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Tyrosine-protein kinase ABL Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
ImatinibIC50234.0 [1]
ImatinibKi13.0 [1], 37.0 [2], 7000.0 [3]
PonatinibIC501.08 [1]
DasatinibIC501.0 [1]
NilotinibIC5028.0 [1]
StaurosporineIC50105.9 [1]
BosutinibIC501.1 [1]
CID 51038269IC500.34 [1]
CID 71605047IC500.3 [1]
4-Methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-([1,2,4]triazolo[1,5-a]pyrimidin-6-yl)ethynyl]benzamideIC503.2 [1]
N-[4-[(4-Methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]benzamideIC500.46 [1]
4-Ethyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]benzamideIC501.92 [1]
4-Cyclopropyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]benzamideIC504.44 [1]
4-Chloro-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]benzamideIC500.77 [1]
4-Methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(3-methyl-2H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]benzamideIC500.63 [1]
3-[2-(3-Cyclopropyl-2H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamideIC500.93 [1]
4-Methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(3-phenyl-2H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]benzamideIC503.47 [1]
3-[2-(3-Methoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamideIC505.15 [1]
3-[2-(1H-Indazol-5-yl)ethynyl]-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamideIC5029.1 [1]
4-Methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1-methylpyrazolo[3,4-b]pyridin-5-yl)ethynyl]benzamideIC501.08 [1]
1-[5-(2-Imidazo[1,2-a]pyrazin-5-ylethynyl)-1-methylpyrazol-3-yl]-3-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]ureaIC501.6 [1]
1-[5-(2-Imidazo[1,2-a]pyrazin-3-ylethynyl)-1-methylpyrazol-3-yl]-3-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]ureaIC500.5 [1]
1-[5-(2-Imidazo[1,2-b]pyridazin-3-ylethynyl)-1-methylpyrazol-3-yl]-3-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]ureaIC500.4 [1]
CID 11478363IC5061.0 [1]
Bcr-abl Inhibitor IIKi120.0 [1]
1-(2-Chloro-2-phenylethyl)-N-[(3-fluorophenyl)methyl]pyrazolo[3,4-d]pyrimidin-4-amineKi40.0 [1], 16700.0 [2]
3-[(E)-2-[6-(Cyclopropylamino)purin-9-yl]ethenyl]-4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]benzamideIC5025.0 [1], 400.0 [2], 478.0 [3], 25000.0 [4]
1-[2-Chloro-2-(4-fluorophenyl)ethyl]-N-(3-fluorophenyl)pyrazolo[3,4-d]pyrimidin-4-amineKi700.0 [1], 732.0 [2], 750.0 [3], 2430.0 [4], 3000.0 [5]
N-[3-(7-Anilino-1-methyl-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl)-4-methylphenyl]-3-(trifluoromethyl)benzamideIC505.0 [1], 130.0 [2], 135.0 [3], 206.0 [4]
SunitinibIC50410.0 [1], 504.0 [2], 1613.0 [3], 50000.0 [4]
AxitinibIC500.42 [1], 0.55 [2], 2.6 [3], 7.78 [4]
N-Benzyl-1-(2-chloro-2-phenylethyl)-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidin-4-amineKi260.0 [1], 300.0 [2]
7-(2,6-Dichlorophenyl)-5-methyl-N-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-1,2,4-benzotriazin-3-amineKi19.4 [1], 20.0 [2], 10300.0 [3]
N-Benzyl-1-(2-chloro-2-phenylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amineKi370.0 [1], 400.0 [2]
N-[3-(7-Amino-1-methyl-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl)-4-methylphenyl]-3-(trifluoromethyl)benzamideIC505.0 [1], 1567.0 [2]
7-(2,6-Dimethylphenyl)-5-methyl-N-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-1,2,4-benzotriazin-3-amineIC5020.0 [1], 5990.0 [2]
7-(2,6-Dimethylphenyl)-5-methyl-N-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-1,2,4-benzotriazin-3-amineKi11.0 [1], 4240.0 [2]
1-[2-Chloro-2-(4-chlorophenyl)ethyl]-N-(4-fluorobenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amineKi80.0 [1], 160.0 [2]
6-Bromo-3-[(3E)-3-[2-[4-(2-methoxyethyl)piperazin-1-yl]ethoxyimino]indol-2-yl]-1H-indol-2-olIC50468.0 [1], 3440.0 [2], 10000.0 [3]
3-(2-Imidazo[1,2-a]pyridin-3-ylethynyl)-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamideIC501.4 [1], 1.6 [2], 9.0 [3], 56.0 [4]
3-[(E)-2-[6-(Cyclopropylamino)purin-9-yl]ethenyl]-4-methyl-N-[4-(trifluoromethyl)pyridin-2-yl]benzamideIC5020.0 [1], 14142.0 [2], 14412.0 [3], 20000.0 [4]
3-[(E)-2-[6-(Cyclopropylamino)purin-9-yl]ethenyl]-N-[3-imidazol-1-yl-5-(trifluoromethyl)phenyl]-4-methylbenzamideIC5013.0 [1], 542.0 [2], 13000.0 [3]
3-(4-Methylimidazol-1-yl)-N-[4-methyl-3-[1-methyl-7-(methylamino)-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]-5-(trifluoromethyl)benzamideIC505.0 [1], 720.0 [2]
CID 46864270IC500.2 [1], 0.4 [2], 17.2 [3], 60.2 [4]
N-[4-[Chloro(difluoro)methoxy]phenyl]-6-[(3S,4S)-3,4-dihydroxypyrrolidin-1-yl]-5-pyrimidin-5-ylpyridine-3-carboxamideIC500.13 [1], 0.5 [2], 1.0 [3], 213.0 [4]
Methyl 5-[[2-methyl-5-[[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)benzoyl]amino]phenyl]methylamino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylateIC506.0 [1], 46.0 [2], 51.0 [3], 73.0 [4]
6-[(3R)-3-Hydroxypyrrolidin-1-yl]-5-pyrimidin-5-yl-N-[4-(trifluoromethoxy)phenyl]pyridine-3-carboxamideIC501.2 [1], 3.0 [2], 4.0 [3], 88.0 [4]
N-[4-[Chloro(difluoro)methoxy]phenyl]-6-[(3R)-3-hydroxypyrrolidin-1-yl]-5-pyrimidin-5-ylpyridine-3-carboxamideIC500.13 [1], 0.3 [2], 3.0 [3], 13.0 [4]
6-[(3R)-3-Hydroxypyrrolidin-1-yl]-5-pyrimidin-5-yl-N-[4-(trifluoromethylsulfanyl)phenyl]pyridine-3-carboxamideIC500.2 [1], 0.4 [2], 5.0 [3], 19.0 [4]
CrizotinibIC5024.0 [1], 1000.0 [2], 1159.0 [3]
SeliciclibIC5010000.0 [1], 100000.0 [2]
SaracatinibIC5030.0 [1]
DanusertibIC505.0 [1], 7.94 [2], 25.0 [3]
1-Cyclopropyl-3-(3-(5-(morpholinomethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazol-4-yl)ureaIC504.0 [1], 10.0 [2]
3-(6-((4-(Trifluoromethoxy)phenyl)amino)pyrimidin-4-yl)benzamideIC509.0 [1], 2800.0 [2], 10000.0 [3]
1-(2-Chloro-2-phenylethyl)-6-(methylthio)-N-phenethyl-1H-pyrazolo[3,4-d]pyrimidin-4-amineKi7030.0 [1], 7300.0 [2]
1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amineIC502.0 [1], 18.0 [2]
Gnf-5IC5017.0 [1], 2000.0 [2], 10000.0 [3]
1-(2-Chloro-2-phenylethyl)-N-(3-chlorophenyl)-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidin-4-amineKi600.0 [1]
N-(3-Chlorophenyl)-1-(2-chloro-2-phenylethyl)-6-(2-morpholin-4-ylethylsulfanyl)pyrazolo[3,4-d]pyrimidin-4-amineKi120.0 [1], 180.0 [2]
1-(2-Chloro-2-phenylethyl)-6-(2-morpholin-4-ylethylsulfanyl)-N-phenylpyrazolo[3,4-d]pyrimidin-4-amineKi150.0 [1], 220.0 [2]
N-(3-Bromophenyl)-6-methylsulfanyl-1-(2-phenylpropyl)pyrazolo[3,4-d]pyrimidin-4-amineKi1070.0 [1]
N-[3-[2-(4-Amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)ethynyl]phenyl]-3-(trifluoromethyl)benzamideIC500.6 [1], 0.8 [2]
1-[2-Chloro-2-(4-fluorophenyl)ethyl]-N-[(3-fluorophenyl)methyl]pyrazolo[3,4-d]pyrimidin-4-amineKi100.0 [1], 23600.0 [2]
1-(1-Methylethyl)-3-Quinolin-6-Yl-1h-Pyrazolo[3,4-D]pyrimidin-4-AmineIC5042.0 [1], 140.0 [2]
1-Cyclobutyl-3-(3,4-dimethoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amineIC50170.0 [1], 340.0 [2]
1-[2-(4-Bromophenyl)-2-chloroethyl]-N-phenylpyrazolo[3,4-d]pyrimidin-4-amineKi90.0 [1], 610.0 [2]
6-[(3S)-3-Hydroxypyrrolidin-1-yl]-5-pyrimidin-5-yl-N-[4-(trifluoromethoxy)phenyl]pyridine-3-carboxamideIC502.3 [1], 4.8 [2], 9.0 [3]
3-Pyrimidin-5-yl-N-[4-(trifluoromethoxy)phenyl]benzamideIC503.4 [1], 5.6 [2], 18.0 [3]
6-[(3R)-3-Hydroxy-3-methylpyrrolidin-1-yl]-5-(1H-pyrazol-5-yl)-N-[4-(trifluoromethoxy)phenyl]pyridine-3-carboxamideIC501.6 [1], 2.5 [2], 2.8 [3]
N-[4-[Chloro(difluoro)methoxy]phenyl]-5-(5-fluoropyridin-3-yl)-6-[(3R)-3-hydroxypyrrolidin-1-yl]pyridine-3-carboxamideIC500.13 [1], 4.0 [2], 12.0 [3]
5-(5-Fluoropyridin-3-yl)-6-[(3R)-3-hydroxypyrrolidin-1-yl]-N-[4-(trifluoromethylsulfinyl)phenyl]pyridine-3-carboxamideIC5011.0 [1], 15.0 [2], 580.0 [3]
6-[(3R)-3-Hydroxypyrrolidin-1-yl]-N-[4-(1,1,2,2,2-pentafluoroethyl)phenyl]-5-pyrimidin-5-ylpyridine-3-carboxamideIC500.6 [1], 3.0 [2], 130.0 [3]
N-[4-[Chloro(difluoro)methoxy]phenyl]-5-(5-cyanopyridin-3-yl)-6-[2-hydroxyethyl(methyl)amino]pyridine-3-carboxamideIC500.2 [1], 4.0 [2], 38.0 [3]
5-(5-Fluoropyridin-3-yl)-6-[(3R)-3-hydroxypyrrolidin-1-yl]-N-[4-(1,1,2,2-tetrafluoroethoxy)phenyl]pyridine-3-carboxamideIC507.0 [1], 11.0 [2], 442.0 [3]
N-[4-[Chloro(difluoro)methyl]sulfanylphenyl]-5-(5-fluoropyridin-3-yl)-6-[(3R)-3-hydroxypyrrolidin-1-yl]pyridine-3-carboxamideIC500.6 [1], 3.0 [2], 10.0 [3]
N-[4-(2-Chloro-1,1,2,2-tetrafluoroethyl)phenyl]-6-[(3R)-3-hydroxypyrrolidin-1-yl]-5-pyrimidin-5-ylpyridine-3-carboxamideIC500.5 [1], 1.0 [2], 24.0 [3]
5-(5-Fluoropyridin-3-yl)-6-[(3R)-3-hydroxypyrrolidin-1-yl]-N-[4-(trifluoromethylsulfanyl)phenyl]pyridine-3-carboxamideIC500.2 [1], 4.0 [2], 24.0 [3]
N-[3-Fluoro-4-(trifluoromethoxy)phenyl]-6-[(3S)-3-(hydroxymethyl)pyrrolidin-1-yl]-5-pyrimidin-5-ylpyridine-3-carboxamideIC501.9 [1], 4.0 [2], 273.0 [3]
N-[4-[Chloro(difluoro)methoxy]phenyl]-5-(5-cyanopyridin-3-yl)-6-[(3R,4S)-3,4-dihydroxypyrrolidin-1-yl]pyridine-3-carboxamideIC500.4 [1], 0.5 [2], 93.0 [3]
N-[4-[Chloro(difluoro)methoxy]phenyl]-6-[(3R,4S)-3-hydroxy-4-(hydroxymethyl)piperidin-1-yl]-5-pyrimidin-5-ylpyridine-3-carboxamideIC500.6 [1], 3.0 [2], 38.0 [3]
6-(3-Hydroxy-3-methylazetidin-1-yl)-5-(2-methylpyrimidin-5-yl)-N-[4-(trifluoromethoxy)phenyl]pyridine-3-carboxamideIC505.4 [1], 8.0 [2], 513.0 [3]
6-[(3R)-3-(Aminomethyl)pyrrolidin-1-yl]-5-pyrimidin-5-yl-N-[4-(trifluoromethoxy)phenyl]pyridine-3-carboxamideIC500.6 [1], 3.0 [2], 800.0 [3]
N-[4-(1,1-Difluoroethoxy)phenyl]-6-[(3R)-3-hydroxypyrrolidin-1-yl]-5-pyrimidin-5-ylpyridine-3-carboxamideIC501.2 [1], 7.9 [2], 554.0 [3]
4-[(3S,4S)-3-Amino-4-hydroxypyrrolidin-1-yl]-N-[4-[chloro(difluoro)methoxy]phenyl]-3-(5-fluoropyridin-3-yl)benzamideIC500.6 [1], 1.0 [2], 165.0 [3]
N-[4-[Chloro(difluoro)methoxy]phenyl]-6-[(3S,4R)-3,4-dihydroxypyrrolidin-1-yl]-5-pyrimidin-5-ylpyridine-3-carboxamideIC500.7 [1], 1.0 [2], 130.0 [3]
GenisteinIC5010000.0 [1]
SorafenibIC5080.0 [1], 120.0 [2]
MebendazoleIC505000.0 [1]
MebendazoleKi4600.0 [1]
IbrutinibIC5086.1 [1]
VandetanibIC5086.0 [1], 151.0 [2]
SemaxanibIC5010000.0 [1], 11000.0 [2]
TozasertibKi30.0 [1], 42.0 [2]
DovitinibIC50228.0 [1], 450.0 [2]
2-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-olIC50410.0 [1], 3600.0 [2]
(E)-N-(5-Methyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-styrylpyrimidin-4-amineIC5081.0 [1], 295.0 [2]
PDGF Receptor Tyrosine Kinase Inhibitor IVIC5022.0 [1]
1-Tert-butyl-3-(naphthalen-1-ylmethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amineIC50120.0 [1], 3400.0 [2]
3-(1H-Indol-5-yl)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrrolo[2,3-b]pyridineIC503.0 [1], 6.8 [2]



References

This online tool may be cited as follows

MLA

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

APA

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