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Target
Cyclin-dependent kinase 6/G1/S-specific cyclin-D1
Ligand
BDBM50347388
Substrate
n/a
Meas. Tech.
ChEMBL_755647 (CHEMBL1805472)
IC50
35500±n/a nM
Citation
 Heathcote, DA; Patel, H; Kroll, SH; Hazel, P; Periyasamy, M; Alikian, M; Kanneganti, SK; Jogalekar, AS; Scheiper, B; Barbazanges, M; Blum, A; Brackow, J; Siwicka, A; Pace, RD; Fuchter, MJ; Snyder, JP; Liotta, DC; Freemont, PS; Aboagye, EO; Coombes, RC; Barrett, AG; Ali, 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 
Target
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:
MEHQLLCCEVETIRRAYPDANLLNDRVLRAMLKAEETCAPSVSYFKCVQKEVLPSMRKIVATWMLEVCEEQKCEEEVFPLAMNYLDRFLSLEPVKKSRLQLLGATCMFVASKMKETIPLTAEKLCIYTDNSIRPEELLQMELLLVNKLKWNLAAMTPHDFIEHFLSKMPEAEENKQIIRKHAQTFVALCATDVKFISNPPSMVAAGSVVAAVQGLNLRSPNNFLSYYRLTRFLSRVIKCDPDCLRACQEQIEALLESSLRQAQQNMDPKAAEEEEEEEEEVDLACTPTDVRDVDI
  
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:
MEKDGLCRADQQYECVAEIGEGAYGKVFKARDLKNGGRFVALKRVRVQTGEEGMPLSTIREVAVLRHLETFEHPNVVRLFDVCTVSRTDRETKLTLVFEHVDQDLTTYLDKVPEPGVPTETIKDMMFQLLRGLDFLHSHRVVHRDLKPQNILVTSSGQIKLADFGLARIYSFQMALTSVVVTLWYRAPEVLLQSSYATPVDLWSVGCIFAEMFRRKPLFRGSSDVDQLGKILDVIGLPGEEDWPRDVALPRQAFHSKSAQPIEKFVTDIDELGKDLLLKCLTFNPAKRISAYSALSHPYFQDLERCKENLDSHLPPSQNTSELNTA
  
Inhibitor
Name:
BDBM50347388
Synonyms:
CHEMBL1234833
Type:
Small organic molecule
Emp. Form.:
C20H27N5O3
Mol. Mass.:
385.4601
SMILES:
CC(C)c1cnn2c(NCc3ccccc3)cc(N[C@@H](CO)[C@H](O)CO)nc12 |r|
Structure:
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