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Target
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 [L188C]
Ligand
BDBM6650
Substrate
G1 peptide
Meas. Tech.
CDKs Assay
Temperature
303.15±n/a K
IC50
410000±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
More Info.:
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:
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:
Human
Description:
P24385[L188C]
Residue:
295
Sequence:
MEHQLLCCEVETIRRAYPDANLLNDRVLRAMLKAEETCAPSVSYFKCVQKEVLPSMRKIVATWMLEVCEEQKCEEEVFPLAMNYLDRFLSLEPVKKSRLQLLGATCMFVASKMKETIPLTAEKLCIYTDGSIRPEELLQMELLLVNKLKWNLAAMTPHDFIEHFLSKMPEAEENKQIIRKHAQTFVASCATDVKFISNPPSMVAAGSVVAAVQGLNLRSPNNFLSYYRLTRFLSRVIKCDPDCLRACQEQIEALLESSLRQAQQNMDPKAAEEEEEEEEEVDLACTPTDVRDVDI
Inhibitor
Name:
BDBM6650
Synonyms:
1-benzyl-3-(7-hydroxynaphthalen-1-yl)urea | CHEMBL139989 | Diarylurea deriv. 1e | N-Benzyl-N -(7-hydroxy-1-naphthyl)urea
Type:
Small organic molecule
Emp. Form.:
C18H16N2O2
Mol. Mass.:
292.3318
SMILES:
Oc1ccc2cccc(NC(=O)NCc3ccccc3)c2c1
Substrate
Name:
G1 peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1483.28
Organism:
n/a
Description:
n/a
Residue:
13
Sequence:
RPPTLSPIPHIPR