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Tyrosine-protein kinase ITK/TSK Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
N-[1-(3-Amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]-4-cyanobenzamideIC5017.0 [1]
N-[1-(3-Aminopropyl)-5-[cyclohexanecarbonyl(methyl)amino]benzimidazol-2-yl]thiophene-2-carboxamideIC5025.0 [1], 110.0 [2], 320.0 [3], 1600.0 [4], 5000.0 [5]
N-[1-(3-Amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]thiophene-2-carboxamideIC5014.0 [1], 25.0 [2], 58.0 [3], 2400.0 [4], 2700.0 [5]
IbrutinibIC5010.7 [1], 11.7 [2], 13.9 [3]
N-[5-[[3-(4-Acetylpiperazine-1-carbonyl)-4,5-dimethylphenyl]methylsulfanyl]-1,3-thiazol-2-yl]-4-[(3,3-dimethylbutan-2-ylamino)methyl]benzamideIC5090.0 [1], 96.0 [2], 650.0 [3], 700.0 [4]
3-[4-Amino-1-[(3R)-1-prop-2-enoylpiperidin-3-yl]pyrazolo[3,4-d]pyrimidin-3-yl]-N-(3-methyl-4-propan-2-ylphenyl)benzamideIC502.0 [1], 31.0 [2], 48.0 [3]
N-[1-(3-Amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]-4-chlorobenzamideIC506.0 [1], 18.0 [2], 340.0 [3], 1300.0 [4]
N-[1-[(1S)-3-(Dimethylamino)-1-phenylpropyl]pyrazol-4-yl]-6-(1H-pyrazol-4-yl)-1H-indazole-3-carboxamideIC5025.0 [1], 173.0 [2]
N-[1-[(1S)-3-(Dimethylamino)-1-phenylpropyl]pyrazol-4-yl]-6-(1H-pyrazol-4-yl)-1H-indazole-3-carboxamideKi0.1 [1]
N-[1-(3-Cyanobenzyl)-1h-Pyrazol-4-Yl]-6-(1h-Pyrazol-4-Yl)-1h-Indazole-3-CarboxamideIC50210.0 [1], 231.0 [2]
N-[1-(3-Cyanobenzyl)-1h-Pyrazol-4-Yl]-6-(1h-Pyrazol-4-Yl)-1h-Indazole-3-CarboxamideKi0.8 [1], 1.1 [2]
N-(1-Benzylpyrazol-4-yl)-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamideIC505200.0 [1]
N-(1-Benzylpyrazol-4-yl)-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamideKi5.3 [1]
N-(1-Benzylpyrazol-4-yl)-5a-methyl-4,4a,5,6-tetrahydro-1H-cyclopropa[f]indazole-3-carboxamideIC50410.0 [1]
N-(1-Benzylpyrazol-4-yl)-5a-methyl-4,4a,5,6-tetrahydro-1H-cyclopropa[f]indazole-3-carboxamideKi3.0 [1], 200.0 [2]
6,6-Dimethyl-N-[1-[(1S)-3-methylsulfonyl-1-phenylpropyl]pyrazol-4-yl]-1,4,5,7-tetrahydroindazole-3-carboxamideIC50310.0 [1]
6,6-Dimethyl-N-[1-[(1S)-3-methylsulfonyl-1-phenylpropyl]pyrazol-4-yl]-1,4,5,7-tetrahydroindazole-3-carboxamideKi6.2 [1]
3-[4-Amino-1-[(3R)-1-prop-2-enoylpiperidin-3-yl]pyrazolo[3,4-d]pyrimidin-3-yl]-N-[(4-tert-butylphenyl)methyl]benzamideIC5010.0 [1], 516.0 [2], 6731.0 [3]
2-PropenaMide, N-[cis-4-[4-aMino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyriMidin-1-yl]cyclohexyl]-IC50909.9 [1], 1954.0 [2]
StaurosporineIC504.02 [1], 12.81 [2], 16000.0 [3]
N-[1-(2-Hydroxy-2-methylpropyl)-5-(morpholin-4-ylmethyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC502.0 [1], 13.0 [2], 220.0 [3]
N-[1-(3-Amino-3-oxopropyl)-5-[cyclohexanecarbonyl(methyl)amino]benzimidazol-2-yl]-4-cyanobenzamideIC504.0 [1], 300.0 [2]
N-[1-(3-Amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]benzamideIC503.0 [1], 180.0 [2], 2300.0 [3]
N-[1-(3-Amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]-1,2-oxazole-5-carboxamideIC5010.0 [1], 100.0 [2], 5000.0 [3]
N-[1-(3-Amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]-5-cyanothiophene-2-carboxamideIC508.0 [1], 15.0 [2], 150.0 [3]
N-[1-(3-Cyanobenzyl)-1h-Pyrazol-4-Yl]-2h-Indazole-3-CarboxamideIC504600.0 [1]
N-[1-(3-Cyanobenzyl)-1h-Pyrazol-4-Yl]-2h-Indazole-3-CarboxamideKi15.0 [1], 43.0 [2]
N-[1-[(1S)-3-(Dimethylamino)-1-phenylpropyl]pyrazol-4-yl]-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamideIC5045.0 [1], 55.0 [2]
N-[1-[(1S)-3-(Dimethylamino)-1-phenylpropyl]pyrazol-4-yl]-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamideKi0.7 [1]
N-[5-[[[(2S)-3,3-Dimethylbutan-2-yl]amino]methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC501.0 [1], 4.0 [2], 13.0 [3]
N-[5-[Benzoyl(methyl)amino]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamideIC503.0 [1], 110.0 [2], 200.0 [3]
N-[1-(2-Hydroxy-2-methylpropyl)-5-[(N-methylanilino)methyl]benzimidazol-2-yl]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamideIC50100.0 [1], 5000.0 [2]
N-[5-(Anilinomethyl)-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamideIC5011.0 [1], 180.0 [2], 5000.0 [3]
N-[5-[[Cyclohexyl(methyl)amino]methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamideIC508.0 [1], 180.0 [2], 670.0 [3]
N-[5-[(Cyclohexylamino)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(2-methyl-1,3-oxazol-5-yl)thiophene-2-carboxamideIC508.0 [1], 210.0 [2], 940.0 [3]
N-[1-(2-Hydroxy-2-methylpropyl)-5-[(N-methylanilino)methyl]benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC508.0 [1], 120.0 [2], 780.0 [3]
N-[5-(Anilinomethyl)-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC502.0 [1], 21.0 [2], 75.0 [3]
N-[5-[[Cyclohexyl(methyl)amino]methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC502.0 [1], 13.0 [2], 160.0 [3]
N-[5-[(Cyclohexylamino)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC501.0 [1], 20.0 [2], 99.0 [3]
N-[5-(Aminomethyl)-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC504.0 [1], 900.0 [2], 5000.0 [3]
N-[1-(2-Hydroxy-2-methylpropyl)-5-(methylaminomethyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC502.0 [1], 420.0 [2], 5000.0 [3]
N-[5-[(Dimethylamino)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC503.0 [1], 26.0 [2], 490.0 [3]
N-[5-[(Benzylamino)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC501.0 [1], 19.0 [2], 140.0 [3]
N-[1-(2-Hydroxy-2-methylpropyl)-5-[[methyl(pyridin-3-ylmethyl)amino]methyl]benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC501.0 [1], 6.0 [2], 100.0 [3]
N-[5-[(Butan-2-ylamino)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC502.0 [1], 25.0 [2], 390.0 [3]
N-[1-(2-Hydroxy-2-methylpropyl)-5-[(2-methylpropylamino)methyl]benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC501.0 [1], 12.0 [2], 140.0 [3]
N-[5-[[[(2R)-3,3-Dimethylbutan-2-yl]amino]methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC501.0 [1], 3.0 [2], 20.0 [3]
N-[5-[[[(2R)-3,3-Dimethylbutan-2-yl]-methylamino]methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC501.0 [1], 2.0 [2], 20.0 [3]
N-[5-[[[(2S)-3,3-Dimethylbutan-2-yl]-methylamino]methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC501.0 [1], 3.0 [2], 8.0 [3]
N-[5-[[2-(Dimethylamino)ethyl-methylamino]methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC502.0 [1], 62.0 [2], 180.0 [3]
N-[1-(2-Hydroxy-2-methylpropyl)-5-(piperidin-1-ylmethyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC503.0 [1], 11.0 [2], 250.0 [3]
N-[5-[[2-(Hydroxymethyl)piperidin-1-yl]methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC503.0 [1], 58.0 [2], 660.0 [3]
N-[5-[(3,5-Dimethylmorpholin-4-yl)methyl]-1-(2-hydroxy-2-methylpropyl)benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC501.0 [1], 3.0 [2], 98.0 [3]
N-[1-(2-Hydroxy-2-methylpropyl)-5-[(3-hydroxypyrrolidin-1-yl)methyl]benzimidazol-2-yl]-5-(1H-pyrazol-4-yl)thiophene-2-carboxamideIC502.0 [1], 130.0 [2], 310.0 [3]
3-[4-Amino-1-[(3S)-1-prop-2-enoylpiperidin-3-yl]pyrazolo[3,4-d]pyrimidin-3-yl]-N-(4-propan-2-ylphenyl)benzamideIC50400.0 [1], 780.0 [2], 1350.0 [3]
3-[4-Amino-1-[(3R)-1-prop-2-enoylpiperidin-3-yl]pyrazolo[3,4-d]pyrimidin-3-yl]-N-(4-propan-2-ylphenyl)benzamideIC5010.0 [1], 40.0 [2], 160.0 [3]
3-[4-Amino-1-(1-prop-2-enoylpiperidin-3-yl)pyrazolo[3,4-d]pyrimidin-3-yl]-N-(3-tert-butylphenyl)benzamideIC5010.0 [1], 73.0 [2], 2210.0 [3]
1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-oneIC508510.0 [1]
1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-oneKi26.9 [1]
Bms-509744IC5019.0 [1]
Bms-509744Ki16.0 [1]
Bms-986142IC5015.0 [1], 410.0 [2]
2-(1H-Indazol-3-yl)-1H-indole-6-carboxylic acidIC503980.0 [1]
3-(6-Methoxy-1H-indol-2-yl)-1H-pyrazolo[4,3-b]pyridineIC5060.0 [1]
N-[1-(3-Amino-3-oxopropyl)-5-[(4,4-difluorocyclohexanecarbonyl)-methylamino]benzimidazol-2-yl]-4-cyanobenzamideIC508.0 [1], 2300.0 [2]
trans-4-{[4-(1,3-Benzothiazol-2-ylamino)-6-(phenylmethyl)-2-pyrimidinyl]amino}cyclohexanolKi1.0 [1], 4.0 [2]
N-[5-[[3-(4-Acetylpiperazine-1-carbonyl)phenyl]methylsulfanyl]-1,3-thiazol-2-yl]-4-(dimethylamino)benzamideIC501000.0 [1]
1-(3-Aminopropyl)-N-cyclohexyl-N-methyl-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamideIC50950.0 [1], 20000.0 [2]
1-(3-Amino-3-oxopropyl)-2-[(4-bromobenzoyl)amino]-N-cyclohexyl-N-prop-2-enylbenzimidazole-5-carboxamideIC50230.0 [1], 1200.0 [2]
1-(3-Amino-3-oxopropyl)-N-cyclohexyl-2-[(4-fluorobenzoyl)amino]-N-methylbenzimidazole-5-carboxamideIC50250.0 [1], 4100.0 [2]
N-Cyclohexyl-N-methyl-1-[3-(methylamino)-3-oxopropyl]-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamideIC50160.0 [1], 24000.0 [2]
1-(3-Amino-3-oxopropyl)-N-cyclohexyl-2-[(4-methoxybenzoyl)amino]-N-methylbenzimidazole-5-carboxamideIC501100.0 [1], 17000.0 [2]
N-Cyclohexyl-1-(3-hydroxypropyl)-N-methyl-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamideIC5092.0 [1], 2000.0 [2]
Ethyl 3-[5-[cyclohexyl(methyl)carbamoyl]-2-(thiophene-2-carbonylamino)benzimidazol-1-yl]propanoateIC50270.0 [1], 1100.0 [2]
N-Cyclohexyl-N-methyl-1-(2-phenylethyl)-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamideIC501300.0 [1], 1800.0 [2]
1-(3-Amino-3-oxopropyl)-2-[(4-bromobenzoyl)amino]-N-cyclohexyl-N-methylbenzimidazole-5-carboxamideIC50260.0 [1], 1200.0 [2]
N-Cyclohexyl-N-methyl-1-propyl-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamideIC50760.0 [1], 1600.0 [2]
1-(3-Amino-3-oxopropyl)-2-benzamido-N-cyclohexyl-N-methylbenzimidazole-5-carboxamideIC50370.0 [1], 11000.0 [2]
1-(3-Amino-3-oxopropyl)-N-cyclohexyl-N-methyl-2-(pyridine-3-carbonylamino)benzimidazole-5-carboxamideIC5069.0 [1], 2700.0 [2]
1-(3-Amino-3-oxopropyl)-N-cyclohexyl-2-[(3-fluorobenzoyl)amino]-N-methylbenzimidazole-5-carboxamideIC50110.0 [1], 7400.0 [2]
1-(5-Amino-5-oxopentyl)-N-cyclohexyl-N-methyl-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamideIC5060.0 [1], 3100.0 [2]
1-(3-Amino-3-oxopropyl)-2-benzamido-N-cyclohexyl-N-ethylbenzimidazole-5-carboxamideIC50390.0 [1], 8100.0 [2]
1-(3-Amino-3-oxopropyl)-2-[(4-cyanobenzoyl)amino]-N-cyclohexyl-N-methylbenzimidazole-5-carboxamideIC50200.0 [1], 7200.0 [2]
N-Cyclohexyl-1-(2-hydroxyethyl)-N-methyl-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamideIC50190.0 [1], 4600.0 [2]
1-(3-Amino-3-oxopropyl)-N-cyclohexyl-N-methyl-2-[(4-nitrobenzoyl)amino]benzimidazole-5-carboxamideIC5076.0 [1], 6900.0 [2]
1-(3-Amino-3-oxopropyl)-2-[(4-bromobenzoyl)amino]-N-cyclohexyl-N-ethylbenzimidazole-5-carboxamideIC5081.0 [1], 1200.0 [2]
1-(3-Amino-3-oxopropyl)-2-benzamido-N-methyl-N-phenylbenzimidazole-5-carboxamideIC50330.0 [1], 2600.0 [2]
1-(3-Amino-3-oxopropyl)-N-cyclohexyl-N-methyl-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamideIC50110.0 [1], 2700.0 [2]
1-(4-Amino-4-oxobutyl)-N-cyclohexyl-N-methyl-2-(thiophene-2-carbonylamino)benzimidazole-5-carboxamideIC50140.0 [1], 4600.0 [2]
1-(3-Amino-3-oxopropyl)-2-benzamido-N-cyclohexyl-N-prop-2-enylbenzimidazole-5-carboxamideIC50730.0 [1], 7200.0 [2]
N-[1-(3-Amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]-5-pyridin-2-ylthiophene-2-carboxamideIC5019.0 [1], 650.0 [2]
N-[1-(3-Amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]-5-phenylthiophene-2-carboxamideIC5039.0 [1], 820.0 [2]
N-[1-(3-Amino-3-oxopropyl)-5-[benzoyl(methyl)amino]benzimidazol-2-yl]-5-pyridin-4-ylthiophene-2-carboxamideIC502.0 [1], 510.0 [2]
N-[1-[(S)-(1,1-Dioxothiolan-3-yl)-phenylmethyl]pyrazol-4-yl]-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamideIC5025.0 [1]
N-[1-[(S)-(1,1-Dioxothiolan-3-yl)-phenylmethyl]pyrazol-4-yl]-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamideKi0.5 [1]
N-[1-[(S)-(1,1-Dioxothian-3-yl)-phenylmethyl]pyrazol-4-yl]-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamideIC5036.0 [1]
N-[1-[(S)-(1,1-Dioxothian-3-yl)-phenylmethyl]pyrazol-4-yl]-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamideKi0.2 [1]
N-[1-[(R)-(1,1-Dioxothian-2-yl)-phenylmethyl]pyrazol-4-yl]-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamideIC5014.0 [1]
N-[1-[(R)-(1,1-Dioxothian-2-yl)-phenylmethyl]pyrazol-4-yl]-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamideKi0.3 [1]
N-[1-[(S)-(1,1-Dioxothian-4-yl)-phenylmethyl]pyrazol-4-yl]-6,6-dimethyl-1,4,5,7-tetrahydroindazole-3-carboxamideIC5060.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Tyrosine-protein kinase ITK/TSK Inhibitors (IC50, Ki)." AAT Bioquest, Inc.10 May2024https://www.aatbio.com/data-sets/tyrosine-protein-kinase-itk-tsk-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 10). Quest Database™ Tyrosine-protein kinase ITK/TSK Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/tyrosine-protein-kinase-itk-tsk-inhibitors-ic50-ki.
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