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Assay Detail

CHEMBL3094589

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

Binding
Binding affinity to human wild type 5-HT3A receptor expressed in HEK293 cells after 24 hrs by liquid scintillation counting analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 3A (CHEMBL1899)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exploring a potential palonosetron allosteric binding site in the 5-HT(3) receptor.
Del Cadia M, De Rienzo F, Weston DA, Thompson AJ, Menziani MC, Lummis SC.
Bioorg Med Chem (2013) 21 : 7523 -7528
PubMed 24128813 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 9.39 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1189679 PALONOSETRON 4.0 1 9.49
CHEMBL289469 GRANISETRON 4.0 1 9.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1189679 PALONOSETRON Kd = 0.32 nM 9.49
CHEMBL289469 GRANISETRON Kd = 0.53 nM 9.28