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Assay Detail

CHEMBL3076138

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

Binding
Inhibition of [3H]alpha-BGT binding to alpha1 nicotinic acetylcholine receptor in Homo sapiens (human) TE671 cells co-expressing gammaalpha1deltabeta1 nicotinic acetylcholine receptor subunits
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type TE-671
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholine receptor subunit alpha (CHEMBL4808)
Type SINGLE PROTEIN
Organism Homo sapiens

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 5.14 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6623 EPIBATIDINE 1 6.80
CHEMBL71046 DESCYANOTHIACLOPRID 1 5.22
CHEMBL72675 1 5.10
CHEMBL309804 DESNITROIMIDACLOPRID 1 4.96
CHEMBL3 NICOTINE 4.0 1 4.68
CHEMBL2270633 1 4.09
CHEMBL451432 THIACLOPRID 1 -
CHEMBL406819 IMIDACLOPRID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6623 EPIBATIDINE IC50 = 160.0 nM 6.80
CHEMBL71046 DESCYANOTHIACLOPRID IC50 = 6000.0 nM 5.22
CHEMBL72675 IC50 = 8000.0 nM 5.10
CHEMBL309804 DESNITROIMIDACLOPRID IC50 = 11000.0 nM 4.96
CHEMBL3 NICOTINE IC50 = 21000.0 nM 4.68
CHEMBL2270633 IC50 = 81000.0 nM 4.09
CHEMBL451432 THIACLOPRID IC50 = 120000.0 nM -
CHEMBL406819 IMIDACLOPRID IC50 > 300000.0 nM -