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Assay Detail

CHEMBL2061925

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

Functional
Agonist activity at 5HT4 receptor in guinea pig colon assessed as longitudinal muscle plexus contraction
4
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Colon
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 4 (CHEMBL5017)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Discovery, oral pharmacokinetics and in vivo efficacy of a highly selective 5-HT4 receptor agonist: clinical compound TD-2749.
Long DD, Armstrong SR, Beattie DT, Choi SK, Fatheree PR, Gendron RA, Goldblum AA, Humphrey PP, Marquess DG, Shaw JP, Smith JA, Derek Turner S, Vickery RG.
Bioorg Med Chem Lett (2012) 22 : 4849 -4853
PubMed 22683222 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.07 8.20
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76370 TEGASEROD 4.0 1 8.20
CHEMBL2059590 2 8.00
CHEMBL39 SEROTONIN 3.0 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76370 TEGASEROD EC50 = 6.31 nM 8.20
CHEMBL2059590 EC50 = 10.0 nM 8.00
CHEMBL39 SEROTONIN EC50 = 10.0 nM 8.00
CHEMBL2059590 Activity - -