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Assay Detail

CHEMBL3375970

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

Binding
Inhibition of human alpha7 nAChR expressed in Xenopus oocytes assessed as inhibition of Ach-evoked current after 5 mins by voltage-clamp technique
3
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dicarba analogues of α-conotoxin RgIA. Structure, stability, and activity at potential pain targets.
Chhabra S, Belgi A, Bartels P, van Lierop BJ, Robinson SD, Kompella SN, Hung A, Callaghan BP, Adams DJ, Robinson AJ, Norton RS.
J Med Chem (2014) 57 : 9933 -9944
PubMed 25393758 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.44 5.48
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1836968 2 5.48
CHEMBL3355199 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1836968 IC50 = 3300.0 nM 5.48
CHEMBL3355199 IC50 = 3950.0 nM 5.40
CHEMBL1836968 Inhibition - % -