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TargetCyclin-Dependent Kinase 4 (CDK4)
LigandBDBM50347388
Substrate/Competitorn/a
Meas. Tech.ChEMBL_755645
IC50 20000±n/a nM
Citation Heathcote DAPatel HKroll SHHazel PPeriyasamy MAlikian MKanneganti SKJogalekar ASScheiper BBarbazanges MBlum ABrackow JSiwicka APace RDFuchter MJSnyder JPLiotta DCFreemont PSAboagye EOCoombes RCBarrett AGAli S A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. J Med Chem 53:8508-22 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Cyclin-Dependent Kinase 4 (CDK4)
Name:Cyclin-Dependent Kinase 4 (CDK4)
Synonyms:CDK4/CycD | CDK4/CycD1 | CDK4/Cyclin D1 | CDK4/D1 | Cyclin-dependent kinase 4/G1/S-specific cyclin D1 | Cyclin-dependent kinase 4/cyclin D1
Type:Protein Complex
Mol. Mass.:n/a
Description:CDK4/D1 complexes were purified from insect cells co-infected with baculovirus vectors containing each of the components.
Components:This complex has 2 components.
Component 1
Name:CDK4/CDK9
Synonyms:CDK4 | Cell division protein kinase 4 | Cyclin-dependent kinase 4 (CDK 4) | PSK-J3
Type:Enzyme Subunit
Mol. Mass.:33731.96
Organism:Homo sapiens (Human)
Description:P11802
Residue:303
Sequence:
MATSRYEPVAEIGVGAYGTVYKARDPHSGHFVALKSVRVPNGGGGGGGLPISTVREVALL
RRLEAFEHPNVVRLMDVCATSRTDREIKVTLVFEHVDQDLRTYLDKAPPPGLPAETIKDL
MRQFLRGLDFLHANCIVHRDLKPENILVTSGGTVKLADFGLARIYSYQMALTPVVVTLWY
RAPEVLLQSTYATPVDMWSVGCIFAEMFRRKPLFCGNSEADQLGKIFDLIGLPPEDDWPR
DVSLPRGAFPPRGPRPVQSVVPEMEESGAQLLLEMLTFNPHKRISAFRALQHSYLHKDEG
NPE
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Component 2
Name:G1/S-specific cyclin-D1
Synonyms:B-cell lymphoma 1 protein | BCL-1 | BCL-1 oncogene | CCND1 | PRAD1 oncogene
Type:Enzyme Subunit
Mol. Mass.:33717.70
Organism:Homo sapiens (Human)
Description:n/a
Residue:295
Sequence:
MEHQLLCCEVETIRRAYPDANLLNDRVLRAMLKAEETCAPSVSYFKCVQKEVLPSMRKIV
ATWMLEVCEEQKCEEEVFPLAMNYLDRFLSLEPVKKSRLQLLGATCMFVASKMKETIPLT
AEKLCIYTDNSIRPEELLQMELLLVNKLKWNLAAMTPHDFIEHFLSKMPEAEENKQIIRK
HAQTFVALCATDVKFISNPPSMVAAGSVVAAVQGLNLRSPNNFLSYYRLTRFLSRVIKCD
PDCLRACQEQIEALLESSLRQAQQNMDPKAAEEEEEEEEEVDLACTPTDVRDVDI
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BDBM50347388
n/a
NameBDBM50347388
Synonyms:CHEMBL1234833
TypeSmall organic molecule
Emp. Form.C20H27N5O3
Mol. Mass.385.4601
SMILESCC(C)c1cnn2c(NCc3ccccc3)cc(N[C@@H](CO)[C@H](O)CO)nc12 |r|
Structure
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