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Assay Detail

CHEMBL619759

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

Functional
5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum
15
Total Activities
14
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

New esters of 4-amino-5-chloro-2-methoxybenzoic acid as potent agonists and antagonists for 5-HT4 receptors.
Yang D, Soulier JL, Sicsic S, Mathé-Allainmat M, Brémont B, Croci T, Cardamone R, Aureggi G, Langlois M.
J Med Chem (1997) 40 : 608 -621
PubMed 9046352 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.08 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL155917 2 7.96
CHEMBL33884 1 7.89
CHEMBL41769 1 7.52
CHEMBL287045 1 7.11
CHEMBL123377 1 7.00
CHEMBL160237 1 7.00
CHEMBL155682 1 6.82
CHEMBL156970 1 6.70
CHEMBL351570 1 6.52
CHEMBL288199 1 6.35
CHEMBL160705 1 6.22
CHEMBL156499 1 -
CHEMBL420969 1 -
CHEMBL156088 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL155917 IC50 = 11.0 nM 7.96
CHEMBL155917 IC50 = 13.0 nM 7.89
CHEMBL33884 IC50 = 13.0 nM 7.89
CHEMBL41769 IC50 = 30.0 nM 7.52
CHEMBL287045 IC50 = 77.0 nM 7.11
CHEMBL123377 IC50 = 100.0 nM 7.00
CHEMBL160237 IC50 = 100.0 nM 7.00
CHEMBL155682 IC50 = 150.0 nM 6.82
CHEMBL156970 IC50 = 200.0 nM 6.70
CHEMBL351570 IC50 = 300.0 nM 6.52
CHEMBL288199 IC50 = 450.0 nM 6.35
CHEMBL160705 IC50 = 600.0 nM 6.22
CHEMBL156499 IC50 > 1000.0 nM -
CHEMBL420969 IC50 > 1000.0 nM -
CHEMBL156088 IC50 ~ 20.0 nM -