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Assay Detail

CHEMBL619025

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

Functional
Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 receptor using the rat tunica muscularis mucosae (TMM) esophagus strip assay
7
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 4 (CHEMBL4317)
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
EC50 7 6.64 7.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2448165 1 7.29
CHEMBL1729 CISAPRIDE 4.0 1 7.26
CHEMBL296522 RENZAPRIDE 3.0 1 7.01
CHEMBL28992 1 6.69
CHEMBL295155 2 6.58
CHEMBL2448137 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2448165 EC50 = 51.3 nM 7.29
CHEMBL1729 CISAPRIDE EC50 = 55.0 nM 7.26
CHEMBL296522 RENZAPRIDE EC50 = 98.0 nM 7.01
CHEMBL28992 EC50 = 203.0 nM 6.69
CHEMBL295155 EC50 = 262.0 nM 6.58
CHEMBL295155 EC50 = 538.0 nM 6.27
CHEMBL2448137 EC50 = 3870.0 nM 5.41