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Assay Detail

CHEMBL617981

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

Binding
In vitro displacement of [3H]-LY 278584 from rat cerebral cortex 5-hydroxytryptamine 3 receptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Novel benzimidazole-4-carboxylic acid derivatives as potent and selective 5-HT3 receptor ligands
Lopez-Rodriguez ML, Morcillo MJ, Benhamu B, Riaguas MD
Bioorg Med Chem Lett (1996) 6 : 1195 -1198
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.97 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19006 1 9.54
CHEMBL18041 ZACOPRIDE 2.0 1 9.38
CHEMBL56564 TROPISETRON 3.0 1 8.89
CHEMBL18274 1 8.43
CHEMBL19039 1 8.31
CHEMBL279850 1 8.21
CHEMBL416172 1 8.03
CHEMBL18769 1 7.53
CHEMBL277543 1 6.89
CHEMBL18473 1 6.84
CHEMBL19022 1 6.81
CHEMBL275356 1 6.73
CHEMBL279823 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19006 Ki = 0.29 nM 9.54
CHEMBL18041 ZACOPRIDE Ki = 0.42 nM 9.38
CHEMBL56564 TROPISETRON Ki = 1.28 nM 8.89
CHEMBL18274 Ki = 3.7 nM 8.43
CHEMBL19039 Ki = 4.9 nM 8.31
CHEMBL279850 Ki = 6.1 nM 8.21
CHEMBL416172 Ki = 9.3 nM 8.03
CHEMBL18769 Ki = 29.5 nM 7.53
CHEMBL277543 Ki = 129.0 nM 6.89
CHEMBL18473 Ki = 145.0 nM 6.84
CHEMBL19022 Ki = 154.0 nM 6.81
CHEMBL275356 Ki = 185.0 nM 6.73
CHEMBL279823 Ki > 1000.0 nM -