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Target
Cyclin-A2/Cyclin-dependent kinase 2
Ligand
BDBM99471
Substrate
n/a
Meas. Tech.
ChEMBL_1296275 (CHEMBL3132603)
IC50
580±n/a nM
Citation
 Okaniwa, M; Hirose, M; Arita, T; Yabuki, M; Nakamura, A; Takagi, T; Kawamoto, T; Uchiyama, N; Sumita, A; Tsutsumi, S; Tottori, T; Inui, Y; Sang, BC; Yano, J; Aertgeerts, K; Yoshida, S; Ishikawa, T Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives. J Med Chem 56:6478-94 (2013) [PubMed]  Article 
Target
Name:
Cyclin-A2/Cyclin-dependent kinase 2
Synonyms:
CDK2-CyclinA | CDK2/A | CDK2/Cyclin A | CDK2/Cyclin A2 | Cyclin A2/dependent kinase 2 | Cyclin-Dependent Kinase 2 (CDK2) | Cyclin-Dependent Kinase 2 (CDK2A)
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
Cdk2/Cyclin A kinase was purified from insect cells coinfected with Cyclin A/Cdk2 baculovirus.
Components:
This complex has 2 components.
Component 1
Name:
Cyclin-dependent kinase 2
Synonyms:
CDK2 | CDK2-Kinase | CDK2_HUMAN | CDKN2 | Cell division protein kinase 2 | Cyclin-dependent kinase 2 (CDK2) | Protein cereblon/Cyclin-dependent kinase 2 | p33 protein kinase
Type:
Enzyme Subunit
Mol. Mass.:
33938.17
Organism:
Homo sapiens (Human)
Description:
P24941
Residue:
298
Sequence:
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
  
Component 2
Name:
Cyclin-A2
Synonyms:
CCN1 | CCNA | CCNA1 | CCNA2 | CCNA2_HUMAN | Cyclin A | Cyclin-A
Type:
Enzyme Subunit
Mol. Mass.:
48550.19
Organism:
Homo sapiens (Human)
Description:
P20248
Residue:
432
Sequence:
MLGNSAPGPATREAGSALLALQQTALQEDQENINPEKAAPVQQPRTRAALAVLKSGNPRGLAQQQRPKTRRVAPLKDLPVNDEHVTVPPWKANSKQPAFTIHVDEAEKEAQKKPAESQKIEREDALAFNSAISLPGPRKPLVPLDYPMDGSFESPHTMDMSIILEDEKPVSVNEVPDYHEDIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHLAVNYIDRFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRMEHLVLKVLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSVIAGAAFHLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYKNSKYHGVSLLNPPETLNL
  
Inhibitor
Name:
BDBM99471
Synonyms:
US8497274, 32
Type:
Small organic molecule
Emp. Form.:
C27H18F4N4O3S
Mol. Mass.:
554.515
SMILES:
Fc1ccc(Oc2ccc3nc(NC(=O)C4CC4)sc3c2C#N)cc1NC(=O)Cc1cccc(c1)C(F)(F)F
Structure:
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