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Target
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1
Ligand
BDBM6857
Substrate
Rb(21)
Meas. Tech.
Kinase Inhibition Assay
pH
7.0000±n/a
Temperature
295.1500±n/a K
IC50
630±n/a nM
Citation
 Zhu, G; Conner, SE; Zhou, X; Shih, C; Li, T; Anderson, BD; Brooks, HB; Campbell, RM; Considine, E; Dempsey, JA; Faul, MM; Ogg, C; Patel, B; Schultz, RM; Spencer, CD; Teicher, B; Watkins, SA Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. J Med Chem 46:2027-30 (2003) [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 | Cyclin-Dependent Kinase 4 (CDK4) | Cyclin-dependent kinase 4/cyclin D1 | Cyclin-dependent kinase 4/G1/S-specific 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:
Cell division protein kinase 4 | Cyclin-dependent kinase 4 (CDK 4) | PSK-J3 | CDK4_HUMAN | CDK4
Type:
Enzyme Subunit
Mol. Mass.:
33731.96
Organism:
Human
Description:
P11802
Residue:
303
Sequence:
MATSRYEPVAEIGVGAYGTVYKARDPHSGHFVALKSVRVPNGGGGGGGLPISTVREVALLRRLEAFEHPNVVRLMDVCATSRTDREIKVTLVFEHVDQDLRTYLDKAPPPGLPAETIKDLMRQFLRGLDFLHANCIVHRDLKPENILVTSGGTVKLADFGLARIYSYQMALTPVVVTLWYRAPEVLLQSTYATPVDMWSVGCIFAEMFRRKPLFCGNSEADQLGKIFDLIGLPPEDDWPRDVSLPRGAFPPRGPRPVQSVVPEMEESGAQLLLEMLTFNPHKRISAFRALQHSYLHKDEGNPE
  
Component 2
Name:
G1/S-specific cyclin-D1
Synonyms:
B-cell lymphoma 1 protein | BCL-1 oncogene | BCL-1 | PRAD1 oncogene | CCND1_HUMAN | CCND1 | BCL1 | PRAD1
Type:
Enzyme Subunit
Mol. Mass.:
33717.70
Organism:
Human
Description:
n/a
Residue:
295
Sequence:
MEHQLLCCEVETIRRAYPDANLLNDRVLRAMLKAEETCAPSVSYFKCVQKEVLPSMRKIVATWMLEVCEEQKCEEEVFPLAMNYLDRFLSLEPVKKSRLQLLGATCMFVASKMKETIPLTAEKLCIYTDNSIRPEELLQMELLLVNKLKWNLAAMTPHDFIEHFLSKMPEAEENKQIIRKHAQTFVALCATDVKFISNPPSMVAAGSVVAAVQGLNLRSPNNFLSYYRLTRFLSRVIKCDPDCLRACQEQIEALLESSLRQAQQNMDPKAAEEEEEEEEEVDLACTPTDVRDVDI
  
Inhibitor
Name:
BDBM6857
Synonyms:
6-bromo-20-methoxy-3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^{11,15}.0^{17,22}]tricosa-1(16),2(10),4(9),5,7,11(15),17(22),18,20-nonaene-12,14-dione | Indolocarbazole deriv. 4m
Type:
Small organic molecule
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Rb(21)
Synonyms:
RB_HUMAN | RB1 | C-terminal retinoblastoma protein
Type:
Other Protein Type
Mol. Mass.:
17129.60
Organism:
Human
Description:
Amino acids 769-921 of human retinoblastoma 1.
Residue:
153
Sequence:
LQYASTRPPTLSPIPHIPRSPYKFPSSPLRIPGGNIYISPLKSPYKISEGLPTPTKMTPRSRILVSIGESFGTSEKFQKINQMVCNSDRVLKRSAEGSNPPKPLKKLRFDIEGSDEADGSKHLPGESKFQQKLAEMTSTRTRMQKQKMNDSMD