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Assay Detail

CHEMBL3082113

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

Binding
Inhibition of Sus scrofa (pig) carboxylesterase isolated from liver in using p-nitrophenyl acetate as substrate incubated for 5 min prior to substrate addition measured for 2 min by spectrophotometric analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Liver carboxylesterase (CHEMBL3383)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Synthesis of new carboxylesterase inhibitors and evaluation of potency and water solubility.
Wheelock CE, Severson TF, Hammock BD.
Chem Res Toxicol (2001) 14 : 1563 -1572
PubMed 11743738 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.29 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL89506 1 7.43
CHEMBL440542 1 7.26
CHEMBL460809 1 7.12
CHEMBL270375 1 6.92
CHEMBL270374 1 6.87
CHEMBL467450 1 6.33
CHEMBL467451 1 5.85
CHEMBL2268509 1 5.47
CHEMBL460807 1 5.25
CHEMBL449775 1 4.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL89506 IC50 = 36.8 nM 7.43
CHEMBL440542 IC50 = 54.3 nM 7.26
CHEMBL460809 IC50 = 75.3 nM 7.12
CHEMBL270375 IC50 = 119.0 nM 6.92
CHEMBL270374 IC50 = 135.0 nM 6.87
CHEMBL467450 IC50 = 473.0 nM 6.33
CHEMBL467451 IC50 = 1420.0 nM 5.85
CHEMBL2268509 IC50 = 3390.0 nM 5.47
CHEMBL460807 IC50 = 5640.0 nM 5.25
CHEMBL449775 IC50 = 39000.0 nM 4.41