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TargetCyclin-Dependent Kinase 2 (CDK2)
LigandBDBM7114
Substrate/CompetitorHistone H1
Meas. Tech.Kinase SPA Assay
IC50 11±n/a nM
Citation Pevarello, P; Brasca, MG; Orsini, P; Traquandi, G; Longo, A; Nesi, M; Orzi, F; Piutti, C; Sansonna, P; Varasi, M; Cameron, A; Vulpetti, A; Roletto, F; Alzani, R; Ciomei, M; Albanese, C; Pastori, W; Marsiglio, A; Pesenti, E; Fiorentini, F; Bischoff, JR; Mercurio, C 3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization. J Med Chem48:2944-56 (2005) [PubMed]  Article
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Cyclin-Dependent Kinase 2 (CDK2)
Name:Cyclin-Dependent Kinase 2 (CDK2)
Synonyms:CDK2-CyclinA | CDK2/A | CDK2/Cyclin A | Cyclin A2/dependent kinase 2 | 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:CDK2/Bovine cyclin A
Synonyms:CDK2 | CDK2-Kinase | Cell division protein kinase 2 | Cyclin-dependent kinase 2 (CDK2) | p33 protein kinase
Type:Enzyme Subunit
Mol. Mass.:33938.17
Organism:Homo sapiens (Human)
Description:P24941
Residue:298
Sequence:
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNH
PNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHS
HRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYY
STAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSF
PKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
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Component 2
Name:Cyclin-A2
Synonyms:CCN1 | CCNA | CCNA1 | Cyclin A | Cyclin-A
Type:Enzyme Subunit
Mol. Mass.:48550.19
Organism:Homo sapiens (Human)
Description:n/a
Residue:432
Sequence:
MLGNSAPGPATREAGSALLALQQTALQEDQENINPEKAAPVQQPRTRAALAVLKSGNPRG
LAQQQRPKTRRVAPLKDLPVNDEHVTVPPWKANSKQPAFTIHVDEAEKEAQKKPAESQKI
EREDALAFNSAISLPGPRKPLVPLDYPMDGSFESPHTMDMSIILEDEKPVSVNEVPDYHE
DIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHLAVNYID
RFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRMEHLVLK
VLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSVIAGAAF
HLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYKNSKYHG
VSLLNPPETLNL
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BDBM7114
NameBDBM7114
Synonyms:3-Aminopyrazole deriv. 27 | N-(5-Cyclopropyl-1H-pyrazol-3-yl)-2-[4-(2-oxo-2,3-dihydro-1H-imidazol-1-yl)phenyl]propanamide
TypeSmall organic molecule
Emp. Form.C18H19N5O2
Mol. Mass.337.3758
SMILESCC(C(=O)Nc1cc(n[nH]1)C1CC1)c1ccc(cc1)-n1cc[nH]c1=O
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
Histone H1
Name:Histone H1
Synonyms:n/a
Type:Other Protein Type
Mol. Mass.:358.43
Organism:Bos taurus (bovine)
Description:n/a
Residue:3
Sequence:
n/a