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Target
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 [L188C]
Ligand
BDBM6658
Substrate
G1 peptide
Meas. Tech.
CDKs Assay
Temperature
303.15±n/a K
IC50
3600±n/a nM
Comments
extracted
Citation
 Honma, T; Hayashi, K; Aoyama, T; Hashimoto, N; Machida, T; Fukasawa, K; Iwama, T; Ikeura, C; Ikuta, M; Suzuki-Takahashi, I; Iwasawa, Y; Hayama, T; Nishimura, S; Morishima, H Structure-based generation of a new class of potent Cdk4 inhibitors: new de novo design strategy and library design. J Med Chem 44:4615-27 (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:
BDBM6658
Synonyms:
3-(1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl)-1-pyridin-2-ylurea | Diarylurea deriv. 14c | N-(1,3-Dioxo-2,3-dihydro-1H-isoindol-4-yl)-N -pyridin-2-ylurea
Type:
Small organic molecule
Emp. Form.:
C14H10N4O3
Mol. Mass.:
282.2542
SMILES:
O=C(Nc1ccccn1)Nc1cccc2C(=O)NC(=O)c12
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