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Assay Detail

CHEMBL620719

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

Functional
Compound was evaluated in vivo for the antagonistic activity towards 5-hydroxytryptamine 3 receptor
7
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 3A (CHEMBL2411)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

New aza(nor)adamantanes are agonists at the newly identified serotonin 5-HT4 receptor and antagonists at the 5-HT3 receptor
Flynn DL, Becker DP, Spangler DP, Nosal R, Gullikson GW, Moummi C, Yang D
Bioorg Med Chem Lett (1992) 2 : 1613 -1618
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.94 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28992 1 9.64
CHEMBL2448165 1 8.92
CHEMBL2448137 1 8.41
CHEMBL296522 RENZAPRIDE 3.0 1 8.25
CHEMBL295155 2 8.05
CHEMBL1729 CISAPRIDE 4.0 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28992 Ki = 0.23 nM 9.64
CHEMBL2448165 Ki = 1.2 nM 8.92
CHEMBL2448137 Ki = 3.9 nM 8.41
CHEMBL296522 RENZAPRIDE Ki = 5.6 nM 8.25
CHEMBL295155 Ki = 9.0 nM 8.05
CHEMBL295155 Ki = 336.0 nM 6.47
CHEMBL1729 CISAPRIDE Ki = 1500.0 nM 5.82