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Assay Detail

CHEMBL619756

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

Functional
5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design of a potent 5-HT4 receptor agonist with nanomolar affinity
Langlois M, Zhang L, Bre mont B, Shen S, Manara L, Croci T
Bioorg Med Chem Lett (1994) 4 : 1433 -1436
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.03 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41769 1 7.52
CHEMBL34224 1 7.22
CHEMBL288199 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41769 IC50 = 30.0 nM 7.52
CHEMBL34224 IC50 = 60.0 nM 7.22
CHEMBL288199 IC50 = 450.0 nM 6.35