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Assay Detail

CHEMBL962554

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

Binding
Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type C6
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis, and biological evaluation of new 5-HT4 receptor agonists: application as amyloid cascade modulators and potential therapeutic utility in Alzheimer's disease.
Russo O, Cachard-Chastel M, Rivière C, Giner M, Soulier JL, Berthouze M, Richard T, Monti JP, Sicsic S, Lezoualc'h F, Berque-Bestel I.
J Med Chem (2009) 52 : 2214 -2225
PubMed 19334715 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.72 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL488325 1 8.70
CHEMBL286136 1 8.30
CHEMBL490852 1 8.30
CHEMBL490050 1 7.92
CHEMBL442869 1 7.85
CHEMBL452353 1 6.96
CHEMBL39 SEROTONIN 3.0 1 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL488325 Ki = 2.0 nM 8.70
CHEMBL286136 Ki = 5.0 nM 8.30
CHEMBL490852 Ki = 5.0 nM 8.30
CHEMBL490050 Ki = 12.0 nM 7.92
CHEMBL442869 Ki = 14.0 nM 7.85
CHEMBL452353 Ki = 111.0 nM 6.96
CHEMBL39 SEROTONIN Ki = 1049.0 nM 5.98