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Assay Detail

CHEMBL4189949

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Binding
Agonist activity at 5-HT4E receptor (unknown origin)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HT4 Receptor Partial Agonists.
Nirogi R, Mohammed AR, Shinde AK, Gagginapally SR, Kancharla DM, Middekadi VR, Bogaraju N, Ravella SR, Singh P, Birangal SR, Subramanian R, Palacharla RC, Benade V, Muddana N, Jayarajan P.
J Med Chem (2018) 61 : 4993 -5008
PubMed 29763304 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.31 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2152922 PF-04995274 1.0 1 9.59
CHEMBL3306918 PRX-03140 2.0 1 7.77
CHEMBL117287 PRUCALOPRIDE 4.0 1 7.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2152922 PF-04995274 EC50 = 0.26 nM 9.59
CHEMBL3306918 PRX-03140 EC50 = 17.0 nM 7.77
CHEMBL117287 PRUCALOPRIDE EC50 = 26.0 nM 7.58