Reaction Details Report a problem with these data
Target
Endothelial lipase
Ligand
BDBM187290
Substrate
n/a
Meas. Tech.
ChEMBL_1825990 (CHEMBL4325754)
IC50
400±n/a nM
Citation
 Tora, G; Kim, SH; Pi, Z; Johnson, JA; Jiang, J; Phillips, M; Lloyd, J; Abell, LM; Lu, H; Locke, G; Adam, LP; Taylor, DS; Yin, X; Behnia, K; Zhao, L; Yang, R; Basso, M; Caporuscio, C; Chen, AY; Liu, E; Kirshgessner, T; Onorato, JM; Ryan, C; Traeger, SC; Gordon, D; Wexler, RR; Finlay, HJ Identification of Reversible Small Molecule Inhibitors of Endothelial Lipase (EL) That Demonstrate HDL-C Increase In Vivo. J Med Chem 63:1660-1670 (2020) [PubMed]  Article 
Target
Name:
Endothelial lipase
Synonyms:
EDL | EL | Endothelial cell-derived lipase | LIPE_HUMAN | LIPG
Type:
Protein
Mol. Mass.:
56805.62
Organism:
Homo sapiens (Human)
Description:
Q9Y5X9
Residue:
500
Sequence:
MSNSVPLLCFWSLCYCFAAGSPVPFGPEGRLEDKLHKPKATQTEVKPSVRFNLRTSKDPEHEGCYLSVGHSQPLEDCSFNMTAKTFFIIHGWTMSGIFENWLHKLVSALHTREKDANVVVVDWLPLAHQLYTDAVNNTRVVGHSIARMLDWLQEKDDFSLGNVHLIGYSLGAHVAGYAGNFVKGTVGRITGLDPAGPMFEGADIHKRLSPDDADFVDVLHTYTRSFGLSIGIQMPVGHIDIYPNGGDFQPGCGLNDVLGSIAYGTITEVVKCEHERAVHLFVDSLVNQDKPSFAFQCTDSNRFKKGICLSCRKNRCNSIGYNAKKMRNKRNSKMYLKTRAGMPFRVYHYQMKIHVFSYKNMGEIEPTFYVTLYGTNADSQTLPLEIVERIEQNATNTFLVYTEEDLGDLLKIQLTWEGASQSWYNLWKEFRSYLSQPRNPGRELNIRRIRVKSGETQRKLTFCTEDPENTSISPGRELWFRKCRDGWRMKNETSPTVELP
  
Inhibitor
Name:
BDBM187290
Synonyms:
US9169240, 30
Type:
Small organic molecule
Emp. Form.:
C19H16N6O6S2
Mol. Mass.:
488.497
SMILES:
COC(=O)Nc1ccc(cc1)-c1ccc2nc(sc2c1)C(=O)c1nnc(CNS(N)(=O)=O)o1
Structure:
Search PDB for entries with ligand similarity: