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

CHEMBL859606

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

Functional
Agonism at 5HT4 receptor in rat tunica muscularis mucosa
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.
Becker DP, Flynn DL, Moormann AE, Nosal R, Villamil CI, Loeffler R, Gullikson GW, Moummi C, Yang DC.
J Med Chem (2006) 49 : 1125 -1139
PubMed 16451077 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 7.19 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201621 1 8.82
CHEMBL34291 1 7.78
CHEMBL2448165 1 7.29
CHEMBL1729 CISAPRIDE 4.0 1 7.26
CHEMBL2448558 1 7.01
CHEMBL199866 1 6.89
CHEMBL201019 1 6.71
CHEMBL37333 1 6.49
CHEMBL201414 1 6.43
CHEMBL202434 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201621 EC50 = 1.5 nM 8.82
CHEMBL34291 EC50 = 16.5 nM 7.78
CHEMBL2448165 EC50 = 51.0 nM 7.29
CHEMBL1729 CISAPRIDE EC50 = 54.7 nM 7.26
CHEMBL2448558 EC50 = 98.0 nM 7.01
CHEMBL199866 EC50 = 129.0 nM 6.89
CHEMBL201019 EC50 = 195.0 nM 6.71
CHEMBL37333 EC50 = 323.0 nM 6.49
CHEMBL201414 EC50 = 374.2 nM 6.43
CHEMBL202434 EC50 > 10000.0 nM -