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Assay Detail

CHEMBL953570

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

Functional
Antagonist activity at human 5HT3 receptor by calcium influx assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 3A (CHEMBL1899)
Type SINGLE PROTEIN
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 4.40 4.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL499536 1 4.70
CHEMBL459689 1 4.60
CHEMBL503427 1 4.30
CHEMBL459900 1 4.00
CHEMBL454407 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL499536 IC50 = 19952.62 nM 4.70
CHEMBL459689 IC50 = 25118.86 nM 4.60
CHEMBL503427 IC50 = 50118.72 nM 4.30
CHEMBL459900 IC50 = 100000.0 nM 4.00
CHEMBL454407 IC50 = 251188.64 nM -