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Assay Detail

CHEMBL3095194

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

Binding
Inhibition of recombinant human endothelial lipase using bis-BODIPY-FL C11-PC as substrate preincubated for 30 mins followed by substrate addition by FELA method
25
Total Activities
25
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 25 6.52 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3093304 1 7.60
CHEMBL3093396 1 7.06
CHEMBL3093307 1 6.88
CHEMBL3093309 1 6.81
CHEMBL3093302 1 6.74
CHEMBL3093401 1 6.68
CHEMBL3093395 1 6.67
CHEMBL3093393 1 6.66
CHEMBL3093308 1 6.63
CHEMBL3093306 1 6.63
CHEMBL3093392 1 6.62
CHEMBL3093394 1 6.60
CHEMBL3093303 1 6.59
CHEMBL3093391 1 6.44
CHEMBL3093305 1 6.43
CHEMBL3093398 1 6.30
CHEMBL3093399 1 6.26
CHEMBL3093397 1 6.24
CHEMBL3093400 1 6.18
CHEMBL3093405 1 6.00
CHEMBL3093301 1 5.71
CHEMBL3093404 1 5.71
CHEMBL3093402 1 -
CHEMBL3093403 1 -
CHEMBL3093300 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3093304 IC50 = 25.0 nM 7.60
CHEMBL3093396 IC50 = 88.0 nM 7.06
CHEMBL3093307 IC50 = 131.0 nM 6.88
CHEMBL3093309 IC50 = 156.0 nM 6.81
CHEMBL3093302 IC50 = 184.0 nM 6.74
CHEMBL3093401 IC50 = 209.0 nM 6.68
CHEMBL3093395 IC50 = 214.0 nM 6.67
CHEMBL3093393 IC50 = 219.0 nM 6.66
CHEMBL3093308 IC50 = 236.0 nM 6.63
CHEMBL3093306 IC50 = 236.0 nM 6.63
CHEMBL3093392 IC50 = 237.0 nM 6.62
CHEMBL3093394 IC50 = 252.0 nM 6.60
CHEMBL3093303 IC50 = 259.0 nM 6.59
CHEMBL3093391 IC50 = 366.0 nM 6.44
CHEMBL3093305 IC50 = 372.0 nM 6.43
CHEMBL3093398 IC50 = 499.0 nM 6.30
CHEMBL3093399 IC50 = 551.0 nM 6.26
CHEMBL3093397 IC50 = 570.0 nM 6.24
CHEMBL3093400 IC50 = 659.0 nM 6.18
CHEMBL3093405 IC50 = 1010.0 nM 6.00
CHEMBL3093301 IC50 = 1960.0 nM 5.71
CHEMBL3093404 IC50 = 1946.0 nM 5.71
CHEMBL3093402 IC50 > 10000.0 nM -
CHEMBL3093403 IC50 > 10000.0 nM -
CHEMBL3093300 IC50 > 10000.0 nM -