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Target
Serine/threonine-protein kinase PLK2
Ligand
BDBM50436749
Substrate
n/a
Meas. Tech.
ChEMBL_971578 (CHEMBL2406852)
IC50
9.0±n/a nM
Citation
 Bowers, S; Truong, AP; Ye, M; Aubele, DL; Sealy, JM; Neitz, RJ; Hom, RK; Chan, W; Dappen, MS; Galemmo, RA; Konradi, AW; Sham, HL; Zhu, YL; Beroza, P; Tonn, G; Zhang, H; Hoffman, J; Motter, R; Fauss, D; Tanaka, P; Bova, MP; Ren, Z; Tam, D; Ruslim, L; Baker, J; Pandya, D; Diep, L; Fitzgerald, K; Artis, DR; Anderson, JP; Bergeron, M Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors. Bioorg Med Chem Lett 23:2743-9 (2013) [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:
BDBM50436749
Synonyms:
CHEMBL2401966
Type:
Small organic molecule
Emp. Form.:
C21H21F3N6O
Mol. Mass.:
430.4262
SMILES:
CC[C@H]1N(CCC(F)(F)F)c2nc(ncc2N(C)C1=O)-n1ccnc1-c1ccccc1 |r|
Structure:
Search PDB for entries with ligand similarity: