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Assay Detail

CHEMBL2182409

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

Binding
Inhibition of human 5HT3R
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Discovery of (2S,3R)-N-[2-(pyridin-3-ylmethyl)-1-azabicyclo[2.2.2]oct-3-yl]benzo[b]furan-2-carboxamide (TC-5619), a selective α7 nicotinic acetylcholine receptor agonist, for the treatment of cognitive disorders.
Mazurov AA, Kombo DC, Hauser TA, Miao L, Dull G, Genus JF, Fedorov NB, Benson L, Sidach S, Xiao Y, Hammond PS, James JW, Miller CH, Yohannes D.
J Med Chem (2012) 55 : 9793 -9809
PubMed 23126648 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.02 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365323 1 7.30
CHEMBL2179862 1 4.73
CHEMBL1258006 BRADANICLINE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365323 Ki = 49.8 nM 7.30
CHEMBL2179862 Ki = 18600.0 nM 4.73
CHEMBL1258006 BRADANICLINE Ki > 10000.0 nM -