Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2185240

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

Functional
Agonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 4 (CHEMBL4317)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Identification of multiple 5-HT₄ partial agonist clinical candidates for the treatment of Alzheimer's disease.
Brodney MA, Johnson DE, Sawant-Basak A, Coffman KJ, Drummond EM, Hudson EL, Fisher KE, Noguchi H, Waizumi N, McDowell LL, Papanikolaou A, Pettersen BA, Schmidt AW, Tseng E, Stutzman-Engwall K, Rubitski DM, Vanase-Frawley MA, Grimwood S.
J Med Chem (2012) 55 : 9240 -9254
PubMed 22974325 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 9.07 9.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2152922 PF-04995274 1.0 1 9.23
CHEMBL2179583 1 9.05
CHEMBL2179582 PF-03382792 1.0 1 8.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2152922 PF-04995274 EC50 = 0.59 nM 9.23
CHEMBL2179583 EC50 = 0.9 nM 9.05
CHEMBL2179582 PF-03382792 EC50 = 1.15 nM 8.94