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Assay Detail

CHEMBL4141683

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

Binding
Inhibition of BChE (unknown origin) using thiocholine as substrate preincubated for 15 mins followed by substrate addition measured after 5 mins by Ellman's method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Arylbenzofurans from Artocarpus lakoocha and methyl ether analogs with potent cholinesterase inhibitory activity.
Namdaung U, Athipornchai A, Khammee T, Kuno M, Suksamrarn S.
Eur J Med Chem (2018) 143 : 1301 -1311
PubMed 29126732 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.68 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL465156 LAKOOCHIN B 1 7.00
CHEMBL4174409 1 6.51
CHEMBL4167602 1 6.29
CHEMBL4175479 1 6.20
CHEMBL4160372 1 6.00
CHEMBL4167195 1 5.96
CHEMBL4165259 1 5.81
CHEMBL43065 OXYRESVERATROL 1 5.53
CHEMBL659 GALANTAMINE 4.0 1 5.43
CHEMBL4175881 1 5.05
CHEMBL463296 LAKOOCHIN A 1 4.86
CHEMBL4159281 1 4.83
CHEMBL4175343 1 4.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL465156 LAKOOCHIN B IC50 = 100.0 nM 7.00
CHEMBL4174409 IC50 = 310.0 nM 6.51
CHEMBL4167602 IC50 = 510.0 nM 6.29
CHEMBL4175479 IC50 = 630.0 nM 6.20
CHEMBL4160372 IC50 = 990.0 nM 6.00
CHEMBL4167195 IC50 = 1110.0 nM 5.96
CHEMBL4165259 IC50 = 1560.0 nM 5.81
CHEMBL43065 OXYRESVERATROL IC50 = 2950.0 nM 5.53
CHEMBL659 GALANTAMINE IC50 = 3720.0 nM 5.43
CHEMBL4175881 IC50 = 8860.0 nM 5.05
CHEMBL463296 LAKOOCHIN A IC50 = 13880.0 nM 4.86
CHEMBL4159281 IC50 = 14930.0 nM 4.83
CHEMBL4175343 IC50 = 47210.0 nM 4.33