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Assay Detail

CHEMBL4042379

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

Binding
Antagonist activity at human alpha3beta4 nAChR expressed in GH4CL cells by whole-cell patch clamp method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

From pyrrolidinyl-benzodioxane to pyrrolidinyl-pyridodioxanes, or from unselective antagonism to selective partial agonism at α4β2 nicotinic acetylcholine receptor.
Bolchi C, Bavo F, Gotti C, Fumagalli L, Fasoli F, Binda M, Mucchietto V, Sciaccaluga M, Plutino S, Fucile S, Pallavicini M.
Eur J Med Chem (2017) 125 : 1132 -1144
PubMed 27810599 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.56 5.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1186866 1 5.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1186866 IC50 = 2780.0 nM 5.56