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Assay Detail

CHEMBL618130

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

Binding
In vitro Binding affinity towards 5-hydroxytryptamine 3 receptor was determined
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 3 (5-HT3) receptor (CHEMBL2094132)
Type PROTEIN COMPLEX GROUP
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 7 7.58 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL108799 1 8.96
CHEMBL56564 TROPISETRON 3.0 1 8.28
CHEMBL111583 1 8.14
CHEMBL320963 1 8.00
CHEMBL46 ONDANSETRON 4.0 1 7.92
CHEMBL289469 GRANISETRON 4.0 1 7.62
CHEMBL3 NICOTINE 4.0 1 4.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL108799 Ki = 1.1 nM 8.96
CHEMBL56564 TROPISETRON Ki = 5.3 nM 8.28
CHEMBL111583 Ki = 7.2 nM 8.14
CHEMBL320963 Ki = 10.0 nM 8.00
CHEMBL46 ONDANSETRON Ki = 12.0 nM 7.92
CHEMBL289469 GRANISETRON Ki = 24.0 nM 7.62
CHEMBL3 NICOTINE Ki = 71000.0 nM 4.15