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Assay Detail

CHEMBL824052

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Functional
Effective concentration that causes inhibition of alpha-7 nAChR, was determined. Values are expressed as EC50 +/- SEM.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist.
Macor JE, Gurley D, Lanthorn T, Loch J, Mack RA, Mullen G, Tran O, Wright N, Gordon JC.
Bioorg Med Chem Lett (2001) 11 : 319 -321
PubMed 11212100 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.00 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL111583 1 6.55
CHEMBL108799 1 6.24
CHEMBL56564 TROPISETRON 3.0 1 5.89
CHEMBL320963 1 5.32
CHEMBL667 ACETYLCHOLINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL111583 EC50 = 280.0 nM 6.55
CHEMBL108799 EC50 = 580.0 nM 6.24
CHEMBL56564 TROPISETRON EC50 = 1300.0 nM 5.89
CHEMBL320963 EC50 = 4800.0 nM 5.32
CHEMBL667 ACETYLCHOLINE EC50 = 230000.0 nM -