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Assay Detail

CHEMBL5325636

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

Binding
Antagonist activity at human alpha3beta4 nAChRs expressed in HEK293 cells assessed as inhibition of (+/-)-epibatidine-induced Ca+2 influx incubated for 5 mins by FLIPR analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

What We Have Gained from Ibogaine: α3β4 Nicotinic Acetylcholine Receptor Inhibitors as Treatments for Substance Use Disorders.
Straub CJ, Rusali LE, Kremiller KM, Riley AP.
J Med Chem (2023) 66 : 107 -121
PubMed 36440853 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.93 6.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1215855 1 6.02
CHEMBL5440131 1 5.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1215855 IC50 = 950.0 nM 6.02
CHEMBL5440131 IC50 = 1470.0 nM 5.83