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Assay Detail

CHEMBL1954845

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

Binding
Inhibition of human endothelial lipase overexpressed in HUVEC cells using bis-BD-PC and mono-BD-TG as substrate incubated for 10 mins prior to substrate addition by micelle assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Endothelial lipase (CHEMBL5080)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of boronic acid inhibitors of endothelial lipase.
O'Connell DP, LeBlanc DF, Cromley D, Billheimer J, Rader DJ, Bachovchin WW.
Bioorg Med Chem Lett (2012) 22 : 1397 -1401
PubMed 22225633 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.66 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL485946 1 7.00
CHEMBL1952298 1 6.70
CHEMBL1952297 1 6.50
CHEMBL1952296 1 6.33
CHEMBL1952307 1 6.00
CHEMBL1949700 1 6.00
CHEMBL1952308 1 5.96
CHEMBL1952303 1 5.96
CHEMBL1952304 1 5.96
CHEMBL1952309 1 5.89
CHEMBL1952305 1 5.85
CHEMBL1952310 1 5.80
CHEMBL1952313 1 5.77
CHEMBL1952311 1 5.54
CHEMBL1952312 1 5.51
CHEMBL1952295 1 5.40
CHEMBL1952300 1 5.30
CHEMBL1952302 1 5.22
CHEMBL1952301 1 4.96
CHEMBL1952294 1 4.72
CHEMBL1952299 1 4.66
CHEMBL140780 TOLYL BORONIC ACID 1 4.66
CHEMBL1952306 1 4.46
CHEMBL1952314 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL485946 IC50 = 100.0 nM 7.00
CHEMBL1952298 IC50 = 200.0 nM 6.70
CHEMBL1952297 IC50 = 320.0 nM 6.50
CHEMBL1952296 IC50 = 470.0 nM 6.33
CHEMBL1952307 IC50 = 1000.0 nM 6.00
CHEMBL1949700 IC50 = 1000.0 nM 6.00
CHEMBL1952308 IC50 = 1100.0 nM 5.96
CHEMBL1952303 IC50 = 1100.0 nM 5.96
CHEMBL1952304 IC50 = 1100.0 nM 5.96
CHEMBL1952309 IC50 = 1300.0 nM 5.89
CHEMBL1952305 IC50 = 1400.0 nM 5.85
CHEMBL1952310 IC50 = 1600.0 nM 5.80
CHEMBL1952313 IC50 = 1700.0 nM 5.77
CHEMBL1952311 IC50 = 2900.0 nM 5.54
CHEMBL1952312 IC50 = 3100.0 nM 5.51
CHEMBL1952295 IC50 = 4000.0 nM 5.40
CHEMBL1952300 IC50 = 5000.0 nM 5.30
CHEMBL1952302 IC50 = 6000.0 nM 5.22
CHEMBL1952301 IC50 = 11000.0 nM 4.96
CHEMBL1952294 IC50 = 19000.0 nM 4.72
CHEMBL1952299 IC50 = 22000.0 nM 4.66
CHEMBL140780 TOLYL BORONIC ACID IC50 = 22000.0 nM 4.66
CHEMBL1952306 IC50 = 35000.0 nM 4.46
CHEMBL1952314 IC50 = 300000.0 nM -