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Target
Serine/threonine-protein kinase PLK2
Ligand
BDBM25518
Substrate
CHK2 Substrate Peptide
Meas. Tech.
Plk in Vitro Assay
pH
7.2±n/a
Temperature
303.15±n/a K
IC50
597±n/a nM
Citation
Fucini, RV; Hanan, EJ; Romanowski, MJ; Elling, RA; Lew, W; Barr, KJ; Zhu, J; Yoburn, JC; Liu, Y; Fahr, BT; Fan, J; Lu, Y; Pham, P; Choong, IC; VanderPorten, EC; Bui, M; Purkey, HE; Evanchik, MJ; Yang, W Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors. Bioorg Med Chem Lett 18:5648-52 (2008) [PubMed] Article
More Info.:
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:
BDBM25518
Synonyms:
2-amino-pyrazolopyridine, 29 | 3-[3-chloro-5-(3-methyl-6-{[(1S)-1-phenylethyl]amino}-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
Type:
Small organic molecule
Emp. Form.:
C24H24ClN5O
Mol. Mass.:
433.933
SMILES:
C[C@H](Nc1cc2n(nc(C)c2cn1)-c1cc(Cl)cc(CCC(N)=O)c1)c1ccccc1 |r|
Substrate
Name:
CHK2 Substrate Peptide
Synonyms:
CHK2tide
Type:
Fluorophore tagged peptide
Mol. Mass.:
1755.03
Organism:
n/a
Description:
n/a
Residue:
14
Sequence:
AMRLERQDSIFYPK