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Assay Detail

CHEMBL1019596

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Binding
Inhibition of human carboxylesterase 1
30
Total Activities
30
Compounds Tested
2
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 29 6.55 8.10
pKi 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL362996 1 8.10
CHEMBL190672 1 7.52
CHEMBL189886 BENZIL 1 7.35
CHEMBL192180 1 7.32
CHEMBL193229 1 7.13
CHEMBL192241 1 7.11
CHEMBL193140 1 7.00
CHEMBL373345 1 6.90
CHEMBL371858 1 6.90
CHEMBL192252 1 6.80
CHEMBL192474 1 6.76
CHEMBL192139 1 6.74
CHEMBL192592 1 6.68
CHEMBL192589 1 6.67
CHEMBL365445 1 6.67
CHEMBL192410 1 6.64
CHEMBL189162 1 6.59
CHEMBL191847 1 6.53
CHEMBL372716 1 6.44
CHEMBL193180 1 6.43
CHEMBL370059 1 6.28
CHEMBL192625 1 6.27
CHEMBL371181 1 5.93
CHEMBL435109 1 5.81
CHEMBL365392 1 5.78
CHEMBL195713 1 5.77
CHEMBL191822 1 5.48
CHEMBL191513 1 5.47
CHEMBL191796 1 4.74
CHEMBL365517 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL362996 Ki = 7.943 nM 8.10
CHEMBL190672 Ki = 30.2 nM 7.52
CHEMBL189886 BENZIL Ki = 44.67 nM 7.35
CHEMBL192180 Ki = 47.86 nM 7.32
CHEMBL193229 Ki = 74.13 nM 7.13
CHEMBL192241 Ki = 77.62 nM 7.11
CHEMBL193140 Ki = 100.0 nM 7.00
CHEMBL373345 Ki = 125.89 nM 6.90
CHEMBL371858 Ki = 125.89 nM 6.90
CHEMBL192252 Ki = 158.49 nM 6.80
CHEMBL192474 Ki = 173.78 nM 6.76
CHEMBL192139 Ki = 181.97 nM 6.74
CHEMBL192592 Ki = 208.93 nM 6.68
CHEMBL192589 Ki = 213.8 nM 6.67
CHEMBL365445 Ki = 213.8 nM 6.67
CHEMBL192410 Ki = 229.09 nM 6.64
CHEMBL189162 Ki = 257.04 nM 6.59
CHEMBL191847 Ki = 295.12 nM 6.53
CHEMBL372716 Ki = 363.08 nM 6.44
CHEMBL193180 Ki = 371.54 nM 6.43
CHEMBL370059 Ki = 524.81 nM 6.28
CHEMBL192625 Ki = 537.03 nM 6.27
CHEMBL371181 Ki = 1174.9 nM 5.93
CHEMBL435109 Ki = 1548.82 nM 5.81
CHEMBL365392 Ki = 1659.59 nM 5.78
CHEMBL195713 Ki = 1698.24 nM 5.77
CHEMBL191822 Ki = 3311.31 nM 5.48
CHEMBL191513 Ki = 3388.44 nM 5.47
CHEMBL191796 Ki = 18197.01 nM 4.74
CHEMBL365517 pKi - -