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Target
Cyclin-A2/Cyclin-dependent kinase 2
Ligand
BDBM7773
Substrate
Peptide Substrate
Meas. Tech.
Kinase Inhibition SPA Assay
IC50
8.9±n/a nM
Citation
 Bramson, HN; Corona, J; Davis, ST; Dickerson, SH; Edelstein, M; Frye, SV; Gampe, RT; Harris, PA; Hassell, A; Holmes, WD; Hunter, RN; Lackey, KE; Lovejoy, B; Luzzio, MJ; Montana, V; Rocque, WJ; Rusnak, D; Shewchuk, L; Veal, JM; Walker, DH; Kuyper, LF Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis. J Med Chem 44:4339-58 (2001) [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:
BDBM7773
Synonyms:
3-{[(2,2-Dioxido-1,3-dihydro-2-benzothien-5-yl)amino]-methylene}-5-(1,3-oxazol-5-yl)-1,3-dihydro-2H-indol-2-one | 5-({[(3Z)-5-(1,3-oxazol-5-yl)-2-oxo-2,3-dihydro-1H-indol-3-ylidene]methyl}amino)-1,3-dihydro-2-benzothiophene-2,2-dione | Oxindole-Based Inhibitor 109
Type:
Small organic molecule
Emp. Form.:
C20H15N3O4S
Mol. Mass.:
393.416
SMILES:
O=C1Nc2ccc(cc2C1C=Nc1ccc2CS(=O)(=O)Cc2c1)-c1cnco1 |w:10.11|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
5198.94
Organism:
n/a
Description:
n/a
Residue:
46
Sequence:
ITINAMINHEYLALAARGARGPRMETSERPRLYSLYSLYSALACNH