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Assay Detail

CHEMBL947458

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

Binding
Displacement of [3H]nicotine from chick alpha4beta2 nAChR
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Gallus gallus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-4 (CHEMBL5569)
Type SINGLE PROTEIN
Organism Gallus gallus

Publication

Potency and selectivity of trifluoroacetylimino and pyrazinoylimino nicotinic insecticides and their fit at a unique binding site niche.
Tomizawa M, Kagabu S, Ohno I, Durkin KA, Casida JE.
J Med Chem (2008) 51 : 4213 -4218
PubMed 18570364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.00 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL518310 1 6.30
CHEMBL451432 THIACLOPRID 1 6.07
CHEMBL494278 1 6.05
CHEMBL406819 IMIDACLOPRID 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL518310 IC50 = 500.0 nM 6.30
CHEMBL451432 THIACLOPRID IC50 = 860.0 nM 6.07
CHEMBL494278 IC50 = 900.0 nM 6.05
CHEMBL406819 IMIDACLOPRID IC50 = 2600.0 nM 5.58