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Target
Serine/threonine-protein kinase PLK2
Ligand
BDBM50318079
Substrate
n/a
Meas. Tech.
ChEMBL_631390 (CHEMBL1109142)
IC50
>10000±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:
BDBM50318079
Synonyms:
8-{[2-Acetyl-5-(4-methylpiperazin-1-yl)phenyl]amino}-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1095716
Type:
Small organic molecule
Emp. Form.:
C24H28N8O2
Mol. Mass.:
460.5315
SMILES:
CN1CCN(CC1)c1ccc(C(C)=O)c(Nc2ncc3CCc4c(nn(C)c4-c3n2)C(N)=O)c1
Structure:
Search PDB for entries with ligand similarity: