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Assay Detail

CHEMBL805837

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

Binding
Ability to block 5-HT4 receptor mediated effect of 5-HT was assessed in the guinea-pig distal colon longitudinal muscle myenteric plexus preparation (LMMP)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

5-HT4receptor antagonists : oxazolo, oxazino and oxazepino[3,2-a]indole derivatives
Gaster L, Wyman P, Ellis E, Brown A, Young T
Bioorg Med Chem Lett (1994) 4 : 667 -668
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 9.96 10.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL358119 1 10.60
CHEMBL68131 1 10.10
CHEMBL145075 1 10.00
CHEMBL143862 1 9.80
CHEMBL143426 1 9.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL358119 IC50 = 0.02512 nM 10.60
CHEMBL68131 IC50 = 0.07943 nM 10.10
CHEMBL145075 IC50 = 0.1 nM 10.00
CHEMBL143862 IC50 = 0.1585 nM 9.80
CHEMBL143426 IC50 = 0.5012 nM 9.30