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Assay Detail

CHEMBL617706

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

Binding
Inhibition of [3H]BRL-43694 binding to rat 5-hydroxytryptamine 3 receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties.
Monge A, Peña MC, Palop JA, Calderó JM, Roca J, García E, Romero G, del Río J, Lasheras B.
J Med Chem (1994) 37 : 1320 -1325
PubMed 8176710 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.22 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL46 ONDANSETRON 4.0 1 7.34
CHEMBL1729 CISAPRIDE 4.0 1 6.05
CHEMBL24909 1 6.02
CHEMBL282234 1 5.48
CHEMBL27395 1 -
CHEMBL27054 1 -
CHEMBL25396 1 -
CHEMBL26700 1 -
CHEMBL27896 1 -
CHEMBL24895 1 -
CHEMBL24854 1 -
CHEMBL281123 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL46 ONDANSETRON IC50 = 46.0 nM 7.34
CHEMBL1729 CISAPRIDE IC50 = 900.0 nM 6.05
CHEMBL24909 IC50 = 950.0 nM 6.02
CHEMBL282234 IC50 = 3300.0 nM 5.48
CHEMBL27395 IC50 > 100000.0 nM -
CHEMBL27054 IC50 > 100000.0 nM -
CHEMBL25396 IC50 > 100000.0 nM -
CHEMBL26700 IC50 > 100000.0 nM -
CHEMBL27896 IC50 > 100000.0 nM -
CHEMBL24895 IC50 > 100000.0 nM -
CHEMBL24854 IC50 > 100000.0 nM -
CHEMBL281123 IC50 > 100000.0 nM -