Reaction Details 
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Cyclin-A2/Cyclin-dependent kinase 2
Ligand
BDBM7160
Substrate
Histone H1
Meas. Tech.
Kinase SPA Assay
IC50
9±n/a nM
Citation
Pevarello, P; Brasca, MG; Amici, R; Orsini, P; Traquandi, G; Corti, L; Piutti, C; Sansonna, P; Villa, M; Pierce, BS; Pulici, M; Giordano, P; Martina, K; Fritzen, EL; Nugent, RA; Casale, E; Cameron, A; Ciomei, M; Roletto, F; Isacchi, A; Fogliatto, G; Pesenti, E; Pastori, W; Marsiglio, A; Leach, KL; Clare, PM; Fiorentini, F; Varasi, M; Vulpetti, A; Warpehoski, MA 3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding. J Med Chem 47:3367-80 (2004) [PubMed] ArticleMore Info.:
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:
BDBM7160
Synonyms:
3-Phenylacetamidoaminopyrazole deriv. 37 | N-(5-Cyclopropyl-1H-pyrazol-3-yl)-2-(3 -methyl[1,1 -biphenyl]-4-yl)acetamide | N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-[4-(3-methylphenyl)phenyl]acetamide
Type:
Small organic molecule
Emp. Form.:
C21H21N3O
Mol. Mass.:
331.4109
SMILES:
Cc1cccc(c1)-c1ccc(CC(=O)Nc2cc(n[nH]2)C2CC2)cc1
Structure:
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