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Target
Cyclin-dependent kinase/G2/mitotic-specific cyclin- 1
Ligand
BDBM27084
Substrate
Histone H1
Meas. Tech.
Aurora Kinase Assay
IC50
2900±n/a nM
Citation
Howard, S; Berdini, V; Boulstridge, JA; Carr, MG; Cross, DM; Curry, J; Devine, LA; Early, TR; Fazal, L; Gill, AL; Heathcote, M; Maman, S; Matthews, JE; McMenamin, RL; Navarro, EF; O'Brien, MA; O'Reilly, M; Rees, DC; Reule, M; Tisi, D; Williams, G; Vinković, M; Wyatt, PG Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity. J Med Chem 52:379-88 (2009) [PubMed] Article
More Info.:
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:
BDBM27084
Synonyms:
1-cyclohexyl-3-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-benzodiazol-2-yl]-1H-pyrazol-4-yl}urea | pyrazole-benzimidazole urea analogue, 13
Type:
Small organic molecule
Emp. Form.:
C22H29N7O2
Mol. Mass.:
423.5114
SMILES:
O=C(NC1CCCCC1)Nc1c[nH]nc1-c1nc2ccc(CN3CCOCC3)cc2[nH]1
Substrate
Name:
Histone H1
Synonyms:
n/a
Type:
Other Protein Type
Mol. Mass.:
358.43
Organism:
Bos taurus (bovine)
Description:
n/a
Residue:
3
Sequence:
NA