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Target
Cyclin-dependent kinase/G2/mitotic-specific cyclin- 1
Ligand
BDBM6873
Substrate
Biotinylated CDK1 Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
pH
8±n/a
Temperature
303.15±n/a K
IC50
130±n/a nM
Citation
 Lin, R; Connolly, PJ; Huang, S; Wetter, SK; Lu, Y; Murray, WV; Emanuel, SL; Gruninger, RH; Fuentes-Pesquera, AR; Rugg, CA; Middleton, SA; Jolliffe, LK 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem 48:4208-11 (2005) [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:
BDBM6873
Synonyms:
1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3i | 4-({5-amino-1-[(2,6-difluorophenyl)carbonyl]-1H-1,2,4-triazol-3-yl}amino)-N-[2-(dimethylamino)ethyl]benzene-1-sulfonamide | 4-{[5-amino-1-(2,6-difluorobenzoyl)-1H-1,2,4-triazol-3-yl]amino}-N-[2-(dimethylamino)ethyl]benzenesulfonamide
Type:
Small organic molecule
Emp. Form.:
C19H21F2N7O3S
Mol. Mass.:
465.477
SMILES:
CN(C)CCNS(=O)(=O)c1ccc(Nc2nc(N)n(n2)C(=O)c2c(F)cccc2F)cc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Biotinylated CDK1 Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
3057.82
Organism:
n/a
Description:
n/a
Residue:
27
Sequence:
ITINKTPKKAKKPKTPKKAKKLAMIDE