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Assay Detail

CHEMBL5351783

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

Binding
Antagonist activity at rat alpha4beta2 nACh receptor expressed in Xenopus oocyte assessed as inhibition of acetylcholine-induced response at -70 mV holding potential by voltage-clamp based electrophysiological assay
2
Total Activities
2
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; alpha4/beta2 (CHEMBL1907596)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Structure-Activity Relationships of Alanine Scan Mutants αO-Conotoxins GeXIVA[1,2] and GeXIVA[1,4].
Xu P, Zhang P, Zhu X, Wu Y, Harvey PJ, Kaas Q, Zhangsun D, Craik DJ, Luo S.
J Med Chem (2023) 66 : 10092 -10107
PubMed 37464764 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.82 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4553407 1 6.14
CHEMBL5409922 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4553407 IC50 = 730.0 nM 6.14
CHEMBL5409922 IC50 = 3150.0 nM 5.50