Ki Summary

Reaction Details

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Target

Serine/threonine-protein kinase PLK2

Ligand

BDBM50329919

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_675878 (CHEMBL1272695)

IC50

>10000±n/a nM

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

More Info.:

Get all data from this article, Assay Method

Serine/threonine-protein kinase PLK2

Name:

Serine/threonine-protein kinase PLK2

Synonyms:

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

BDBM50329919

n/a

Name

BDBM50329919

Synonyms:

1-(3-(3-carbamoyl-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazolin-8-ylamino)-4-(trifluoromethoxy)phenyl)-4-methylpiperazine 1,4-dioxide | CHEMBL1271694

Type

Small organic molecule

Emp. Form.

C23H25F3N8O4

Mol. Mass.

534.491

SMILES

Cn1nc(C(N)=O)c2CCc3cnc(Nc4cc(ccc4OC(F)(F)F)[N+]4([O-])CC[N+](C)([O-])CC4)nc3-c12 |(40.62,-1.5,;41.66,-.36,;43.19,-.53,;43.83,.88,;45.36,.88,;46.14,-.45,;46.13,2.21,;42.69,1.92,;42.69,3.47,;41.34,4.25,;40,3.47,;38.67,4.24,;37.34,3.47,;37.34,1.92,;36,1.15,;36,-.38,;37.33,-1.15,;37.34,-2.68,;36,-3.46,;34.67,-2.69,;34.67,-1.15,;33.34,-.38,;32,-1.15,;30.67,-.38,;32,-2.69,;30.67,-1.9,;38.67,-3.45,;38.27,-1.95,;38.67,-4.98,;40,-5.75,;41.33,-4.98,;42.81,-5.38,;41.32,-6.52,;41.33,-3.44,;40,-2.67,;38.67,1.15,;40,1.92,;41.34,1.15,)|

Structure