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Assay Detail

CHEMBL1912301

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

Binding
Displacement of [3H]-epibatidine from alpha4beta2 nAChR in rat cortical membranes after 2 hrs by liquid scintillation counting
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Docking studies of benzylidene anabaseine interactions with α7 nicotinic acetylcholine receptor (nAChR) and acetylcholine binding proteins (AChBPs): application to the design of related α7 selective ligands.
Kombo DC, Mazurov A, Tallapragada K, Hammond PS, Chewning J, Hauser TA, Vasquez-Valdivieso M, Yohannes D, Talley TT, Taylor P, Caldwell WS.
Eur J Med Chem (2011) 46 : 5625 -5635
PubMed 21986237 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.51 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1162395 1 7.72
CHEMBL134713 GTS-21 2.0 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1162395 Ki = 19.0 nM 7.72
CHEMBL134713 GTS-21 Ki = 51.0 nM 7.29