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JAK3/JAK1 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
TofacitinibIC5033.0 [1]
FilgotinibIC50148.0 [1], 154.0 [2], 2140.0 [3]
Jak-IN-1IC5031.0 [1], 1008.0 [2]
RuxolitinibIC5023.0 [1], 1850.0 [2]
BaricitinibIC5067.0 [1], 259.0 [2]
N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamideIC50511.0 [1], 1298.0 [2]
N-[(2R)-1-(3-Cyanoazetidin-1-yl)-1-oxopropan-2-yl]-2-cyclopropyl-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC50328.0 [1], 805.0 [2]
Jak3-IN-6IC50280.0 [1], 5100.0 [2]
4-Amino-2-(4-morpholin-4-ylphenyl)thieno[3,2-c]pyridine-7-carboxamideIC50548.0 [1], 25000.0 [2]
2-Cyclopropyl-N-[(2s)-3-Hydroxy-3-Methylbutan-2-Yl]-5h-Pyrrolo[2,3-B]pyrazine-7-CarboxamideIC502230.0 [1], 15700.0 [2]
N-[(1R)-2-(3-Cyanoazetidin-1-yl)-1-cyclopropyl-2-oxoethyl]-2-cyclopropyl-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC5030.0 [1], 511.0 [2]
N-[(1R)-2-[(3S)-3-Cyanopyrrolidin-1-yl]-1-cyclopropyl-2-oxoethyl]-2-cyclopropyl-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC5028.0 [1], 1150.0 [2]
4-Amino-2-[4-(Tert-Butylsulfamoyl)phenyl]-N-Methylthieno[3,2-C]pyridine-7-CarboxamideIC50625.0 [1], 25000.0 [2]
2-Cyclopropyl-N-[(2s)-3,3-Dimethylbutan-2-Yl]-5h-Pyrrolo[2,3-B]pyrazine-7-CarboxamideIC50211.0 [1], 2460.0 [2]
N-[(2S)-3-Cyano-3-methylbutan-2-yl]-2-cyclopropyl-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC50214.0 [1], 1090.0 [2]
4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-[2-(dimethylamino)ethyl]thieno[3,2-c]pyridine-7-carboxamideIC5025000.0 [1]
4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-morpholin-4-ylethyl)thieno[3,2-c]pyridine-7-carboxamideIC507300.0 [1], 25000.0 [2]
4-Amino-2-[4-(tert-butylsulfamoyl)phenyl]-N-(2-methoxyethyl)thieno[3,2-c]pyridine-7-carboxamideIC504450.0 [1], 25000.0 [2]
N-[(2R)-1-(3-Cyanopyrrolidin-1-yl)-1-oxopropan-2-yl]-2-cyclopropyl-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC50553.0 [1], 5020.0 [2]
Bms-911543IC50990.0 [1]
DecernotinibIC50932.0 [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)methanoneIC501800.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(4-fluorophenyl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50420.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-pyrimidin-5-ylpyrrolo[1,2-b]pyridazine-3-carboxamideIC50240.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(3-fluoropyridin-4-yl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50120.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(3-methoxyphenyl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50200.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(3-methylphenyl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50700.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(6-fluoropyridin-3-yl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50100.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(2-methoxyphenyl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50680.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(3-cyanophenyl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC501000.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(6-propan-2-yloxypyridin-3-yl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50400.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(2-fluoropyridin-4-yl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50270.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(4-cyanophenyl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC5066.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(6-cyanopyridin-3-yl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50430.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(1H-pyrazol-5-yl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC5081.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-pyridin-4-ylpyrrolo[1,2-b]pyridazine-3-carboxamideIC5056.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(3-fluorophenyl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC501000.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(4-methoxyphenyl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50170.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(2-fluorophenyl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50630.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(6-methylpyridin-3-yl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC5084.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(3-chlorophenyl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50780.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(2-methylphenyl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50490.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(6-ethoxypyridin-3-yl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50800.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(3-methylpyridin-4-yl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC5075.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(4-methylphenyl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC502000.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(2-methoxypyridin-4-yl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50350.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(5-fluoropyridin-3-yl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50220.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-phenylpyrrolo[1,2-b]pyridazine-3-carboxamideIC50200.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(2-chlorophenyl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC501000.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(2-cyanophenyl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50500.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(2-methylpyridin-4-yl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC5055.0 [1]
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-oneIC50280.0 [1]
6-Anilino-4-[[3-(prop-2-enoylamino)phenyl]methylamino]pyridine-3-carboxamideIC5051.0 [1]
N-[(2R)-1-(3-Cyanoazetidin-1-yl)-1-oxopropan-2-yl]-2-(3,4,5-trimethoxyphenyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC50100.0 [1]
2-[[(3R)-3-Acetamido-2,3-dihydro-1H-inden-5-yl]oxy]-N-[(1R)-1-cyclopropylethyl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC501750.0 [1]
CID 67008828IC50700.0 [1]
N-[(2R)-1-(3-Cyanoazetidin-1-yl)-1-oxopropan-2-yl]-2-(6-fluoro-1-methylindazol-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC50150.0 [1]
2-(6-Chloro-4-fluoro-1-methylindazol-3-yl)-N-[(2R)-1-(3-cyanoazetidin-1-yl)-1-oxopropan-2-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC50430.0 [1]
N-[(2R)-1-(3-Cyanoazetidin-1-yl)-1-oxopropan-2-yl]-2-(6-methoxy-1-methylindazol-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC50180.0 [1]
2-(6-Chloro-1-methylindazol-3-yl)-N-[(2R)-1-(3-cyanoazetidin-1-yl)-1-oxopropan-2-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC50240.0 [1]
N-[(2R)-1-(3-Cyanoazetidin-1-yl)-1-oxopropan-2-yl]-2-(6,8-difluoroimidazo[1,5-a]pyridin-1-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC501290.0 [1]
2-(6-Chloro-1-methylindol-3-yl)-N-[(2R)-1-(3-cyanoazetidin-1-yl)-1-oxopropan-2-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC5050.0 [1]
N-[(2R)-1-(3-Cyanoazetidin-1-yl)-1-oxopropan-2-yl]-2-(6-fluoroimidazo[1,5-a]pyridin-1-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC50300.0 [1]
2-[[(3R)-3-Acetamido-2,3-dihydro-1H-inden-5-yl]oxy]-N-[(1R)-2-(3-cyanoazetidin-1-yl)-1-cyclopropyl-2-oxoethyl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamideIC507410.0 [1]
4-[(5-Hydroxy-2-adamantyl)amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide;hydrobromideIC5018.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(6-methoxypyridin-3-yl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC50100.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-pyridin-3-ylpyrrolo[1,2-b]pyridazine-3-carboxamideIC50110.0 [1]
4-[[(1R,3S)-3-Amino-2,2,3-trimethylcyclopentyl]amino]-6-(4-methylpyridin-3-yl)pyrrolo[1,2-b]pyridazine-3-carboxamideIC5097.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ JAK3/JAK1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.8 May2024https://www.aatbio.com/data-sets/jak3-jak1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 8). Quest Database™ JAK3/JAK1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/jak3-jak1-inhibitors-ic50-ki.
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