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Assay Detail

CHEMBL4381866

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

Binding
Antagonist activity at rat alpha4beta2 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of Ach-induced response at -70 mV holding potential by two electrode voltage-clamp assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Structure and Activity Studies of Disulfide-Deficient Analogues of αO-Conotoxin GeXIVA.
Xu P, Kaas Q, Wu Y, Zhu X, Li X, Harvey PJ, Zhangsun D, Craik DJ, Luo S.
J Med Chem (2020) 63 : 1564 -1575
PubMed 31986036 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.37 5.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4460879 1 5.37
CHEMBL4553407 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4460879 IC50 = 4290.0 nM 5.37
CHEMBL4553407 IC50 = 4290.0 nM 5.37