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Assay Detail

CHEMBL617970

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

Binding
Potency at neuronal 5-hydroxytryptamine 3 receptor in the rabbit heart
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Conformation-activity relationship study of 5-HT3 receptor antagonists and a definition of a model for this receptor site.
Hibert MF, Hoffmann R, Miller RC, Carr AA.
J Med Chem (1990) 33 : 1594 -1600
PubMed 2342053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 9.00 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289469 GRANISETRON 4.0 1 10.70
CHEMBL46 ONDANSETRON 4.0 1 10.10
CHEMBL2107804 BEMESETRON 2.0 1 9.30
CHEMBL40883 1 9.00
CHEMBL301281 1 7.70
CHEMBL1947052 1 7.20
CHEMBL56564 TROPISETRON 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289469 GRANISETRON Kd = 0.01995 nM 10.70
CHEMBL46 ONDANSETRON Kd = 0.07943 nM 10.10
CHEMBL2107804 BEMESETRON Kd = 0.5012 nM 9.30
CHEMBL40883 Kd = 1.0 nM 9.00
CHEMBL301281 Kd = 19.95 nM 7.70
CHEMBL1947052 Kd = 63.1 nM 7.20
CHEMBL56564 TROPISETRON Kd = 106.0 nM -