Target
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1
Ligand
BDBM6732
Substrate
ING Peptide
Meas. Tech.
CDK Kinase Inhibition Assay
pH
7±n/a
Temperature
295.15±n/a K
IC50
160±n/a nM
Citation
 Al-awar, RSRay, JEHecker, KAHuang, JWaid, PPShih, CBrooks, HBSpencer, CDWatkins, SAPatel, BRStamm, NBOgg, CASchultz, RMConsidine, ELFaul, MMSullivan, KAKolis, SPGrutsch, JLJoseph, S 1,7-annulated indolocarbazoles as cyclin-dependent kinase inhibitors. Bioorg Med Chem Lett 14:3217-20 (2004) [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:
BDBM6732
Synonyms:
1,7-Annulated indolocarbazole deriv. 6o | 7-(pyridin-3-yl)-1,4,14-triazaheptacyclo[16.7.1.0^{2,17}.0^{3,11}.0^{5,10}.0^{12,16}.0^{22,26}]hexacosa-2(17),3(11),5(10),6,8,12(16),18(26),19,21-nonaene-13,15-dione
Type:
Small organic molecule
Emp. Form.:
C28H18N4O2
Mol. Mass.:
442.4681
SMILES:
O=C1NC(=O)c2c1c1c3ccc(cc3[nH]c1c1n3CCCc4cccc(c34)c21)-c1cccnc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
ING Peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1341.50
Organism:
n/a
Description:
amino acid residues 246-257 from human retinoblastoma 1 protein.
Residue:
12
Sequence:
INGSPRTPRRGQ