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Assay Detail

CHEMBL618929

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

Functional
5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum
31
Total Activities
29
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
EC50 31 7.73 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL158238 1 8.52
CHEMBL286136 1 8.40
CHEMBL157880 3 8.40
CHEMBL348311 1 8.36
CHEMBL39 SEROTONIN 3.0 1 8.30
CHEMBL156088 1 8.28
CHEMBL86 METOCLOPRAMIDE 4.0 1 8.24
CHEMBL349809 1 8.22
CHEMBL158147 1 8.11
CHEMBL156348 1 7.89
CHEMBL347235 1 7.85
CHEMBL156349 1 7.82
CHEMBL155631 1 7.77
CHEMBL156554 1 7.72
CHEMBL33676 1 7.57
CHEMBL156579 1 7.54
CHEMBL83954 1 7.52
CHEMBL156970 1 7.40
CHEMBL156965 1 7.40
CHEMBL59834 1 7.37
CHEMBL28992 1 7.11
CHEMBL41769 1 6.96
CHEMBL157631 1 6.95
CHEMBL288199 1 6.82
CHEMBL27846 (R)ZACOPRIDE 1 6.78
CHEMBL160705 1 6.75
CHEMBL351557 1 -
CHEMBL420969 1 -
CHEMBL156499 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL158238 EC50 = 3.0 nM 8.52
CHEMBL286136 EC50 = 4.0 nM 8.40
CHEMBL157880 EC50 = 4.0 nM 8.40
CHEMBL348311 EC50 = 4.4 nM 8.36
CHEMBL157880 EC50 = 5.0 nM 8.30
CHEMBL39 SEROTONIN EC50 = 5.0 nM 8.30
CHEMBL156088 EC50 = 5.3 nM 8.28
CHEMBL86 METOCLOPRAMIDE EC50 = 5.7 nM 8.24
CHEMBL349809 EC50 = 6.0 nM 8.22
CHEMBL158147 EC50 = 7.8 nM 8.11
CHEMBL157880 EC50 = 10.0 nM 8.00
CHEMBL156348 EC50 = 13.0 nM 7.89
CHEMBL347235 EC50 = 14.0 nM 7.85
CHEMBL156349 EC50 = 15.0 nM 7.82
CHEMBL155631 EC50 = 17.0 nM 7.77
CHEMBL156554 EC50 = 19.0 nM 7.72
CHEMBL33676 EC50 = 27.0 nM 7.57
CHEMBL156579 EC50 = 29.0 nM 7.54
CHEMBL83954 EC50 = 30.0 nM 7.52
CHEMBL156970 EC50 = 40.0 nM 7.40
CHEMBL156965 EC50 = 40.0 nM 7.40
CHEMBL59834 EC50 = 43.0 nM 7.37
CHEMBL28992 EC50 = 77.0 nM 7.11
CHEMBL41769 EC50 = 110.0 nM 6.96
CHEMBL157631 EC50 = 113.0 nM 6.95
CHEMBL288199 EC50 = 153.0 nM 6.82
CHEMBL27846 (R)ZACOPRIDE EC50 = 166.0 nM 6.78
CHEMBL160705 EC50 = 180.0 nM 6.75
CHEMBL351557 EC50 ~ 930.0 nM -
CHEMBL420969 EC50 > 1000.0 nM -
CHEMBL156499 EC50 > 1000.0 nM -