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Assay Detail

CHEMBL828284

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

Binding
Inhibition constant against human liver carboxylesterase 1 (hCE1) using nitrophenyl acetate (o-NPA) as substrate
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases.
Wadkins RM, Hyatt JL, Wei X, Yoon KJ, Wierdl M, Edwards CC, Morton CL, Obenauer JC, Damodaran K, Beroza P, Danks MK, Potter PM.
J Med Chem (2005) 48 : 2906 -2915
PubMed 15828829 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 61 6.24 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL362996 1 8.10
CHEMBL189886 BENZIL 1 7.35
CHEMBL192180 1 7.32
CHEMBL193229 1 7.13
CHEMBL192241 1 7.11
CHEMBL192627 CHLORANIL 1 7.08
CHEMBL365161 1 7.05
CHEMBL193140 1 7.00
CHEMBL371858 1 6.90
CHEMBL192252 1 6.80
CHEMBL192474 1 6.76
CHEMBL192139 1 6.74
CHEMBL192589 1 6.67
CHEMBL192410 1 6.64
CHEMBL191847 1 6.53
CHEMBL193180 1 6.43
CHEMBL370059 1 6.28
CHEMBL192625 1 6.27
CHEMBL435109 1 5.81
CHEMBL365392 1 5.78
CHEMBL195713 1 5.77
CHEMBL191822 1 5.48
CHEMBL191513 1 5.47
CHEMBL192258 1 5.28
CHEMBL364729 1 5.26
CHEMBL190677 BENZOIN -1.0 1 5.14
CHEMBL364734 1 4.82
CHEMBL364588 1 4.77
CHEMBL191796 1 4.74
CHEMBL371523 DIBENZOYLMETHANE -1.0 1 4.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL362996 Ki = 8.0 nM 8.10
CHEMBL189886 BENZIL Ki = 45.1 nM 7.35
CHEMBL192180 Ki = 47.4 nM 7.32
CHEMBL193229 Ki = 73.5 nM 7.13
CHEMBL192241 Ki = 77.6 nM 7.11
CHEMBL192627 CHLORANIL Ki = 83.9 nM 7.08
CHEMBL365161 Ki = 88.6 nM 7.05
CHEMBL193140 Ki = 99.1 nM 7.00
CHEMBL371858 Ki = 125.0 nM 6.90
CHEMBL192252 Ki = 160.0 nM 6.80
CHEMBL192474 Ki = 175.0 nM 6.76
CHEMBL192139 Ki = 182.0 nM 6.74
CHEMBL192589 Ki = 215.0 nM 6.67
CHEMBL192410 Ki = 231.0 nM 6.64
CHEMBL191847 Ki = 295.0 nM 6.53
CHEMBL193180 Ki = 372.0 nM 6.43
CHEMBL370059 Ki = 524.0 nM 6.28
CHEMBL192625 Ki = 532.0 nM 6.27
CHEMBL435109 Ki = 1540.0 nM 5.81
CHEMBL365392 Ki = 1650.0 nM 5.78
CHEMBL195713 Ki = 1690.0 nM 5.77
CHEMBL191822 Ki = 3300.0 nM 5.48
CHEMBL191513 Ki = 3410.0 nM 5.47
CHEMBL192258 Ki = 5270.0 nM 5.28
CHEMBL364729 Ki = 5440.0 nM 5.26
CHEMBL190677 BENZOIN Ki = 7250.0 nM 5.14
CHEMBL364734 Ki = 15300.0 nM 4.82
CHEMBL364588 Ki = 16900.0 nM 4.77
CHEMBL191796 Ki = 18100.0 nM 4.74
CHEMBL371523 DIBENZOYLMETHANE Ki = 26000.0 nM 4.58
CHEMBL191800 Ki > 100000.0 nM -
CHEMBL365129 Ki > 100000.0 nM -
CHEMBL284028 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE Ki > 100000.0 nM -
CHEMBL192712 Ki > 100000.0 nM -
CHEMBL8320 BENZOQUINONE Ki > 100000.0 nM -
CHEMBL193228 Ki > 100000.0 nM -
CHEMBL190496 Ki > 100000.0 nM -
CHEMBL189988 BENZYLSULFONYLBENZENE Ki > 100000.0 nM -
CHEMBL365809 BUTANEDIONE Ki > 100000.0 nM -
CHEMBL191676 Ki > 100000.0 nM -
CHEMBL372856 Ki > 100000.0 nM -
CHEMBL192657 Ki > 100000.0 nM -
CHEMBL192039 Ki > 100000.0 nM -
CHEMBL366205 Ki > 100000.0 nM -
CHEMBL425192 Ki > 100000.0 nM -
CHEMBL365517 Ki > 100000.0 nM -
CHEMBL90039 BENZOPHENONE Ki > 100000.0 nM -
CHEMBL191739 Ki > 100000.0 nM -
CHEMBL192648 Ki > 100000.0 nM -
CHEMBL365982 Ki > 100000.0 nM -