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Assay Detail

CHEMBL857027

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

Functional
Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 4 (CHEMBL1875)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Ketones related to the benzoate 5-HT4 receptor antagonist RS-23597 are high affinity partial agonists
Clark R, Jahangir A, Langston J, Weinhardt K, Miller A, Leung E, Eglen R
Bioorg Med Chem Lett (1994) 4 : 2477 -2480
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 7.41 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL83899 1 8.60
CHEMBL85251 1 8.40
CHEMBL84398 1 8.00
CHEMBL79637 1 7.90
CHEMBL82360 1 7.80
CHEMBL34291 1 7.70
CHEMBL286136 1 7.70
CHEMBL80015 1 7.40
CHEMBL83841 1 7.40
CHEMBL314489 1 7.20
CHEMBL310451 1 6.90
CHEMBL82833 1 6.90
CHEMBL420969 1 6.60
CHEMBL309655 1 6.50
CHEMBL86 METOCLOPRAMIDE 4.0 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL83899 EC50 = 2.512 nM 8.60
CHEMBL85251 EC50 = 3.981 nM 8.40
CHEMBL84398 EC50 = 10.0 nM 8.00
CHEMBL79637 EC50 = 12.59 nM 7.90
CHEMBL82360 EC50 = 15.85 nM 7.80
CHEMBL34291 EC50 = 19.95 nM 7.70
CHEMBL286136 EC50 = 19.95 nM 7.70
CHEMBL80015 EC50 = 39.81 nM 7.40
CHEMBL83841 EC50 = 39.81 nM 7.40
CHEMBL314489 EC50 = 63.1 nM 7.20
CHEMBL310451 EC50 = 125.89 nM 6.90
CHEMBL82833 EC50 = 125.89 nM 6.90
CHEMBL420969 EC50 = 251.19 nM 6.60
CHEMBL309655 EC50 = 316.23 nM 6.50
CHEMBL86 METOCLOPRAMIDE EC50 = 794.33 nM 6.10