Reaction Details Report a problem with these data
Target
Phospholipase A2, membrane associated
Ligand
BDBM23771
Substrate
BDBM23751
Meas. Tech.
Fluorimetric Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
470±n/a nM
Citation
Boukli, L; Touaibia, M; Meddad-Belhabich, N; Djimdé, A; Park, CH; Kim, JJ; Yoon, JH; Lamouri, A; Heymans, F Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4'-yl(oyl)] piperazines. Bioorg Med Chem 16:1242-53 (2008) [PubMed] Article
More Info.:
Target
Name:
Phospholipase A2, membrane associated
Synonyms:
GIIC sPLA2 | Group IIA phospholipase A2 | NPS-PLA2 | Non-Pancreatic Secretory Phospholipase A2 | Non-pancreatic secretory phospholipase A2 (hnps-PLA2) | PA2GA_HUMAN | PLA2B | PLA2G2A | PLA2L | Phosphatidylcholine 2-acylhydrolase | Phospholipase A2 group IIA | RASF-A
Type:
Hydrolase
Mol. Mass.:
16101.20
Organism:
Homo sapiens (Human)
Description:
The human nps PLA2 was cloned, and expressed in E. coli. There was a refolding process in the purification.
Residue:
144
Sequence:
MKTLLLLAVIMIFGLLQAHGNLVNFHRMIKLTTGKEAALSYGFYGCHCGVGGRGSPKDATDRCCVTHDCCYKRLEKRGCGTKFLSYKFSNSGSRITCAKQDSCRSQLCECDKAAATCFARNKTTYNKKYQYYSNKHCRGSTPRC
Inhibitor
Name:
BDBM23771
Synonyms:
(3-{[1-benzyl-3-(carbamoylmethyl)-2-ethyl-1H-indol-5-yl]oxy}propyl)phosphonic acid | CHEMBL146186 | LY311727
Type:
Small organic molecule
Emp. Form.:
C22H27N2O5P
Mol. Mass.:
430.4339
SMILES:
CCc1c(CC(N)=O)c2cc(OCCCP(O)(O)=O)ccc2n1Cc1ccccc1