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Target
Cyclin-A2/Cyclin-dependent kinase 2
Ligand
BDBM7751
Substrate
Peptide Substrate
Meas. Tech.
Kinase Inhibition SPA Assay
IC50
0.54±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:
BDBM7751
Synonyms:
(12Z)-12-{[(4-{[2-(2-hydroxyethoxy)ethyl]sulfamoyl}phenyl)amino]methylidene}-3-thia-5,10-diazatricyclo[7.3.0.0^{2,6}]dodeca-1,4,6,8-tetraen-11-one | N-[2-(2-Hydroxyethoxy)ethyl]-4-{[(7-oxo-6,7-dihydro-8H-[1,3]thiazolo[5,4-e]indol-8-ylidene)methyl]amino}-benzenesulfonamide | Oxindole-Based Inhibitor 87
Type:
Small organic molecule
Emp. Form.:
C20H20N4O5S2
Mol. Mass.:
460.527
SMILES:
OCCOCCNS(=O)(=O)c1ccc(cc1)N=CC1C(=O)Nc2ccc3ncsc3c12 |w:17.18|
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