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Assay Detail

CHEMBL3076134

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

Binding
Inhibition of [3H]nicotine binding to alpha4 nicotinic acetylcholine receptor in Mus musculus (mouse) M10 cells co-expressing beta2 nicotinic acetylcholine receptor subunits
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type M10
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-4 (CHEMBL4457)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Neonicotinoid insecticides: molecular features conferring selectivity for insect versus mammalian nicotinic receptors.
Tomizawa M, Lee DL, Casida JE.
J Agric Food Chem (2000) 48 : 6016 -6024
PubMed 11312774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.83 10.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6623 EPIBATIDINE 1 10.43
CHEMBL72675 1 8.85
CHEMBL71046 DESCYANOTHIACLOPRID 1 8.36
CHEMBL3 NICOTINE 4.0 1 8.15
CHEMBL309804 DESNITROIMIDACLOPRID 1 8.09
CHEMBL2270633 1 7.10
CHEMBL451432 THIACLOPRID 1 6.07
CHEMBL406819 IMIDACLOPRID 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6623 EPIBATIDINE IC50 = 0.037 nM 10.43
CHEMBL72675 IC50 = 1.4 nM 8.85
CHEMBL71046 DESCYANOTHIACLOPRID IC50 = 4.4 nM 8.36
CHEMBL3 NICOTINE IC50 = 7.0 nM 8.15
CHEMBL309804 DESNITROIMIDACLOPRID IC50 = 8.2 nM 8.09
CHEMBL2270633 IC50 = 80.0 nM 7.10
CHEMBL451432 THIACLOPRID IC50 = 860.0 nM 6.07
CHEMBL406819 IMIDACLOPRID IC50 = 2600.0 nM 5.58