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Assay Detail

CHEMBL4361689

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

Binding
Agonist activity at human alpha4beta2 nAChR expressed in GH4C1 cells assessed as increase in inward channel current measured after 3 to 4 days at -70 mV holding potential by patch clamp assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel N-aryl nicotinamide derivatives: Taking stock on 3,6-diazabicyclo[3.1.1]heptanes as ligands for neuronal acetylcholine receptors.
Murineddu G, Gotti C, Asproni B, Corona P, Martinello K, Plutino S, Fucile S, Temml V, Moretti M, Viani P, Schuster D, Piras S, Deligia F, Pinna GA.
Eur J Med Chem (2019) 180 : 51 -61
PubMed 31299587 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.17 6.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4460815 1 6.28
CHEMBL4532589 1 6.22
CHEMBL4441630 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4460815 EC50 = 520.0 nM 6.28
CHEMBL4532589 EC50 = 600.0 nM 6.22
CHEMBL4441630 EC50 = 1000.0 nM 6.00