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Assay Detail

CHEMBL2383620

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

Binding
Antagonist activity at (alpha4beta2)2beta2 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Oocyte
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Neonicotinic analogues: selective antagonists for α4β2 nicotinic acetylcholine receptors.
Faundez-Parraguez M, Farias-Rabelo N, Gonzalez-Gutierrez JP, Etcheverry-Berrios A, Alzate-Morales J, Adasme-Carreño F, Varas R, Bermudez I, Iturriaga-Vasquez P.
Bioorg Med Chem (2013) 21 : 2687 -2694
PubMed 23561269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.48 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL293950 1 6.39
CHEMBL2381568 1 5.60
CHEMBL2381563 1 5.44
CHEMBL2381570 1 5.37
CHEMBL2381566 1 4.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL293950 IC50 = 410.0 nM 6.39
CHEMBL2381568 IC50 = 2500.0 nM 5.60
CHEMBL2381563 IC50 = 3600.0 nM 5.44
CHEMBL2381570 IC50 = 4300.0 nM 5.37
CHEMBL2381566 IC50 = 25800.0 nM 4.59