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Target
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1
Ligand
BDBM6754
Substrate
Rb(21)
Meas. Tech.
CDK Kinase Inhibition Assay
pH
7±n/a
Temperature
295.15±n/a K
IC50
84±n/a nM
Citation
 Zhu, G; Conner, SE; Zhou, X; Chan, HK; Shih, C; Engler, TA; Al-Awar, RS; Brooks, HB; Watkins, SA; Spencer, CD; Schultz, RM; Dempsey, JA; Considine, EL; Patel, BR; Ogg, CA; Vasudevan, V; Lytle, ML Synthesis of 1,7-annulated indoles and their applications in the studies of cyclin dependent kinase inhibitors. Bioorg Med Chem Lett 14:3057-61 (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:
BDBM6754
Synonyms:
1,7-Annulated indolocarbazole deriv. 13Bg | 24-(hydroxymethyl)-9-methyl-1,9,14-triazaheptacyclo[16.7.1.0^{2,17}.0^{3,11}.0^{6,10}.0^{12,16}.0^{22,26}]hexacosa-2(17),3(11),4,6(10),7,12(16),18(26),19,21-nonaene-13,15-dione
Type:
Small organic molecule
Emp. Form.:
C25H19N3O3
Mol. Mass.:
409.4367
SMILES:
Cn1ccc2ccc3c4n5CC(CO)Cc6cccc(c4c4C(=O)NC(=O)c4c3c12)c56
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Rb(21)
Synonyms:
C-terminal retinoblastoma protein | RB1 | RB_HUMAN
Type:
Other Protein Type
Mol. Mass.:
17129.60
Organism:
Homo sapiens (Human)
Description:
Amino acids 769-921 of human retinoblastoma 1.
Residue:
153
Sequence:
LQYASTRPPTLSPIPHIPRSPYKFPSSPLRIPGGNIYISPLKSPYKISEGLPTPTKMTPRSRILVSIGESFGTSEKFQKINQMVCNSDRVLKRSAEGSNPPKPLKKLRFDIEGSDEADGSKHLPGESKFQQKLAEMTSTRTRMQKQKMNDSMD