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Assay Detail

CHEMBL4735563

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

Functional
Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type COS7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 6 (CHEMBL3371)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HT receptor antagonist with therapeutic interest in Alzheimer's disease.
Toublet FX,Lalut J,Hatat B,Lecoutey C,Davis A,Since M,Corvaisier S,Freret T,Sopková-de Oliveira Santos J,Claeysen S,Boulouard M,Dallemagne P,Rochais C
Eur J Med Chem (2021) 210 : 113059 -113059
PubMed 33310288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.85 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3286580 IDALOPIRDINE 3.0 1 6.00
CHEMBL4746584 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3286580 IDALOPIRDINE IC50 = 1000.0 nM 6.00
CHEMBL4746584 IC50 = 1995.26 nM 5.70