Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4381855

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

Binding
Antagonist activity at rat alpha9alpha10 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of Ach-induced response at -70 mV holding potential by two electrode voltage-clamp assay
17
Total Activities
15
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

Nicotinic acetylcholine receptor alpha9/alpha10 (CHEMBL3038462)
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 17 7.95 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4553407 2 8.30
CHEMBL4446775 1 8.30
CHEMBL4460879 2 8.30
CHEMBL4534950 1 8.30
CHEMBL4460411 1 8.21
CHEMBL4450578 1 7.96
CHEMBL4525995 1 7.92
CHEMBL4554920 1 7.89
CHEMBL4540592 1 7.89
CHEMBL4522506 1 7.85
CHEMBL4463717 1 7.85
CHEMBL4448288 1 7.80
CHEMBL4577696 1 7.77
CHEMBL4455583 1 7.68
CHEMBL4473421 1 7.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4460879 IC50 = 5.0 nM 8.30
CHEMBL4534950 IC50 = 5.0 nM 8.30
CHEMBL4553407 IC50 = 5.0 nM 8.30
CHEMBL4446775 IC50 = 5.0 nM 8.30
CHEMBL4460411 IC50 = 6.1 nM 8.21
CHEMBL4450578 IC50 = 11.0 nM 7.96
CHEMBL4525995 IC50 = 12.0 nM 7.92
CHEMBL4460879 IC50 = 12.0 nM 7.92
CHEMBL4554920 IC50 = 13.0 nM 7.89
CHEMBL4540592 IC50 = 13.0 nM 7.89
CHEMBL4522506 IC50 = 14.0 nM 7.85
CHEMBL4463717 IC50 = 14.0 nM 7.85
CHEMBL4553407 IC50 = 16.0 nM 7.80
CHEMBL4448288 IC50 = 16.0 nM 7.80
CHEMBL4577696 IC50 = 17.0 nM 7.77
CHEMBL4455583 IC50 = 21.0 nM 7.68
CHEMBL4473421 IC50 = 36.0 nM 7.44