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Assay Detail

CHEMBL617976

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

Functional
Evaluated for the antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor in isolated perfused rabbit heart (RH)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 3 (5-HT3) receptor (CHEMBL2094132)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Design and synthesis of novel ligands for the 5-HT3 and the 5-HT4 receptor
Blum E, Buchheit K, Buescher H, Gamse R, Kloeppner E, Meigel H, Papageorgiou C, Waelchli R, Revesz L
Bioorg Med Chem Lett (1992) 2 : 461 -466
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 8.70 10.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56564 TROPISETRON 3.0 1 10.60
CHEMBL46 ONDANSETRON 4.0 1 10.10
CHEMBL2448558 1 8.60
CHEMBL1729 CISAPRIDE 4.0 1 7.10
CHEMBL86 METOCLOPRAMIDE 4.0 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56564 TROPISETRON Kd = 0.02512 nM 10.60
CHEMBL46 ONDANSETRON Kd = 0.07943 nM 10.10
CHEMBL2448558 Kd = 2.512 nM 8.60
CHEMBL1729 CISAPRIDE Kd = 79.43 nM 7.10
CHEMBL86 METOCLOPRAMIDE Kd = 79.43 nM 7.10