Reaction Details |
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Target | Serine/threonine-protein kinase PLK2 |
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Ligand | BDBM50329915 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_675878 (CHEMBL1272695) |
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IC50 | >10000±n/a nM |
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Citation | Beria, I; Valsasina, B; Brasca, MG; Ceccarelli, W; Colombo, M; Cribioli, S; Fachin, G; Ferguson, RD; Fiorentini, F; Gianellini, LM; Giorgini, ML; Moll, JK; Posteri, H; Pezzetta, D; Roletto, F; Sola, F; Tesei, D; Caruso, M 4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors. Bioorg Med Chem Lett20:6489-94 (2010) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Serine/threonine-protein kinase PLK2 |
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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: | MELLRTITYQPAASTKMCEQALGKGCGADSKKKRPPQPPEESQPPQSQAQVPPAAPHHHH
HHSHSGPEISRIIVDPTTGKRYCRGKVLGKGGFAKCYEMTDLTNNKVYAAKIIPHSRVAK
PHQREKIDKEIELHRILHHKHVVQFYHYFEDKENIYILLEYCSRRSMAHILKARKVLTEP
EVRYYLRQIVSGLKYLHEQEILHRDLKLGNFFINEAMELKVGDFGLAARLEPLEHRRRTI
CGTPNYLSPEVLNKQGHGCESDIWALGCVMYTMLLGRPPFETTNLKETYRCIREARYTMP
SSLLAPAKHLIASMLSKNPEDRPSLDDIIRHDFFLQGFTPDRLSSSCCHTVPDFHLSSPA
KNFFKKAAAALFGGKKDKARYIDTHNRVSKEDEDIYKLRHDLKKTSITQQPSKHRTDEEL
QPPTTTVARSGTPAVENKQQIGDAIRMIVRGTLGSCSSSSECLEDSTMGSVADTVARVLR
GCLENMPEADCIPKEQLSTSFQWVTKWVDYSNKYGFGYQLSDHTVGVLFNNGAHMSLLPD
KKTVHYYAELGQCSVFPATDAPEQFISQVTVLKYFSHYMEENLMDGGDLPSVTDIRRPRL
YLLQWLKSDKALMMLFNDGTFQVNFYHDHTKIIICSQNEEYLLTYINEDRISTTFRLTTL
LMSGCSSELKNRMEYALNMLLQRCN
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BDBM50329915 |
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n/a |
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Name | BDBM50329915 |
Synonyms: | 1-methyl-8-(5-(piperazin-1-yl)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1271644 |
Type | Small organic molecule |
Emp. Form. | C22H23F3N8O2 |
Mol. Mass. | 488.4656 |
SMILES | Cn1nc(C(N)=O)c2CCc3cnc(Nc4cc(ccc4OC(F)(F)F)N4CCNCC4)nc3-c12 |
Structure |
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