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Assay Detail

CHEMBL5215848

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

Binding
Inhibition of rat alpha9alpha10 nAChR expressed in xenopus oocytes assessed as inhibition of Ach- induced response incubated for 5 mins in presence of Ach stimulation by voltage-clamp based electrophysiological method
4
Total Activities
4
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

Nicotinic acetylcholine receptor alpha9/alpha10 (CHEMBL3038462)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Selective Penicillamine Substitution Enables Development of a Potent Analgesic Peptide that Acts through a Non-Opioid-Based Mechanism.
Gajewiak J, Christensen SB, Dowell C, Hararah F, Fisher F, Huynh PN, Olivera BM, McIntosh JM.
J Med Chem (2021) 64 : 9271 -9278
PubMed 34142837 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 9.00 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5219936 1 9.41
CHEMBL5220820 1 8.94
CHEMBL5220229 1 8.83
CHEMBL5220778 1 8.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5219936 IC50 = 0.39 nM 9.41
CHEMBL5220820 IC50 = 1.15 nM 8.94
CHEMBL5220229 IC50 = 1.47 nM 8.83
CHEMBL5220778 IC50 = 1.49 nM 8.83