Reaction Details |
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Target | Serine/threonine-protein kinase PLK2 |
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Ligand | BDBM50343558 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_747146 (CHEMBL1777512) |
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IC50 | 1499±n/a nM |
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Citation | Beria, I; Bossi, RT; Brasca, MG; Caruso, M; Ceccarelli, W; Fachin, G; Fasolini, M; Forte, B; Fiorentini, F; Pesenti, E; Pezzetta, D; Posteri, H; Scolaro, A; Re Depaolini, S; Valsasina, B NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg Med Chem Lett21:2969-74 (2011) [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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BDBM50343558 |
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n/a |
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Name | BDBM50343558 |
Synonyms: | 1-methyl-8-(5-(1-methylpiperidine-4-carboxamido)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1774336 |
Type | Small organic molecule |
Emp. Form. | C25H27F3N8O3 |
Mol. Mass. | 544.5289 |
SMILES | CN1CCC(CC1)C(=O)Nc1ccc(OC(F)(F)F)c(Nc2ncc3CCc4c(nn(C)c4-c3n2)C(N)=O)c1 |
Structure |
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