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Assay Detail

CHEMBL900100

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

Binding
Inhibition of human butyrylcholinesterase
21
Total Activities
21
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

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Planarity and constraint of the carbonyl groups in 1,2-diones are determinants for selective inhibition of human carboxylesterase 1.
Hyatt JL, Wadkins RM, Tsurkan L, Hicks LD, Hatfield MJ, Edwards CC, Ross CR, Cantalupo SA, Crundwell G, Danks MK, Guy RK, Potter PM.
J Med Chem (2007) 50 : 5727 -5734
PubMed 17941623 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 5.79 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL51931 9,10-PHENANTHRENEQUINONE 1 6.72
CHEMBL433282 1 5.78
CHEMBL52347 1,2-NAPHTHOQUINONE 1 5.64
CHEMBL235288 1 5.58
CHEMBL395653 ACENAPHTHOQUINONE 1 5.53
CHEMBL235289 1 5.51
CHEMBL189886 BENZIL 1 -
CHEMBL236337 1 -
CHEMBL236340 1 -
CHEMBL395652 1 -
CHEMBL235287 1 -
CHEMBL235903 1 -
CHEMBL235490 1 -
CHEMBL395654 1 -
CHEMBL235290 1 -
CHEMBL2367723 1 -
CHEMBL235931 1 -
CHEMBL235503 1 -
CHEMBL235504 1 -
CHEMBL362996 1 -
CHEMBL398109 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL51931 9,10-PHENANTHRENEQUINONE Ki = 190.0 nM 6.72
CHEMBL433282 Ki = 1670.0 nM 5.78
CHEMBL52347 1,2-NAPHTHOQUINONE Ki = 2290.0 nM 5.64
CHEMBL235288 Ki = 2630.0 nM 5.58
CHEMBL395653 ACENAPHTHOQUINONE Ki = 2970.0 nM 5.53
CHEMBL235289 Ki = 3100.0 nM 5.51
CHEMBL189886 BENZIL Ki > 100000.0 nM -
CHEMBL236337 Ki > 100000.0 nM -
CHEMBL236340 Ki > 100000.0 nM -
CHEMBL395652 Ki > 100000.0 nM -
CHEMBL235287 Ki > 100000.0 nM -
CHEMBL235903 Ki > 100000.0 nM -
CHEMBL235490 Ki > 100000.0 nM -
CHEMBL395654 Ki > 100000.0 nM -
CHEMBL235290 Ki > 100000.0 nM -
CHEMBL2367723 Ki > 100000.0 nM -
CHEMBL235931 Ki > 100000.0 nM -
CHEMBL235503 Ki > 100000.0 nM -
CHEMBL235504 Ki > 100000.0 nM -
CHEMBL362996 Ki > 100000.0 nM -
CHEMBL398109 Ki > 100000.0 nM -