Reaction Details
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Cyclin-dependent kinase/G2/mitotic-specific cyclin- 1
Ligand
BDBM5667
Substrate
Histone H1
Meas. Tech.
Kinase Inhibition assay
pH
8.0000±n/a
Temperature
303.1500±n/a K
IC50
30±n/a nM
Citation
Kim, KS; Kimball, SD; Misra, RN; Rawlins, DB; Hunt, JT; Xiao, HY; Lu, S; Qian, L; Han, WC; Shan, W; Mitt, T; Cai, ZW; Poss, MA; Zhu, H; Sack, JS; Tokarski, JS; Chang, CY; Pavletich, N; Kamath, A; Humphreys, WG; Marathe, P; Bursuker, I; Kellar, KA; Roongta, U; Batorsky, R; Mulheron, JG; Bol, D; Fairchild, CR; Lee, FY; Webster, KR Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities. J Med Chem 45:3905-27 (2002) [PubMed] Article More Info.:
Target
Name:
Cyclin-dependent kinase/G2/mitotic-specific cyclin- 1
Synonyms:
cdk1 | 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
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:
Cell division control protein 2 homolog | Cell division protein kinase 1 | Cyclin-dependent kinase 1 (CDK1) | p34 protein kinase | CDK1_HUMAN | CDK1 | CDC2 | CDC28A | CDKN1 | P34CDC2
Type:
Enzyme Subunit
Mol. Mass.:
34101.08
Organism:
Human
Description:
P06493
Residue:
297
Sequence:
MEDYTKIEKIGEGTYGVVYKGRHKTTGQVVAMKKIRLESEEEGVPSTAIREISLLKELRHPNIVSLQDVLMQDSRLYLIFEFLSMDLKKYLDSIPPGQYMDSSLVKSYLYQILQGIVFCHSRRVLHRDLKPQNLLIDDKGTIKLADFGLARAFGIPIRVYTHEVVTLWYRSPEVLLGSARYSTPVDIWSIGTIFAELATKKPLFHGDSEIDQLFRIFRALGTPNNEVWPEVESLQDYKNTFPKWKPGSLASHVKNLDENGLDLLSKMLIYDPAKRISGKMALNHPYFNDLDNQIKKM
Component 2
Name:
G2/mitotic-specific cyclin-B1
Synonyms:
CCNB1_HUMAN | CCNB1 | CCNB
Type:
Enzyme Subunit
Mol. Mass.:
48340.95
Organism:
Human
Description:
P14635
Residue:
433
Sequence:
MALRVTRNSKINAENKAKINMAGAKRVPTAPAATSKPGLRPRTALGDIGNKVSEQLQAKMPMKKEAKPSATGKVIDKKLPKPLEKVPMLVPVPVSEPVPEPEPEPEPEPVKEEKLSPEPILVDTASPSPMETSGCAPAEEDLCQAFSDVILAVNDVDAEDGADPNLCSEYVKDIYAYLRQLEEEQAVRPKYLLGREVTGNMRAILIDWLVQVQMKFRLLQETMYMTVSIIDRFMQNNCVPKKMLQLVGVTAMFIASKYEEMYPPEIGDFAFVTDNTYTKHQIRQMEMKILRALNFGLGRPLPLHFLRRASKIGEVDVEQHTLAKYLMELTMLDYDMVHFPPSQIAAGAFCLALKILDNGEWTPTLQHYLSYTEESLLPVMQHLAKNVVMVNQGLTKHMTVKNKYATSKHAKISTLPQLNSALVQDLAKAVAKV
Inhibitor
Name:
BDBM5667
Synonyms:
3-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)-1-(2,6-dichlorophenyl)urea | N-(2,6-Dichlorophenyl)-N-[5-[[[5-tert-butyl-2-oxazolyl]-methyl]thio]-2-thiazolyl]urea | 2-amino-5-thio-substituted thiazole 41
Type:
Small organic molecule
Emp. Form.:
C18H18Cl2N4O2S2
Mol. Mass.:
456.02
SMILES:
CC(C)(C)c1cnc(CSc2cnc(NC(=O)Nc3c(Cl)cccc3Cl)s2)o1
Substrate
Name:
Histone H1
Synonyms:
n/a
Type:
Other Protein Type
Mol. Mass.:
358.43
Organism:
Bovine
Description:
25 uM ATP/0.2 uCi[gamma-33P] as co-substrate.
Residue:
3
Sequence:
NA
