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Assay Detail

CHEMBL3052328

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Binding
Displacement of [3H]IMI from nicotinic acetylcholine receptor in Musca domestica (house fly) head membrane after 90 min by filter binding assay
6
Total Activities
6
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

Insect nicotinic acetylcholine receptor: conserved neonicotinoid specificity of [(3)H]imidacloprid binding site.
Zhang A, Kayser H, Maienfisch P, Casida JE.
J Neurochem (2000) 75 : 1294 -1303
PubMed 10936213 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.18 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL259727 CLOTHIANIDINE 1 8.74
CHEMBL406819 IMIDACLOPRID 1 8.59
CHEMBL148390 1 8.15
CHEMBL2251730 IMIDACLOTHIZ 1 7.92
CHEMBL2269823 1 7.85
CHEMBL2269822 DESMETHYLTHIAMETHOXAM 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL259727 CLOTHIANIDINE IC50 = 1.8 nM 8.74
CHEMBL406819 IMIDACLOPRID IC50 = 2.6 nM 8.59
CHEMBL148390 IC50 = 7.1 nM 8.15
CHEMBL2251730 IMIDACLOTHIZ IC50 = 12.0 nM 7.92
CHEMBL2269823 IC50 = 14.0 nM 7.85
CHEMBL2269822 DESMETHYLTHIAMETHOXAM IC50 = 16.0 nM 7.80