Literature summary for 2.7.11.22 extracted from

Finlay, M.R.; Acton, D.G.; Andrews, D.M.; Barker, A.J.; Dennis, M.; Fisher, E.; Graham, M.A.; Green, C.P.; Heaton, D.W.; Karoutchi, G.; Loddick, S.A.; Morgentin, R.; Roberts, A.; Tucker, J.A.; Weir, H.M.
Imidazole piperazines: SAR and development of a potent class of cyclin-dependent kinase inhibitors with a novel binding mode (2008), Bioorg. Med. Chem. Lett., 18, 4442-4446.

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Inhibitors

Inhibitors	Comment	Organism	Structure
1-[4-[(5-fluoro-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]-N,N-dimethyl-L-prolinamide	-	Homo sapiens
2-[(4-[4-[(5-fluoro-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]piperazin-1-yl)sulfonyl]-2-oxoethanol	-	Homo sapiens
2-[(4-[4-[(6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]piperazin-1-yl)sulfonyl]-1-(methylsulfanyl)-2-oxoethanol	-	Homo sapiens
2-[(4-[4-[(6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]piperazin-1-yl)sulfonyl]-2-oxoethanol	-	Homo sapiens
5-fluoro-6,8-dimethyl-N-(4-morpholin-4-ylphenyl)-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine	-	Homo sapiens
6,8-dimethyl-N-(4-morpholin-4-ylphenyl)-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine	-	Homo sapiens
6,8-dimethyl-N-[4-[4-(methylsulfonyl)piperazin-1-yl]phenyl]-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine	-	Homo sapiens
N-(1-[4-[(5-fluoro-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]azetidin-3-yl)acetamide	-	Homo sapiens
N-(4-[4-[(2-methoxyethyl)sulfonyl]piperazin-1-yl]phenyl)-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine	-	Homo sapiens
N-[(3R)-1-[4-[(5-fluoro-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]pyrrolidin-3-yl]acetamide	-	Homo sapiens
N-[4-(4-[[(diethylamino)acetyl]sulfonyl]piperazin-1-yl)phenyl]-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine	-	Homo sapiens
N-[4-(4-[[(dimethylamino)acetyl]sulfonyl]piperazin-1-yl)phenyl]-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine	-	Homo sapiens
N-[4-(4-[[2-(dimethylamino)ethyl]sulfonyl]piperazin-1-yl)phenyl]-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P24941	-	-

Synonyms

Synonyms	Comment	Organism
CDK2	-	Homo sapiens

Cofactor

Cofactor	Comment	Organism	Structure
cyclin E	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0000003	-	with isozyme CDK2, IC50 above 0.0000003 mM	Homo sapiens	N-[(3R)-1-[4-[(5-fluoro-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]pyrrolidin-3-yl]acetamide
0.0000005	-	with isozyme CDK2	Homo sapiens	N-(1-[4-[(5-fluoro-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]azetidin-3-yl)acetamide
0.000003	-	with isozyme CDK2	Homo sapiens	N-[4-(4-[[2-(dimethylamino)ethyl]sulfonyl]piperazin-1-yl)phenyl]-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
0.000003	-	with isozyme CDK2, IC50 less than 0.000003 mM	Homo sapiens	N-(4-[4-[(2-methoxyethyl)sulfonyl]piperazin-1-yl]phenyl)-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
0.000003	-	with isozyme CDK2, IC50 less than 0.000003 mM	Homo sapiens	6,8-dimethyl-N-[4-[4-(methylsulfonyl)piperazin-1-yl]phenyl]-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
0.000006	-	with isozyme CDK2	Homo sapiens	2-[(4-[4-[(5-fluoro-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]piperazin-1-yl)sulfonyl]-2-oxoethanol
0.000008	-	with isozyme CDK2	Homo sapiens	5-fluoro-6,8-dimethyl-N-(4-morpholin-4-ylphenyl)-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
0.000009	-	with isozyme CDK2	Homo sapiens	6,8-dimethyl-N-(4-morpholin-4-ylphenyl)-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
0.000016	-	with isozyme CDK2	Homo sapiens	N-[4-(4-[[(dimethylamino)acetyl]sulfonyl]piperazin-1-yl)phenyl]-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
0.000017	-	with isozyme CDK2	Homo sapiens	2-[(4-[4-[(6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]piperazin-1-yl)sulfonyl]-2-oxoethanol
0.000017	-	with isozyme CDK2	Homo sapiens	2-[(4-[4-[(6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]piperazin-1-yl)sulfonyl]-1-(methylsulfanyl)-2-oxoethanol
0.000046	-	with isozyme CDK2	Homo sapiens	1-[4-[(5-fluoro-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]-N,N-dimethyl-L-prolinamide

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Release 2023.1 (January 2023)