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Assay Detail

CHEMBL617806

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

Binding
Binding affinity was evaluated in vitro by displacement of [3H]zacopride radioligand from 5-hydroxytryptamine 3 receptor
7
Total Activities
7
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

Azaheteroaromatic ethers as carbonyl bioisosteres. Synthesis and evaluation of a novel class of 5-HT3 receptor antagonists
Cliffe IA, Brammer N, Middlefell V, Swaminathan P, White AC
Bioorg Med Chem Lett (1992) 2 : 245 -248
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.96 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18041 ZACOPRIDE 2.0 1 8.66
CHEMBL56564 TROPISETRON 3.0 1 8.64
CHEMBL82138 1 8.16
CHEMBL46 ONDANSETRON 4.0 1 8.15
CHEMBL84290 1 7.40
CHEMBL2107804 BEMESETRON 2.0 1 7.37
CHEMBL310107 1 7.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18041 ZACOPRIDE IC50 = 2.2 nM 8.66
CHEMBL56564 TROPISETRON IC50 = 2.3 nM 8.64
CHEMBL82138 IC50 = 6.9 nM 8.16
CHEMBL46 ONDANSETRON IC50 = 7.1 nM 8.15
CHEMBL84290 IC50 = 39.6 nM 7.40
CHEMBL2107804 BEMESETRON IC50 = 42.6 nM 7.37
CHEMBL310107 IC50 = 48.0 nM 7.32