Target
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 [L188C]
Ligand
BDBM6629
Substrate
G1 peptide
Meas. Tech.
Tyrosine Kinase Assay
IC50
250±n/a nM
Citation
 Honma, TYoshizumi, THashimoto, NHayashi, KKawanishi, NFukasawa, KTakaki, TIkeura, CIkuta, MSuzuki-Takahashi, IHayama, TNishimura, SMorishima, H A novel approach for the development of selective Cdk4 inhibitors: library design based on locations of Cdk4 specific amino acid residues. J Med Chem 44:4628-40 (2001) [PubMed]  Article 
Target
Name:
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 [L188C]
Synonyms:
CDK4/Cyclin D | Cyclin-Dependent Kinase 4 (CDK4)
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
CDK4/D 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 [L188C]
Synonyms:
BCL1 | CCND1 | CCND1_HUMAN | Cyclin D | PRAD1
Type:
Enzyme Subunit
Mol. Mass.:
33634.57
Organism:
Homo sapiens (Human)
Description:
P24385[L188C]
Residue:
295
Sequence:
MEHQLLCCEVETIRRAYPDANLLNDRVLRAMLKAEETCAPSVSYFKCVQKEVLPSMRKIVATWMLEVCEEQKCEEEVFPLAMNYLDRFLSLEPVKKSRLQLLGATCMFVASKMKETIPLTAEKLCIYTDGSIRPEELLQMELLLVNKLKWNLAAMTPHDFIEHFLSKMPEAEENKQIIRKHAQTFVASCATDVKFISNPPSMVAAGSVVAAVQGLNLRSPNNFLSYYRLTRFLSRVIKCDPDCLRACQEQIEALLESSLRQAQQNMDPKAAEEEEEEEEEVDLACTPTDVRDVDI
  
Inhibitor
Name:
BDBM6629
Synonyms:
1-{5-oxo-1H,2H,3H,5H,9bH-benzo[a]pyrrolizin-9-yl}-3-[5-(piperidin-1-ylmethyl)-1H-pyrazol-3-yl]urea | 5-alkylaminomethyl pyrazole-3-yl urea deriv. 9h | N-(5-Oxo-2,3,5,9b-tetrahydro-1H-pyrrolo[2,1-a]isoindol-9-yl)-N -[5-(piperidin-1-ylmethyl)-1H-pyrazol-3-yl]urea
Type:
Small organic molecule
Emp. Form.:
C21H26N6O2
Mol. Mass.:
394.4701
SMILES:
O=C(Nc1cc(CN2CCCCC2)n[nH]1)Nc1cccc2C(=O)N3CCCC3c12
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
G1 peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1483.28
Organism:
n/a
Description:
n/a
Residue:
13
Sequence:
RPPTLSPIPHIPR