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Assay Detail

CHEMBL2210093

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

Binding
Displacement of [3H]epibatidine from alpha2beta4 nAChR after 4 hrs by liquid scintillation counting analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha2/beta4 (CHEMBL2109230)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

From α4β2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design.
Yu LF, Zhang HK, Gunosewoyo H, Kozikowski AP.
ACS Med Chem Lett (2012) 3 : 1054 -1058
PubMed 23641311 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 6.45 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3 NICOTINE 4.0 1 7.16
CHEMBL2203550 1 5.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3 NICOTINE Ki = 70.0 nM 7.16
CHEMBL2203550 Ki = 1820.0 nM 5.74