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Target
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1
Ligand
BDBM50188069
Substrate
n/a
Meas. Tech.
ChEMBL_378541 (CHEMBL871040)
IC50
410±n/a nM
Citation
 Mahale, S; Aubry, C; James Wilson, A; Jenkins, PR; Maréchal, JD; Sutcliffe, MJ; Chaudhuri, B CA224, a non-planar analogue of fascaplysin, inhibits Cdk4 but not Cdk2 and arrests cells at G0/G1 inhibiting pRB phosphorylation. Bioorg Med Chem Lett 16:4272-8 (2006) [PubMed]  Article 
Target
Name:
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1
Synonyms:
CDK4/CycD | CDK4/CycD1 | CDK4/Cyclin D1 | CDK4/D1 | Cyclin-Dependent Kinase 4 (CDK4) | Cyclin-dependent kinase 4 | 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:
Cyclin-dependent kinase 4
Synonyms:
CDK4 | CDK4_HUMAN | 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:
MATSRYEPVAEIGVGAYGTVYKARDPHSGHFVALKSVRVPNGGGGGGGLPISTVREVALLRRLEAFEHPNVVRLMDVCATSRTDREIKVTLVFEHVDQDLRTYLDKAPPPGLPAETIKDLMRQFLRGLDFLHANCIVHRDLKPENILVTSGGTVKLADFGLARIYSYQMALTPVVVTLWYRAPEVLLQSTYATPVDMWSVGCIFAEMFRRKPLFCGNSEADQLGKIFDLIGLPPEDDWPRDVSLPRGAFPPRGPRPVQSVVPEMEESGAQLLLEMLTFNPHKRISAFRALQHSYLHKDEGNPE
  
Component 2
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
  
Inhibitor
Name:
BDBM50188069
Synonyms:
12-oxo-10,12-dihydro-10-aza-4b-azonia-indeno[2,1-b]fluorene chloride | CHEMBL211632
Type:
Small organic molecule
Emp. Form.:
C18H11N2O
Mol. Mass.:
271.2922
SMILES:
O=C1c2ccccc2-n2cc3c(cc12)[nH+]c1ccccc31
Structure:
Search PDB for entries with ligand similarity: