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Assay Detail

CHEMBL3095184

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human endothelial lipase using HDL as substrate assessed as release of free fatty acids preincubated for 30 mins followed by substrate addition measured after 2 hrs
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Endothelial lipase (CHEMBL5080)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of XEN445: a potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice.
Sun S, Dean R, Jia Q, Zenova A, Zhong J, Grayson C, Xie C, Lindgren A, Samra P, Sojo L, van Heek M, Lin L, Percival D, Fu JM, Winther MD, Zhang Z.
Bioorg Med Chem (2013) 21 : 7724 -7734
PubMed 24211162 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.81 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3093392 1 6.96
CHEMBL3093394 1 6.92
CHEMBL3093393 1 6.89
CHEMBL3093395 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3093392 IC50 = 110.0 nM 6.96
CHEMBL3093394 IC50 = 120.0 nM 6.92
CHEMBL3093393 IC50 = 130.0 nM 6.89
CHEMBL3093395 IC50 = 330.0 nM 6.48