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Assay Detail

CHEMBL3620133

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

Binding
Displacement of [3H]epibatidine from rat alpha4beta2 nAChR expressed in HEK293 cells after 1 hr by scintillation counting assay
2
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Exploration of the molecular architecture of the orthosteric binding site in the α4β2 nicotinic acetylcholine receptor with analogs of 3-(dimethylamino)butyl dimethylcarbamate (DMABC) and 1-(pyridin-3-yl)-1,4-diazepane.
Bach TB, Jensen AA, Petersen JG, Sørensen TE, Della Volpe S, Liu J, Blaazer AR, van Muijlwijk-Koezen JE, Balle T, Frølund B.
Eur J Med Chem (2015) 102 : 425 -444
PubMed 26301559 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 9.14 9.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71085 2 9.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71085 Ki = 0.72 nM 9.14
CHEMBL71085 Ki = 0.7244 nM 9.14