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Tyrosine-protein kinase BTK 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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IbrutinibIC500.5 [1]
IbrutinibKi4.8 [1]
FenebrutinibIC501.4 [1]
FenebrutinibKi0.91 [1], 1.3 [2], 1.6 [3], 3.4 [4], 12.6 [5]
7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxoquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamideIC5026.0 [1]
SpebrutinibIC500.72 [1]
SpebrutinibKi20.7 [1]
CID 46908026IC5013.2 [1]
Bms-986142IC5025.0 [1]
4-Tert-butyl-N-[2-methyl-3-[6-[4-(morpholine-4-carbonyl)anilino]-7H-purin-2-yl]phenyl]benzamideIC509.0 [1]
StaurosporineIC5022.07 [1]
BTK inhibitor 4bIC5013.0 [1]
2-[4-[(2R,6S)-2,6-Dimethylmorpholin-4-yl]anilino]-6-[(3S)-3-(prop-2-enoylamino)pyrrolidin-1-yl]pyridine-3-carboxamideIC506.1 [1]
(7R)-3-Fluoro-4-[3-(8-fluoro-1-methyl-2,4-dioxoquinazolin-3-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-6,7,8,9-tetrahydro-5H-carbazole-1-carboxamideIC502.2 [1], 36.0 [2], 88.3 [3], 150.0 [4], 374.3 [5]
2-PropenaMide, N-[cis-4-[4-aMino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyriMidin-1-yl]cyclohexyl]-IC501.0 [1]
9-(1-Methylpyrazol-4-yl)-1-(1-prop-2-enoyl-2,3-dihydroindol-6-yl)benzo[h][1,6]naphthyridin-2-oneIC506.59 [1], 7.0 [2], 12.0 [3]
9-(1-Methylpyrazol-4-yl)-1-(1-prop-2-enoyl-2,3-dihydroindol-6-yl)benzo[h][1,6]naphthyridin-2-oneKi14.2 [1]
2-Methyl-N-[2-[3-(prop-2-enoylamino)anilino]pyrimidin-5-yl]-5-[[3-(trifluoromethyl)benzoyl]amino]benzamideIC505.0 [1], 8.5 [2], 14.0 [3], 25.0 [4]
2-Methyl-N-[2-[3-(prop-2-enoylamino)anilino]pyrimidin-5-yl]-5-[[3-(trifluoromethyl)benzoyl]amino]benzamideKi27.2 [1]
2-[5-Fluoro-2-(hydroxymethyl)-3-[1-methyl-5-[[5-[4-(oxetan-3-yl)piperazin-1-yl]pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]-3,4,6,7,8,9-hexahydropyrazino[1,2-a]indol-1-oneIC503.9 [1], 4.0 [2], 35.0 [3], 36.5 [4]
2-[5-Fluoro-2-(hydroxymethyl)-3-[1-methyl-5-[[5-[4-(oxetan-3-yl)piperazin-1-yl]pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]-3,4,6,7,8,9-hexahydropyrazino[1,2-a]indol-1-oneKi0.69 [1]
2-[5-Fluoro-2-(hydroxymethyl)-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]-3,4,6,7,8,9-hexahydropyrazino[1,2-a]indol-1-oneIC502.0 [1], 27.6 [2], 29.0 [3]
2-[5-Fluoro-2-(hydroxymethyl)-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]-3,4,6,7,8,9-hexahydropyrazino[1,2-a]indol-1-oneKi0.35 [1]
1-(4-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-oneIC500.58 [1], 3.1 [2], 3.6 [3]
(E)-1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]-4-(dimethylamino)but-2-en-1-oneIC501.1 [1], 2.5 [2]
DasatinibIC501.3 [1], 5.0 [2], 100.0 [3]
AcalabrutinibIC503.0 [1], 3.1 [2], 198.0 [3], 296.9 [4]
Lfm-a13IC502500.0 [1], 17200.0 [2]
CID 24857323IC500.61 [1], 1.9 [2], 8.0 [3], 81.0 [4]
4-(4-((4-((3-Acrylamidophenyl)amino)-5-fluoropyrimidin-2-yl)amino)phenoxy)-N-methylpicolinamideIC501.0 [1], 9.5 [2]
4-(4-((4-((3-Acrylamidophenyl)amino)-5-fluoropyrimidin-2-yl)amino)phenoxy)-N-methylpicolinamideKi209.2 [1]
4-[4-[3-(6-Cyclopropyl-8-fluoro-1-oxoisoquinolin-2-yl)-2-(hydroxymethyl)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-N,N-dimethyl-3,6-dihydro-2H-pyridine-1-carboxamideIC507.0 [1], 21.6 [2]
TirabrutinibIC50103.0 [1], 312.3 [2], 1057.0 [3], 1662.0 [4]
(E)-4-(Dimethylamino)-N-[7-fluoro-4-(2-methylanilino)imidazo[1,5-a]quinoxalin-8-yl]-N-methylbut-2-enamideIC500.7 [1], 1.93 [2], 48.0 [3]
4-[8-Amino-1-[4-[[4-(trifluoromethyl)pyridin-2-yl]carbamoyl]phenyl]imidazo[1,5-a]pyrazin-3-yl]cyclohexane-1-carboxylic acidIC500.5 [1], 1.2 [2], 77.0 [3], 1237.0 [4]
(E)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)but-2-en-1-oneIC5020.0 [1]
1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-yn-1-oneIC500.72 [1]
3-Cyano-4-[3-(8-fluoro-1-methyl-2,4-dioxoquinazolin-3-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamideIC500.27 [1], 6.0 [2], 120.0 [3]
(7S)-3-Chloro-4-[3-(8-fluoro-1-methyl-2,4-dioxoquinazolin-3-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-6,7,8,9-tetrahydro-5H-carbazole-1-carboxamideIC501.2 [1], 1.5 [2], 19.0 [3], 160.0 [4]
4-[3-(8-Fluoro-1-methyl-2,4-dioxoquinazolin-3-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-3-methyl-9H-carbazole-1-carboxamideIC500.65 [1], 0.66 [2], 17.0 [3], 240.0 [4]
3-Fluoro-4-[3-(8-fluoro-1-methyl-2,4-dioxoquinazolin-3-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamideIC500.45 [1], 0.79 [2], 11.0 [3], 90.0 [4]
3-Chloro-4-[3-(8-fluoro-1-methyl-2,4-dioxoquinazolin-3-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamideIC501.8 [1], 4.0 [2], 11.0 [3], 320.0 [4]
(E)-N-[4-[4-Amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]cyclohexyl]-4-(dimethylamino)but-2-enamideIC501.38 [1], 1.4 [2]
PCI-32765 RacemateIC500.5 [1], 0.72 [2], 1.4 [3]
Gdc-0834IC502.3 [1], 6.0 [2], 14.0 [3]
CID 73389638IC501.9 [1], 2.1 [2]
2-Methyl-N-[2-[3-[[2-(prop-2-enoylamino)acetyl]amino]anilino]pyrimidin-5-yl]-5-[[3-(trifluoromethyl)benzoyl]amino]benzamideIC504.4 [1], 13.0 [2]
2-[4-(Morpholine-4-carbonyl)anilino]-6-[(3S)-3-(prop-2-enoylamino)pyrrolidin-1-yl]pyridine-3-carboxamideIC501.5 [1], 1.6 [2]
2-(4-Phenoxyphenoxy)-6-[(1S,4S)-5-prop-2-enoyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]pyridine-3-carboxamideIC500.7 [1], 9.7 [2], 82.0 [3]
4-Tert-butyl-N-[2-methyl-3-[2-[4-(morpholine-4-carbonyl)anilino]pyrimidin-4-yl]phenyl]benzamideIC502.3 [1], 9.0 [2], 1800.0 [3]
(S)-IbrutinibIC500.5 [1], 1.4 [2]
(7R)-3-Chloro-4-[3-(8-fluoro-1-methyl-2,4-dioxoquinazolin-3-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-6,7,8,9-tetrahydro-5H-carbazole-1-carboxamideIC502.6 [1], 84.0 [2], 350.0 [3]
8-Cyclopropyl-4-[3-[2-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-2-(hydroxymethyl)phenyl]-6-fluoro-2,3-dihydro-1,4-benzoxazepin-5-oneIC502.0 [1], 2.6 [2], 83.5 [3]
(7S)-4-[3-(8-Fluoro-1-methyl-2,4-dioxoquinazolin-3-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-6,7,8,9-tetrahydro-5H-carbazole-1-carboxamideIC502.7 [1], 63.0 [2], 380.0 [3]
1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)sulfonyletheneIC500.52 [1], 0.58 [2]
10-[2-(Hydroxymethyl)-3-[1-methyl-6-oxo-5-(pyrimidin-4-ylamino)pyridin-3-yl]phenyl]-4,4-dimethyl-7-thia-10-azatricyclo[6.4.0.02,6]dodeca-1(8),2(6)-dien-9-oneIC5010.0 [1], 87.0 [2]
10-[2-(Hydroxymethyl)-3-[1-methyl-6-oxo-5-(pyrimidin-4-ylamino)pyridin-3-yl]phenyl]-4,4-dimethyl-7-thia-10-azatricyclo[6.4.0.02,6]dodeca-1(8),2(6)-dien-9-oneKi1.28 [1]
2-[2-(Hydroxymethyl)-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]-3,4,6,7,8,9-hexahydropyrazino[1,2-a]indol-1-oneIC504.0 [1], 5.0 [2], 45.0 [3]
10-[2-(Hydroxymethyl)-3-[1-methyl-5-[[5-[4-(oxetan-3-yl)piperazin-1-yl]pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]-4,4-dimethyl-7-thia-10-azatricyclo[6.4.0.02,6]dodeca-1(8),2(6)-dien-9-oneIC504.0 [1], 43.0 [2], 89.0 [3]
8-Cyclopropyl-6-fluoro-4-[2-(hydroxymethyl)-3-[2-[1-(oxetan-3-yl)-3,6-dihydro-2H-pyridin-4-yl]-1H-pyrrolo[2,3-b]pyridin-4-yl]phenyl]-2,3-dihydro-1,4-benzoxazepin-5-oneIC503.1 [1], 22.0 [2], 261.0 [3]
3-Chloro-4-[3-(8-fluoro-2,4-dioxo-1H-quinazolin-3-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamideIC501.2 [1], 20.0 [2]
4-[3-(8-Fluoro-1-methyl-2,4-dioxoquinazolin-3-yl)-2-methylphenyl]-7-(2-hydroxypropan-2-yl)-9H-carbazole-1-carboxamideIC502.3 [1], 19.0 [2], 190.0 [3]
1-[3-[4-Amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]-2-chloroethanoneIC500.58 [1]
1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-oneIC50607.0 [1]
1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-oneKi62300.0 [1]
Bmx-IN-1IC5010.4 [1]
1-Cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amineIC508.2 [1]
5-[4-Amino-1-(2,3-dihydro-1H-inden-2-yl)pyrazolo[3,4-d]pyrimidin-3-yl]-2-bromophenolIC5012.0 [1]
6-(4-Prop-2-enoylpiperazin-1-yl)-2-[4-(2-pyrrolidin-1-ylethyl)anilino]pyridine-3-carboxamideIC500.3 [1], 4.3 [2]
2-[4-[4-Amino-3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-7-yl]pyrazol-1-yl]-N-methylacetamideIC5012.8 [1]
Chmfl-btk-01IC507.0 [1]
Chmfl-btk-01Ki8.9 [1]
6-Cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[6-[1-(morpholine-4-carbonyl)-3,6-dihydro-2H-pyridin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]phenyl]isoquinolin-1-oneIC504.8 [1], 17.0 [2]
4-[2-Methyl-3-(prop-2-enoylamino)phenyl]-1H-indole-7-carboxamideIC501.1 [1], 57.0 [2]
N-[3-[4-Amino-6-[4-(morpholine-4-carbonyl)anilino]-1,3,5-triazin-2-yl]-2-(hydroxymethyl)phenyl]-4-tert-butylbenzamideIC500.3 [1], 43.0 [2]
2-[3-[4-Amino-6-[(1-cyclopropylpyrazol-4-yl)amino]-1,3,5-triazin-2-yl]-2-(hydroxymethyl)phenyl]-6-cyclopropyl-8-fluoroisoquinolin-1-oneIC500.57 [1], 8.3 [2]
N-[3-[4-Amino-6-(4-morpholin-4-ylanilino)-1,3,5-triazin-2-yl]-2-(hydroxymethyl)phenyl]-4-propan-2-ylbenzamideIC502.5 [1], 82.0 [2]
2-[3-[4-Amino-6-(4-morpholin-4-ylanilino)-1,3,5-triazin-2-yl]-2-(hydroxymethyl)phenyl]-6-cyclopropyl-3,4-dihydroisoquinolin-1-oneIC504.2 [1], 350.0 [2]
N-[3-[4-Amino-6-(4-morpholin-4-ylanilino)-1,3,5-triazin-2-yl]-2-(hydroxymethyl)phenyl]-4-(dimethylamino)benzamideIC504.7 [1], 38.0 [2]
10-[3-[4-Amino-6-(4-morpholin-4-ylanilino)-1,3,5-triazin-2-yl]-2-(hydroxymethyl)phenyl]-4,4-dimethyl-1,10-diazatricyclo[6.4.0.02,6]dodeca-2(6),7-dien-9-oneIC500.62 [1], 42.0 [2]
2-[3-[4-Amino-6-(4-morpholin-4-ylanilino)-1,3,5-triazin-2-yl]-2-(hydroxymethyl)phenyl]-6-cyclopropylphthalazin-1-oneIC504.3 [1], 280.0 [2]
N-[3-[4-Amino-6-(4-morpholin-4-ylanilino)-1,3,5-triazin-2-yl]-2-(hydroxymethyl)phenyl]-5-tert-butylthiophene-2-carboxamideIC504.0 [1], 820.0 [2]
2-[2-[3-[4-Amino-6-(4-morpholin-4-ylanilino)-1,3,5-triazin-2-yl]-2-(hydroxymethyl)phenyl]-8-fluoro-1-oxo-3,4-dihydroisoquinolin-6-yl]-2-methylpropanenitrileIC501.6 [1], 110.0 [2]
2-[3-[4-Amino-6-(4-morpholin-4-ylanilino)-1,3,5-triazin-2-yl]-2-(hydroxymethyl)phenyl]-5-tert-butyl-3H-isoindol-1-oneIC503.8 [1], 640.0 [2]
N-[3-[4-Amino-6-(4-morpholin-4-ylanilino)-1,3,5-triazin-2-yl]-2-(hydroxymethyl)phenyl]-4,5,6,7-tetrahydro-1-benzothiophene-2-carboxamideIC500.81 [1], 28.0 [2]
4-Tert-butyl-N-[2-methyl-3-[4-methyl-6-[4-(morpholine-4-carbonyl)anilino]-1,3,5-triazin-2-yl]phenyl]benzamideIC5034.0 [1], 7800.0 [2]
N-[3-[4-Amino-6-(4-morpholin-4-ylanilino)-1,3,5-triazin-2-yl]-2-(hydroxymethyl)phenyl]-5-tert-butyl-1,3-thiazole-2-carboxamideIC5015.0 [1], 2500.0 [2]
4-Tert-butyl-N-[3-[4-methoxy-6-[4-(morpholine-4-carbonyl)anilino]-1,3,5-triazin-2-yl]-2-methylphenyl]benzamideIC5080.0 [1], 10000.0 [2]
N-[3-[4-Amino-6-(4-morpholin-4-ylanilino)-1,3,5-triazin-2-yl]-2-(hydroxymethyl)phenyl]-4-cyclopropylbenzamideIC502.1 [1], 140.0 [2]
4-[[4-Amino-6-[3-(6-cyclopropyl-8-fluoro-1-oxoisoquinolin-2-yl)-2-(hydroxymethyl)phenyl]-1,3,5-triazin-2-yl]amino]-1-ethylpyrrole-2-carbonitrileIC500.58 [1], 6.3 [2]
4-[[4-Amino-6-[3-(6-cyclopropyl-8-fluoro-1-oxoisoquinolin-2-yl)-2-(hydroxymethyl)phenyl]-1,3,5-triazin-2-yl]amino]-1-propan-2-ylpyrrole-2-carbonitrileIC500.53 [1], 5.4 [2]
2-[3-[4-Amino-6-[[1-(1-cyclopropylethyl)pyrazol-4-yl]amino]-1,3,5-triazin-2-yl]-2-(hydroxymethyl)phenyl]-6-cyclopropyl-8-fluoroisoquinolin-1-oneIC500.49 [1], 2.2 [2]
2-[3-[4-Amino-6-(1H-pyrazol-4-ylamino)-1,3,5-triazin-2-yl]-2-(hydroxymethyl)phenyl]-6-cyclopropyl-8-fluoroisoquinolin-1-oneIC500.51 [1], 9.3 [2]
8-Cyclopropyl-6-fluoro-4-[2-(hydroxymethyl)-3-[2-[1-[1-(oxetan-3-yl)piperidin-4-yl]pyrazol-4-yl]-1H-pyrrolo[2,3-b]pyridin-4-yl]phenyl]-2,3-dihydro-1,4-benzoxazepin-5-oneIC501.7 [1]
8-Cyclopropyl-6-fluoro-4-[2-(hydroxymethyl)-3-[2-[1-(2-hydroxy-2-methylpropyl)-3,6-dihydro-2H-pyridin-4-yl]-1H-pyrrolo[2,3-b]pyridin-4-yl]phenyl]-2,3-dihydro-1,4-benzoxazepin-5-oneIC501.4 [1]
2-[3-[6-Amino-2-[(1-methylpyrazol-4-yl)amino]pyrimidin-4-yl]-2-(hydroxymethyl)phenyl]-6-cyclopropyl-8-fluoroisoquinolin-1-oneIC500.4 [1], 3.7 [2]
4-[[4-Amino-6-[3-(6-cyclopropyl-8-fluoro-1-oxoisoquinolin-2-yl)-2-(hydroxymethyl)phenyl]pyrimidin-2-yl]amino]-1-methylpyrrole-2-carbonitrileIC501.7 [1], 20.2 [2]
6-[(7S)-7-(Prop-2-enoylamino)-5-azaspiro[2.4]heptan-5-yl]-2-[4-(2-pyrrolidin-1-ylethyl)anilino]pyridine-3-carboxamideIC500.09 [1], 4.9 [2]
6-[(3S)-3-(Prop-2-enoylamino)pyrrolidin-1-yl]-2-[4-(2-pyrrolidin-1-ylethyl)anilino]pyridine-3-carboxamideIC501.9 [1], 7.0 [2]
6-[(3S)-3-[Methyl(prop-2-enoyl)amino]pyrrolidin-1-yl]-2-[4-(2-pyrrolidin-1-ylethyl)anilino]pyridine-3-carboxamideIC501.3 [1], 41.0 [2]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Tyrosine-protein kinase BTK Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 20 Nov. 2024, https://www.aatbio.com/data-sets/tyrosine-protein-kinase-btk-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, November 20). Quest Database™ Tyrosine-protein kinase BTK Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/tyrosine-protein-kinase-btk-inhibitors-ic50-ki.
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