Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetSerine/threonine-protein kinase PLK2
LigandBDBM50329915
Substrate/Competitorn/a
Meas. Tech.ChEMBL_675878 (CHEMBL1272695)
IC50>10000±n/a nM
Citation Beria, IValsasina, BBrasca, MGCeccarelli, WColombo, MCribioli, SFachin, GFerguson, RDFiorentini, FGianellini, LMGiorgini, MLMoll, JKPosteri, HPezzetta, DRoletto, FSola, FTesei, DCaruso, 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: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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50329915
n/a
NameBDBM50329915
Synonyms:1-methyl-8-(5-(piperazin-1-yl)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1271644
TypeSmall organic molecule
Emp. Form.C22H23F3N8O2
Mol. Mass.488.4656
SMILESCn1nc(C(N)=O)c2CCc3cnc(Nc4cc(ccc4OC(F)(F)F)N4CCNCC4)nc3-c12
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: