Reaction Details  Report a problem with these data
Target
Serine/threonine-protein kinase PLK2
Ligand
BDBM50436739
Substrate
n/a
Meas. Tech.
ChEMBL_971578 (CHEMBL2406852)
IC50
168±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:
BDBM50436739
Synonyms:
CHEMBL2401957
Type:
Small organic molecule
Emp. Form.:
C21H21N9O
Mol. Mass.:
415.4511
SMILES:
CCC1N(c2cnn(C)c2)c2nc(ncc2N(C)C1=O)-c1c[nH]nc1-c1ccccn1
Structure:
Search PDB for entries with ligand similarity: