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Assay Detail

CHEMBL1019602

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Binding
Inhibition of human carboxylesterase 1 after 24 hrs
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Liver carboxylesterase 1 (CHEMBL2265)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Comparison of benzil and trifluoromethyl ketone (TFK)-mediated carboxylesterase inhibition using classical and 3D-quantitative structure-activity relationship analysis.
Harada T, Nakagawa Y, Wadkins RM, Potter PM, Wheelock CE.
Bioorg Med Chem (2009) 17 : 149 -164
PubMed 19062296 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.78 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL467451 1 9.52
CHEMBL467450 1 9.40
CHEMBL463556 1 9.40
CHEMBL464002 1 9.30
CHEMBL460807 1 9.22
CHEMBL460806 1 9.22
CHEMBL449775 1 9.15
CHEMBL449475 1 9.00
CHEMBL86668 1 8.64
CHEMBL460808 1 8.48
CHEMBL270374 1 8.40
CHEMBL89506 1 8.38
CHEMBL440542 1 8.28
CHEMBL402615 1 8.27
CHEMBL510996 1 8.22
CHEMBL460809 1 8.19
CHEMBL270375 1 8.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL467451 Ki = 0.302 nM 9.52
CHEMBL467450 Ki = 0.3981 nM 9.40
CHEMBL463556 Ki = 0.3981 nM 9.40
CHEMBL464002 Ki = 0.5012 nM 9.30
CHEMBL460807 Ki = 0.6026 nM 9.22
CHEMBL460806 Ki = 0.6026 nM 9.22
CHEMBL449775 Ki = 0.7079 nM 9.15
CHEMBL449475 Ki = 1.0 nM 9.00
CHEMBL86668 Ki = 2.291 nM 8.64
CHEMBL460808 Ki = 3.311 nM 8.48
CHEMBL270374 Ki = 3.981 nM 8.40
CHEMBL89506 Ki = 4.169 nM 8.38
CHEMBL440542 Ki = 5.248 nM 8.28
CHEMBL402615 Ki = 5.37 nM 8.27
CHEMBL510996 Ki = 6.026 nM 8.22
CHEMBL460809 Ki = 6.457 nM 8.19
CHEMBL270375 Ki = 7.413 nM 8.13