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TargetCyclin-dependent kinase 6/G1/S-specific cyclin-D1
LigandBDBM50347388
Substrate/Competitorn/a
Meas. Tech.ChEMBL_755647 (CHEMBL1805472)
IC50 35500±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 Chem53:8508-22 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Cyclin-dependent kinase 6/G1/S-specific cyclin-D1
Name:Cyclin-dependent kinase 6/G1/S-specific cyclin-D1
Synonyms:CDK6/cyclin D1 | Cyclin-dependent kinase 6/G1/S-specific cyclin D1
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of ChEMBL is 1935149
Components:This complex has 2 components.
Component 1
Name:G1/S-specific cyclin-D1
Synonyms:B-cell lymphoma 1 protein | BCL-1 | BCL-1 oncogene | BCL1 | CCND1 | CCND1_HUMAN | PRAD1 | 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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Component 2
Name:Cyclin-dependent kinase 6
Synonyms:CDK6 | CDK6_HUMAN | CDKN6 | Cell division protein kinase 6 | Cyclin-dependent kinase 6 (CDK 6) | Serine/threonine-protein kinase PLSTIRE
Type:Enzyme Subunit
Mol. Mass.:36937.42
Organism:Homo sapiens (Human)
Description:Q00534
Residue:326
Sequence:
MEKDGLCRADQQYECVAEIGEGAYGKVFKARDLKNGGRFVALKRVRVQTGEEGMPLSTIR
EVAVLRHLETFEHPNVVRLFDVCTVSRTDRETKLTLVFEHVDQDLTTYLDKVPEPGVPTE
TIKDMMFQLLRGLDFLHSHRVVHRDLKPQNILVTSSGQIKLADFGLARIYSFQMALTSVV
VTLWYRAPEVLLQSSYATPVDLWSVGCIFAEMFRRKPLFRGSSDVDQLGKILDVIGLPGE
EDWPRDVALPRQAFHSKSAQPIEKFVTDIDELGKDLLLKCLTFNPAKRISAYSALSHPYF
QDLERCKENLDSHLPPSQNTSELNTA
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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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