Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3762973

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

Binding
Agonist activity at 5-HT4 receptor in rat esophageal thoracic muscularis mucosae assessed as carbachol-induced contraction
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 4 (CHEMBL4317)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent.
Park JS, Im W, Choi S, Park SJ, Jung JM, Baek KS, Son HP, Sharma S, Kim IS, Jung YH.
Eur J Med Chem (2016) 109 : 75 -88
PubMed 26761776 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 6.37 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3759860 1 7.34
CHEMBL3759944 1 7.00
CHEMBL74656 REL-CISAPRIDE 1 6.99
CHEMBL3758199 1 6.60
CHEMBL3759259 1 6.42
CHEMBL3758932 1 6.17
CHEMBL3759601 1 6.15
CHEMBL3758945 1 5.98
CHEMBL3759348 1 5.81
CHEMBL3759928 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3759860 EC50 = 45.71 nM 7.34
CHEMBL3759944 EC50 = 100.0 nM 7.00
CHEMBL74656 REL-CISAPRIDE EC50 = 102.33 nM 6.99
CHEMBL3758199 EC50 = 251.19 nM 6.60
CHEMBL3759259 EC50 = 380.19 nM 6.42
CHEMBL3758932 EC50 = 676.08 nM 6.17
CHEMBL3759601 EC50 = 707.95 nM 6.15
CHEMBL3758945 EC50 = 1047.13 nM 5.98
CHEMBL3759348 EC50 = 1548.82 nM 5.81
CHEMBL3759928 EC50 = 6025.6 nM 5.22