Target
Endothelial lipase
Ligand
BDBM319458
Substrate
n/a
Meas. Tech.
Biological Activity
IC50
1.000±n/a nM
Citation
 Johnson, JAPi, ZQiao, JXKim, SWang, TCJiang, JFinlay, HLloyd, J Sulfone amide linked benzothiazole inhibitors of endothelial lipase US Patent  US10173991 Publication Date 1/8/2019 
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:
BDBM319458
Synonyms:
2-(6-{4-[(benzyl- carbamoyl) amino]phenyl}- 5-fluoro-1,3- benzothiazol- 2-yl)-N- [(cyclopropyl- carbamoyl) methyl]-2-(3,3,3- trifluoropropane- sulfonyl)acetamide | US10173991, Example 511
Type:
Small organic molecule
Emp. Form.:
C31H29F4N5O5S2
Mol. Mass.:
691.716
SMILES:
Fc1cc2nc(sc2cc1-c1ccc(NC(=O)NCc2ccccc2)cc1)C(C(=O)NCC(=O)NC1CC1)S(=O)(=O)CCC(F)(F)F
Structure:
Search PDB for entries with ligand similarity: