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Assay Detail

CHEMBL4811722

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

Binding
Inhibition of rat alpha3beta4 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response by two-electrode voltage-clamp method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907593)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Computational and Functional Mapping of Human and Rat α6β4 Nicotinic Acetylcholine Receptors Reveals Species-Specific Ligand-Binding Motifs.
Hone AJ, Kaas Q, Kearns I, Hararah F, Gajewiak J, Christensen S, Craik DJ, McIntosh JM.
J Med Chem (2021) 64 : 1685 -1700
PubMed 33523678 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.87 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4869892 1 6.64
CHEMBL4871260 1 5.92
CHEMBL3104239 1 5.82
CHEMBL4867647 1 5.11
CHEMBL4872191 1 -
CHEMBL4865866 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4869892 IC50 = 230.0 nM 6.64
CHEMBL4871260 IC50 = 1200.0 nM 5.92
CHEMBL3104239 IC50 = 1500.0 nM 5.82
CHEMBL4867647 IC50 = 7800.0 nM 5.11
CHEMBL4872191 IC50 > 10000.0 nM -
CHEMBL4865866 IC50 > 10000.0 nM -