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Assay Detail

CHEMBL3067866

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

Binding
Binding affinity to recombinant Gallus gallus (chicken) alpha4beta2 nicotinic acetylcholine receptor assessed as [3H]NIC binding by radioligand binding assay
8
Total Activities
8
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

Unique neonicotinoid binding conformations conferring selective receptor interactions.
Tomizawa M, Casida JE.
J Agric Food Chem (2011) 59 : 2825 -2828
PubMed 21341671 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.92 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6623 EPIBATIDINE 1 11.00
CHEMBL71046 DESCYANOTHIACLOPRID 1 8.92
CHEMBL3 NICOTINE 4.0 1 8.72
CHEMBL309804 DESNITROIMIDACLOPRID 1 8.66
CHEMBL1391421 1 7.22
CHEMBL451432 THIACLOPRID 1 6.62
CHEMBL265941 ACETAMIPRID 1 6.17
CHEMBL406819 IMIDACLOPRID 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6623 EPIBATIDINE Ki = 0.01 nM 11.00
CHEMBL71046 DESCYANOTHIACLOPRID Ki = 1.2 nM 8.92
CHEMBL3 NICOTINE Ki = 1.9 nM 8.72
CHEMBL309804 DESNITROIMIDACLOPRID Ki = 2.2 nM 8.66
CHEMBL1391421 Ki = 60.0 nM 7.22
CHEMBL451432 THIACLOPRID Ki = 240.0 nM 6.62
CHEMBL265941 ACETAMIPRID Ki = 680.0 nM 6.17
CHEMBL406819 IMIDACLOPRID Ki = 970.0 nM 6.01