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Assay Detail

CHEMBL5223861

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

Binding
Partial agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Discovery and Preclinical Characterization of Usmarapride (SUVN-D4010): A Potent, Selective 5-HT<sub>4</sub> Receptor Partial Agonist for the Treatment of Cognitive Deficits Associated with Alzheimer's Disease.
Nirogi R, Mohammed AR, Shinde AK, Gagginapally SR, Kancharla DM, Ravella SR, Bogaraju N, Middekadi VR, Subramanian R, Palacharla RC, Benade V, Muddana N, Abraham R, Medapati RB, Thentu JB, Mekala VR, Petlu S, Lingavarapu BB, Yarra S, Kagita N, Goyal VK, Pandey SK, Jasti V.
J Med Chem (2021) 64 : 10641 -10665
PubMed 34251799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 7.58 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL117287 PRUCALOPRIDE 4.0 1 7.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL117287 PRUCALOPRIDE EC50 = 26.0 nM 7.58