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Target
Cyclin-dependent kinase/G2/mitotic-specific cyclin- 1
Ligand
BDBM6630
Substrate
S1 peptide
Meas. Tech.
Tyrosine Kinase Assay
IC50
31000±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/G2/mitotic-specific cyclin- 1
Synonyms:
CDK1/B | CDK1/Cyclin B | CDK1/CyclinB | Cyclin B/Dependent Kinase 1 (CDK1) | Cyclin-Dependent Kinase 1 (CDK1) | Cyclin-dependent kinase 1/cyclin B1 | Cyclin-dependent kinase/G2/mitotic-specific cyclin 1 | cdk1
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
CDK1/Cyclin B 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 1
Synonyms:
CDC2 | CDC28A | CDK1 | CDK1_HUMAN | CDKN1 | Cell division control protein 2 homolog | Cell division protein kinase 1 | Cyclin-dependent kinase 1 (CDK1) | P34CDC2 | p34 protein kinase
Type:
Enzyme Subunit
Mol. Mass.:
34101.08
Organism:
Homo sapiens (Human)
Description:
P06493
Residue:
297
Sequence:
MEDYTKIEKIGEGTYGVVYKGRHKTTGQVVAMKKIRLESEEEGVPSTAIREISLLKELRHPNIVSLQDVLMQDSRLYLIFEFLSMDLKKYLDSIPPGQYMDSSLVKSYLYQILQGIVFCHSRRVLHRDLKPQNLLIDDKGTIKLADFGLARAFGIPIRVYTHEVVTLWYRSPEVLLGSARYSTPVDIWSIGTIFAELATKKPLFHGDSEIDQLFRIFRALGTPNNEVWPEVESLQDYKNTFPKWKPGSLASHVKNLDENGLDLLSKMLIYDPAKRISGKMALNHPYFNDLDNQIKKM
  
Component 2
Name:
G2/mitotic-specific cyclin-B1
Synonyms:
CCNB | CCNB1 | CCNB1_HUMAN
Type:
Enzyme Subunit
Mol. Mass.:
48340.95
Organism:
Homo sapiens (Human)
Description:
P14635
Residue:
433
Sequence:
MALRVTRNSKINAENKAKINMAGAKRVPTAPAATSKPGLRPRTALGDIGNKVSEQLQAKMPMKKEAKPSATGKVIDKKLPKPLEKVPMLVPVPVSEPVPEPEPEPEPEPVKEEKLSPEPILVDTASPSPMETSGCAPAEEDLCQAFSDVILAVNDVDAEDGADPNLCSEYVKDIYAYLRQLEEEQAVRPKYLLGREVTGNMRAILIDWLVQVQMKFRLLQETMYMTVSIIDRFMQNNCVPKKMLQLVGVTAMFIASKYEEMYPPEIGDFAFVTDNTYTKHQIRQMEMKILRALNFGLGRPLPLHFLRRASKIGEVDVEQHTLAKYLMELTMLDYDMVHFPPSQIAAGAFCLALKILDNGEWTPTLQHYLSYTEESLLPVMQHLAKNVVMVNQGLTKHMTVKNKYATSKHAKISTLPQLNSALVQDLAKAVAKV
  
Inhibitor
Name:
BDBM6630
Synonyms:
3-[(9bR)-5-oxo-1H,2H,3H,5H,9bH-benzo[a]pyrrolizin-9-yl]-1-{5-[(2S)-pyrrolidin-2-yl]-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)-pyrrolidin-2-yl]-1H-pyrazol-3-yl}urea | pyrazole-3-yl urea deriv. 14a
Type:
Small organic molecule
Emp. Form.:
C19H22N6O2
Mol. Mass.:
366.417
SMILES:
O=C(Nc1cc(n[nH]1)[C@@H]1CCCN1)Nc1cccc2C(=O)N3CCC[C@@H]3c12 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
S1 peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1333.73
Organism:
n/a
Description:
50 uM ATP (0.5-1.5 uCi of [33P]-ATP (3000 Ci/mmol)) as co-substrate.
Residue:
12
Sequence:
AKAKKTPKKAKK