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Target
Serine/threonine-protein kinase PLK2
Ligand
BDBM50318076
Substrate
n/a
Meas. Tech.
ChEMBL_631390 (CHEMBL1109142)
IC50
14±n/a nM
Citation
 Beria, I; Ballinari, D; Bertrand, JA; Borghi, D; Bossi, RT; Brasca, MG; Cappella, P; Caruso, M; Ceccarelli, W; Ciavolella, A; Cristiani, C; Croci, V; De Ponti, A; Fachin, G; Ferguson, RD; Lansen, J; Moll, JK; Pesenti, E; Posteri, H; Perego, R; Rocchetti, M; Storici, P; Volpi, D; Valsasina, B Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors. J Med Chem 53:3532-51 (2010) [PubMed]  Article 
Target
Name:
Serine/threonine-protein kinase PLK2
Synonyms:
PLK2 | PLK2_HUMAN | Polo-Like Kinase 2 | SNK | Serine/threonine-protein kinase PLK2 | Serine/threonine-protein kinase SNK | Serum-inducible kinase
Type:
Serine/threonine-protein kinase
Mol. Mass.:
78259.87
Organism:
Homo sapiens (Human)
Description:
Full-length human PLK2 was expressed as GST-fusion protein using baculovirus expression system. GST-PLK2 was purified by using glutathione sepharose chromatography.
Residue:
685
Sequence:
MELLRTITYQPAASTKMCEQALGKGCGADSKKKRPPQPPEESQPPQSQAQVPPAAPHHHHHHSHSGPEISRIIVDPTTGKRYCRGKVLGKGGFAKCYEMTDLTNNKVYAAKIIPHSRVAKPHQREKIDKEIELHRILHHKHVVQFYHYFEDKENIYILLEYCSRRSMAHILKARKVLTEPEVRYYLRQIVSGLKYLHEQEILHRDLKLGNFFINEAMELKVGDFGLAARLEPLEHRRRTICGTPNYLSPEVLNKQGHGCESDIWALGCVMYTMLLGRPPFETTNLKETYRCIREARYTMPSSLLAPAKHLIASMLSKNPEDRPSLDDIIRHDFFLQGFTPDRLSSSCCHTVPDFHLSSPAKNFFKKAAAALFGGKKDKARYIDTHNRVSKEDEDIYKLRHDLKKTSITQQPSKHRTDEELQPPTTTVARSGTPAVENKQQIGDAIRMIVRGTLGSCSSSSECLEDSTMGSVADTVARVLRGCLENMPEADCIPKEQLSTSFQWVTKWVDYSNKYGFGYQLSDHTVGVLFNNGAHMSLLPDKKTVHYYAELGQCSVFPATDAPEQFISQVTVLKYFSHYMEENLMDGGDLPSVTDIRRPRLYLLQWLKSDKALMMLFNDGTFQVNFYHDHTKIIICSQNEEYLLTYINEDRISTTFRLTTLLMSGCSSELKNRMEYALNMLLQRCN
  
Inhibitor
Name:
BDBM50318076
Synonyms:
1-Methyl-8-{[2-(methylsulfanyl)phenyl]amino}-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1094478
Type:
Small organic molecule
Emp. Form.:
C18H18N6OS
Mol. Mass.:
366.44
SMILES:
CSc1ccccc1Nc1ncc2CCc3c(nn(C)c3-c2n1)C(N)=O
Structure:
Search PDB for entries with ligand similarity: