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Assay Detail

CHEMBL4265356

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

Binding
Antagonist activity at human alpha7 nACHR expressed in xenopous laevis oocyte assessed as inhibition of ACh-induced channel current after 5 mins at -70 mV holding potential by two electrode voltage clamp method
7
Total Activities
7
Compounds Tested
1
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

Potent Antiglioblastoma Agents by Hybridizing the Onium-Alkyloxy-Stilbene Based Structures of an α7-nAChR, α9-nAChR Antagonist and of a Pro-Oxidant Mitocan.
Bavo F, Pucci S, Fasoli F, Lammi C, Moretti M, Mucchietto V, Lattuada D, Viani P, De Palma C, Budriesi R, Corradini I, Dowell C, McIntosh JM, Clementi F, Bolchi C, Gotti C, Pallavicini M.
J Med Chem (2018) 61 : 10531 -10544
PubMed 30403486 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.58 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4291079 1 8.19
CHEMBL4293646 1 7.91
CHEMBL4280452 1 7.61
CHEMBL1257065 STILONIUM IODIDE 2.0 1 7.39
CHEMBL4287656 1 7.33
CHEMBL4285772 1 7.04
CHEMBL4276776 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4291079 IC50 = 6.5 nM 8.19
CHEMBL4293646 IC50 = 12.3 nM 7.91
CHEMBL4280452 IC50 = 24.3 nM 7.61
CHEMBL1257065 STILONIUM IODIDE IC50 = 41.0 nM 7.39
CHEMBL4287656 IC50 = 47.0 nM 7.33
CHEMBL4285772 IC50 = 92.0 nM 7.04
CHEMBL4276776 IC50 > 10000.0 nM -