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Assay Detail

CHEMBL619416

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

Binding
Binding affinity to 5-hydroxytryptamine 3 receptor using [3H]quipazine as radioligand in rat cortex
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Serotonin 3 (5-HT3) receptor (CHEMBL2094116)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

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
Ki 4 8.23 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56564 TROPISETRON 3.0 1 9.22
CHEMBL18772 QUIPAZINE 2.0 1 9.00
CHEMBL289469 GRANISETRON 4.0 1 8.04
CHEMBL86 METOCLOPRAMIDE 4.0 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56564 TROPISETRON Ki = 0.6026 nM 9.22
CHEMBL18772 QUIPAZINE Ki = 1.0 nM 9.00
CHEMBL289469 GRANISETRON Ki = 9.12 nM 8.04
CHEMBL86 METOCLOPRAMIDE Ki = 229.09 nM 6.64