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Target
Cyclin-dependent kinase/G2/mitotic-specific cyclin- 1
Ligand
BDBM33214
Substrate
Rb (Ser780) Biotinylated Peptide
Meas. Tech.
CDK1 Inhibition Assay
pH
7.5±n/a
Temperature
296.15±n/a K
Comments
48% inhibition @ 100 uM.
Citation
 Matthews, TP; Klair, S; Burns, S; Boxall, K; Cherry, M; Fisher, M; Westwood, IM; Walton, MI; McHardy, T; Cheung, KM; Van Montfort, R; Williams, D; Aherne, GW; Garrett, MD; Reader, J; Collins, I Identification of inhibitors of checkpoint kinase 1 through template screening. J Med Chem 52:4810-9 (2009) [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:
BDBM33214
Synonyms:
pyrazolopyridine, 13
Type:
Small organic molecule
Emp. Form.:
C15H17N5OS
Mol. Mass.:
315.393
SMILES:
NCC1CN(CCO1)c1c(cnc2[nH]ncc12)-c1ccsc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Rb (Ser780) Biotinylated Peptide
Synonyms:
n/a
Type:
Biotinylated peptide
Mol. Mass.:
723.86
Organism:
n/a
Description:
Peptide contains residues surrounding serine 780 of Rb. Only the peptide core sequence is shown here.
Residue:
7
Sequence:
PTLSPIP