Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2185120

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

Binding
Displacement of [3H]epibatidine from alpha3beta4 nAChR in human SH-SY5Y cells 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 Homo sapiens
Cell Type SH-SY5Y
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of 3-(5-chloro-2-furoyl)-3,7-diazabicyclo[3.3.0]octane (TC-6683, AZD1446), a novel highly selective α4β2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders.
Mazurov AA, Miao L, Bhatti BS, Strachan JP, Akireddy S, Murthy S, Kombo D, Xiao YD, Hammond P, Zhang J, Hauser TA, Jordan KG, Miller CH, Speake JD, Gatto GJ, Yohannes D.
J Med Chem (2012) 55 : 9181 -9194
PubMed 22793665 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 5.78 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3 NICOTINE 4.0 1 6.40
CHEMBL1876219 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3 NICOTINE Ki = 400.0 nM 6.40
CHEMBL1876219 Ki = 7000.0 nM 5.16