Literature summary for 2.7.10.2 extracted from

Hari, S.B.; Perera, B.G.; Ranjitkar, P.; Seeliger, M.A.; Maly, D.J.
Conformation-selective inhibitors reveal differences in the activation and phosphate-binding loops of the tyrosine kinases Abl and Src (2013), ACS Chem. Biol., 8, 2734-2743.

Inhibitors

Inhibitors	Comment	Organism
4-methyl-3-[[3-(pyrimidin-4-yl)pyridin-2-yl]amino]-N-[3-(trifluoromethyl)phenyl]benzamide	-	Homo sapiens
AST-487	-	Homo sapiens
iclusig	potent inhibitor of Abl	Homo sapiens
imatinib	-	Homo sapiens
N-(3-[2-[4-(2-acetamidoethoxy)anilino]quinazolin-6-yl]-4-methylphenyl)-3-(trifluoromethyl)benzamide	-	Homo sapiens
N-(4-methyl-3-[[3-(pyrimidin-4-yl)pyridin-2-yl]amino]phenyl)-3-(trifluoromethyl)benzamide	-	Homo sapiens
N-[3-([3-[4-(4-methoxyanilino)-1,3,5-triazin-2-yl]pyridin-2-yl]amino)-4-methylphenyl]-3-(trifluoromethyl)benzamide	-	Homo sapiens
N-[3-[2-(cyclopropylamino)quinazolin-6-yl]-4-methylphenyl]-3-(trifluoromethyl)benzamide	-	Homo sapiens
N-[4-methyl-3-([3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl]amino)phenyl]-3-(trifluoromethyl)benzamide	-	Homo sapiens
N-[4-methyl-3-([3-[6-(methylamino)pyrimidin-4-yl]pyridin-2-yl]amino)phenyl]-3-(trifluoromethyl)benzamide	-	Homo sapiens
N-[4-[4-amino-1-(propan-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]phenyl]-N'-[3-(trifluoromethyl)phenyl]urea	-	Homo sapiens
rebastinib	potent inhibitor of Abl	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
ATP + a [protein]-L-tyrosine	Homo sapiens	-	ADP + a [protein]-L-tyrosine phosphate	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + a [protein]-L-tyrosine	-	Homo sapiens	ADP + a [protein]-L-tyrosine phosphate	-	?

Synonyms

Synonyms	Comment	Organism
Abl	-	Homo sapiens
Src	-	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism
0.00000011	-	N-(3-[2-[4-(2-acetamidoethoxy)anilino]quinazolin-6-yl]-4-methylphenyl)-3-(trifluoromethyl)benzamide	non-receptor tyrosine kinase Src, pH and temperature not specified in the publication	Homo sapiens
0.00000012	-	N-[3-[2-(cyclopropylamino)quinazolin-6-yl]-4-methylphenyl]-3-(trifluoromethyl)benzamide	non-receptor tyrosine kinase Abl, pH and temperature not specified in the publication	Homo sapiens
0.00000013	-	iclusig	non-receptor tyrosine kinase Abl, pH and temperature not specified in the publication	Homo sapiens
0.00000018	-	N-(3-[2-[4-(2-acetamidoethoxy)anilino]quinazolin-6-yl]-4-methylphenyl)-3-(trifluoromethyl)benzamide	non-receptor tyrosine kinase Abl, pH and temperature not specified in the publication	Homo sapiens
0.00000022	-	N-[4-[4-amino-1-(propan-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]phenyl]-N'-[3-(trifluoromethyl)phenyl]urea	non-receptor tyrosine kinase Abl, pH and temperature not specified in the publication	Homo sapiens
0.00000028	-	N-(4-methyl-3-[[3-(pyrimidin-4-yl)pyridin-2-yl]amino]phenyl)-3-(trifluoromethyl)benzamide	non-receptor tyrosine kinase Abl, pH and temperature not specified in the publication	Homo sapiens
0.00000039	-	N-[4-methyl-3-([3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl]amino)phenyl]-3-(trifluoromethyl)benzamide	non-receptor tyrosine kinase Abl, pH and temperature not specified in the publication	Homo sapiens
0.00000042	-	rebastinib	non-receptor tyrosine kinase Abl, pH and temperature not specified in the publication	Homo sapiens
0.0000005	-	4-methyl-3-[[3-(pyrimidin-4-yl)pyridin-2-yl]amino]-N-[3-(trifluoromethyl)phenyl]benzamide	non-receptor tyrosine kinase Abl, pH and temperature not specified in the publication	Homo sapiens
0.00000068	-	N-[3-[2-(cyclopropylamino)quinazolin-6-yl]-4-methylphenyl]-3-(trifluoromethyl)benzamide	non-receptor tyrosine kinase Src, pH and temperature not specified in the publication	Homo sapiens
0.00000076	-	N-[3-([3-[4-(4-methoxyanilino)-1,3,5-triazin-2-yl]pyridin-2-yl]amino)-4-methylphenyl]-3-(trifluoromethyl)benzamide	non-receptor tyrosine kinase Abl, pH and temperature not specified in the publication	Homo sapiens
0.00000081	-	imatinib	non-receptor tyrosine kinase Abl, pH and temperature not specified in the publication	Homo sapiens
0.00000082	-	N-[4-[4-amino-1-(propan-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]phenyl]-N'-[3-(trifluoromethyl)phenyl]urea	non-receptor tyrosine kinase Src, pH and temperature not specified in the publication	Homo sapiens
0.000001	-	iclusig	non-receptor tyrosine kinase Src, pH and temperature not specified in the publication	Homo sapiens
0.0000016	-	N-[3-([3-[4-(4-methoxyanilino)-1,3,5-triazin-2-yl]pyridin-2-yl]amino)-4-methylphenyl]-3-(trifluoromethyl)benzamide	non-receptor tyrosine kinase Src, pH and temperature not specified in the publication	Homo sapiens
0.0000028	-	N-[4-methyl-3-([3-[6-(methylamino)pyrimidin-4-yl]pyridin-2-yl]amino)phenyl]-3-(trifluoromethyl)benzamide	non-receptor tyrosine kinase Abl, pH and temperature not specified in the publication	Homo sapiens
0.0000051	-	rebastinib	non-receptor tyrosine kinase Src, pH and temperature not specified in the publication	Homo sapiens
0.0000089	-	N-(4-methyl-3-[[3-(pyrimidin-4-yl)pyridin-2-yl]amino]phenyl)-3-(trifluoromethyl)benzamide	non-receptor tyrosine kinase Src, pH and temperature not specified in the publication	Homo sapiens
0.000019	-	N-[4-methyl-3-([3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl]amino)phenyl]-3-(trifluoromethyl)benzamide	non-receptor tyrosine kinase Src, pH and temperature not specified in the publication	Homo sapiens
0.000023	-	4-methyl-3-[[3-(pyrimidin-4-yl)pyridin-2-yl]amino]-N-[3-(trifluoromethyl)phenyl]benzamide	non-receptor tyrosine kinase Src, pH and temperature not specified in the publication	Homo sapiens
0.00053	-	N-[4-methyl-3-([3-[6-(methylamino)pyrimidin-4-yl]pyridin-2-yl]amino)phenyl]-3-(trifluoromethyl)benzamide	non-receptor tyrosine kinase Src, pH and temperature not specified in the publication	Homo sapiens
0.0033	-	imatinib	Ki above 0.0033 mM, non-receptor tyrosine kinase Src, pH and temperature not specified in the publication	Homo sapiens