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Assay Detail

CHEMBL619783

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

Binding
Compound was evaluated for its binding affinity for 5-hydroxytryptamine 3 receptor by measuring displacement [3H]GR-65630 in rat cerebral cortex
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

5-HT3 antagonists derived from aminopyridazine-type muscarinic M1 agonists.
Rival Y, Hoffmann R, Didier B, Rybaltchenko V, Bourguignon JJ, Wermuth CG.
J Med Chem (1998) 41 : 311 -317
PubMed 9464362 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.13 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289469 GRANISETRON 4.0 1 9.22
CHEMBL18772 QUIPAZINE 2.0 1 8.85
CHEMBL56564 TROPISETRON 3.0 1 8.49
CHEMBL46 ONDANSETRON 4.0 1 8.48
CHEMBL2107804 BEMESETRON 2.0 1 7.27
CHEMBL86 METOCLOPRAMIDE 4.0 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289469 GRANISETRON Ki = 0.6 nM 9.22
CHEMBL18772 QUIPAZINE Ki = 1.4 nM 8.85
CHEMBL56564 TROPISETRON Ki = 3.2 nM 8.49
CHEMBL46 ONDANSETRON Ki = 3.3 nM 8.48
CHEMBL2107804 BEMESETRON Ki = 54.0 nM 7.27
CHEMBL86 METOCLOPRAMIDE Ki = 348.0 nM 6.46