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Assay Detail

CHEMBL752378

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

Binding
In vitro Binding affinity towards alpha-3 (PC12) nAChR was determined
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type PC-12
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-3 (CHEMBL3068)
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
Ki 4 5.32 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3 NICOTINE 4.0 1 6.66
CHEMBL111583 1 5.64
CHEMBL56564 TROPISETRON 3.0 1 4.80
CHEMBL289469 GRANISETRON 4.0 1 4.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3 NICOTINE Ki = 220.0 nM 6.66
CHEMBL111583 Ki = 2300.0 nM 5.64
CHEMBL56564 TROPISETRON Ki = 16000.0 nM 4.80
CHEMBL289469 GRANISETRON Ki = 67000.0 nM 4.17