-7-[5-(1,1-dioxo-1,4-thiazinan-4-yl)-1-methylpyrazol-3-yl]-5-[(2S)-3-methylbutan-2-yl]-1H-pyrazolo[4,3-c]pyridin-4-oneIC501.2 [1], 230.0 [2]
3-Amino-5-[(2S)-3-methylbutan-2-yl]-7-[1-methyl-5-(oxan-4-yl)pyrazol-3-yl]-1H-pyrazolo[4,3-c]pyridin-4-oneIC500.98 [1], 110.0 [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-enamideIC50459.0 [1], 11800.0 [2]
4-Amino-2-(4-morpholin-4-ylphenyl)thieno[3,2-c]pyridine-7-carboxamideIC5066.0 [1], 25000.0 [2]
4-Amino-N-Methyl-2-[4-(Morpholin-4-Yl)phenyl]thieno[3,2-C]pyridine-7-CarboxamideIC501330.0 [1], 25000.0 [2]
4-Amino-2-[4-(Tert-Butylsulfamoyl)phenyl]-N-Methylthieno[3,2-C]pyridine-7-CarboxamideIC50266.0 [1], 25000.0 [2]
Infigratinib phosphateIC503303.0 [1], 10000.0 [2]
4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-[2-(dimethylamino)ethyl]thieno[3,2-c]pyridine-7-carboxamideIC504100.0 [1], 25000.0 [2]
4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-morpholin-4-ylethyl)thieno[3,2-c]pyridine-7-carboxamideIC50757.0 [1], 25000.0 [2]
4-Amino-N-methyl-2-(4-methylphenyl)thieno[3,2-c]pyridine-7-carboxamideIC50888.0 [1], 25000.0 [2]
4-Amino-2-(4-tert-butylphenyl)-N-methylthieno[3,2-c]pyridine-7-carboxamideIC50202.0 [1], 25000.0 [2]
4-Amino-N-methyl-2-[4-(trifluoromethoxy)phenyl]thieno[3,2-c]pyridine-7-carboxamideIC50208.0 [1], 25000.0 [2]
4-Amino-2-[4-(2-cyanopropan-2-yl)phenyl]-N-methylthieno[3,2-c]pyridine-7-carboxamideIC50146.0 [1], 25000.0 [2]
4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-hydroxyethyl)thieno[3,2-c]pyridine-7-carboxamideIC50932.0 [1], 25000.0 [2]
4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-methoxyethyl)thieno[3,2-c]pyridine-7-carboxamideIC501480.0 [1], 25000.0 [2]
4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-piperidin-1-ylethyl)thieno[3,2-c]pyridine-7-carboxamideIC502670.0 [1], 25000.0 [2]
4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(3-morpholin-4-ylpropyl)thieno[3,2-c]pyridine-7-carboxamideIC501550.0 [1], 25000.0 [2]
N-[2-(2,6-Dichlorophenyl)-[1,3]thiazolo[5,4-c]pyridin-4-yl]cyclopropanecarboxamideKi0.5 [1]
N-Methyl-N-[3-(propylsulfonylmethyl)cyclobutyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amineIC503610.0 [1], 200000.0 [2]
N-[3-(Butylsulfonylmethyl)cyclobutyl]-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amineIC50553.0 [1], 200000.0 [2]
2,2,2-Trifluoro-N-[3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl]ethanesulfonamideIC501020.0 [1], 200000.0 [2]
2-Methyl-N-[3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl]propane-1-sulfonamideIC50479.0 [1], 200000.0 [2]
N-[3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl]-1-(oxetan-3-yl)methanesulfonamideIC502380.0 [1], 200000.0 [2]
3-N-(Cyclopropylmethylsulfamoyl)-1-N-methyl-1-N-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)cyclobutane-1,3-diamineIC501780.0 [1], 200000.0 [2]
4-[[3-[[2-Cyanoethyl(methyl)sulfamoyl]amino]cyclobutyl]-methylamino]-7H-pyrrolo[2,3-d]pyrimidineIC501190.0 [1], 200000.0 [2]
3-Amino-5-butan-2-yl-7-(1-methylpyrazol-3-yl)-1H-pyrazolo[4,3-c]pyridin-4-oneIC5033.0 [1], 650.0 [2]
3-Amino-5-[(2S)-3-methylbutan-2-yl]-7-(1-methylpyrazol-3-yl)-1H-pyrazolo[4,3-c]pyridin-4-oneIC505.5 [1], 150.0 [2]
2-[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]acetonitrileIC502.9 [1], 170.0 [2]
4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexan-1-olIC5096.0 [1], 150.0 [2]
[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]methanolIC5038.0 [1], 150.0 [2]
1-[[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]methyl]azetidin-3-olIC5049.0 [1], 810.0 [2]
4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexane-1-carbaldehydeIC5055.0 [1], 100.0 [2]
2-[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]propanenitrileIC5025.0 [1], 1000.0 [2]
(3R)-1-[[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]methyl]pyrrolidin-3-olIC5019.0 [1], 770.0 [2]
N-[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]morpholin-4-amineIC50500.0 [1], 1000.0 [2]
2-[[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]amino]-N-(2,2,2-trifluoroethyl)acetamideIC501000.0 [1]
N-(2-Bromo-2,2-difluoroethyl)-4-(4,5,6,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexan-1-amineIC5013.0 [1], 760.0 [2]
N-[(4-Chlorophenyl)methyl]-4-(4,5,6,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexan-1-amineIC50110.0 [1], 150.0 [2]
1,1,1-Trifluoro-3-[[4-(4,5,6,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]amino]-2-phenylpropan-2-olIC50270.0 [1], 1000.0 [2]
N-[(4-Fluorophenyl)methyl]-4-(4,5,6,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexan-1-amineIC50120.0 [1], 310.0 [2]
(3S)-1-[[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]methyl]pyrrolidin-3-olIC50100.0 [1], 1000.0 [2]
N-[[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]methyl]cyclopropanamineIC50100.0 [1], 940.0 [2]
N-Benzyl-4-(4,5,6,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexan-1-amineIC50110.0 [1], 330.0 [2]
2-[4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]-N-(2,2,2-trifluoroethyl)acetamideIC50790.0 [1], 880.0 [2]
N-(Cyanomethyl)-2-[4-(4,5,6,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)cyclohexyl]acetamideIC50540.0 [1], 1000.0 [2]
4-(4,5,6,8,10-Pentazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-3-yl)-N-(3-phenylpropyl)cyclohexan-1-amineIC50450.0 [1], 1000.0 [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]methyl]benzonitrileIC5088.0 [1], 310.0 [2]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Tyrosine-protein kinase TYK2 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Nov. 2024, https://www.aatbio.com/data-sets/tyrosine-protein-kinase-tyk2-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, November 21). Quest Database™ Tyrosine-protein kinase TYK2 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/tyrosine-protein-kinase-tyk2-inhibitors-ic50-ki.
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