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Assay Detail

CHEMBL3081642

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

Binding
Displacement of [3HIMI from nicotinic acetylcholine receptor in Musca domestica (house fly) head membranes incubated for 60 min by liquid scintillation counting method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Musca domestica
Tissue Head
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nicotinic acetylcholine receptor alpha 5 subunit (CHEMBL2366408)
Type SINGLE PROTEIN
Organism Musca domestica

Publication

Asymmetric chloronicotinyl insecticide, 1-[1-(6-chloro-3-pyridyl)ethyl]-2-nitroiminoimidazolidine: preparation, resolution and biological activities toward insects and their nerve preparations.
Kagabu S, Kiriyama K, Nishiwaki H, Kumamoto Y, Tada T, Nishimura K.
Biosci Biotechnol Biochem (2003) 67 : 980 -988
PubMed 12834274 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.21 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL406819 IMIDACLOPRID 1 7.70
CHEMBL2272996 (S)-METHYL-IMIDACLOPRID 1 6.72
CHEMBL2272995 (R,S)-METHYL-IMIDACLOPRID 1 6.68
CHEMBL2272997 (R)-METHYL-IMIDACLOPRID 1 6.02
CHEMBL298826 (-)-EPIBATIDINE 1 5.87
CHEMBL298517 (+)-EPIBATIDINE 1 5.55
CHEMBL3 NICOTINE 4.0 1 4.92
CHEMBL9732 R-NICOTINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL406819 IMIDACLOPRID IC50 = 20.0 nM 7.70
CHEMBL2272996 (S)-METHYL-IMIDACLOPRID IC50 = 190.0 nM 6.72
CHEMBL2272995 (R,S)-METHYL-IMIDACLOPRID IC50 = 210.0 nM 6.68
CHEMBL2272997 (R)-METHYL-IMIDACLOPRID IC50 = 950.0 nM 6.02
CHEMBL298826 (-)-EPIBATIDINE IC50 = 1340.0 nM 5.87
CHEMBL298517 (+)-EPIBATIDINE IC50 = 2790.0 nM 5.55
CHEMBL3 NICOTINE IC50 = 11900.0 nM 4.92
CHEMBL9732 R-NICOTINE IC50 = 422000.0 nM -