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Assay Detail

CHEMBL953569

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

Functional
Antagonist activity at human alpha-1-beta-1-gamma-delta nAChR expressed in human TE671 cells by calcium influx assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type TE-671
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Acetylcholine receptor; alpha1/beta1/delta/gamma (CHEMBL1907588)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.
Enz A, Feuerbach D, Frederiksen MU, Gentsch C, Hurth K, Müller W, Nozulak J, Roy BL.
Bioorg Med Chem Lett (2009) 19 : 1287 -1291
PubMed 19208472 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.88 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL459689 1 5.40
CHEMBL503427 1 5.20
CHEMBL454407 1 4.90
CHEMBL459900 1 4.00
CHEMBL499536 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL459689 IC50 = 3981.07 nM 5.40
CHEMBL503427 IC50 = 6309.57 nM 5.20
CHEMBL454407 IC50 = 12589.25 nM 4.90
CHEMBL459900 IC50 = 100000.0 nM 4.00
CHEMBL499536 IC50 = 125892.54 nM -