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Target
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 [L188C]
Ligand
BDBM6632
Substrate
G1 peptide
Meas. Tech.
Tyrosine Kinase Assay
IC50
1.6±n/a nM
Citation
 Honma, T; Yoshizumi, T; Hashimoto, N; Hayashi, K; Kawanishi, N; Fukasawa, K; Takaki, T; Ikeura, C; Ikuta, M; Suzuki-Takahashi, I; Hayama, T; Nishimura, S; Morishima, 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:
BDBM6632
Synonyms:
3-[(9bR)-5-oxo-1H,2H,3H,5H,9bH-benzo[a]pyrrolizin-9-yl]-1-[5-({[(2S)-5-chloro-2,3-dihydro-1H-inden-2-yl]amino}methyl)-1H-pyrazol-3-yl]urea | N-[(9bR)-5-Oxo-2,3,5,9b-tetrahydro-1H-pyrrolo[2,1-a]-isoindol-9-yl]-N -[5-({[(2S)-5-chloro-2,3-dihydro-1Hinden-2-yl]amino}methyl)-1H-pyrazol-3-yl]urea | pyrazole-3-yl urea deriv. 15a
Type:
Small organic molecule
Emp. Form.:
C25H25ClN6O2
Mol. Mass.:
476.958
SMILES:
Clc1ccc2C[C@@H](Cc2c1)NCc1cc(NC(=O)Nc2cccc3C(=O)N4CCC[C@@H]4c23)[nH]n1 |r|
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