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Assay Detail

CHEMBL4735557

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

Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Subcellular Membrane
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
Ki 6 8.16 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4746584 1 8.37
CHEMBL3286580 IDALOPIRDINE 3.0 1 8.16
CHEMBL4788250 1 7.94
CHEMBL4750581 1 -
CHEMBL4744490 1 -
CHEMBL4761198 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4746584 Ki = 4.3 nM 8.37
CHEMBL3286580 IDALOPIRDINE Ki = 6.9 nM 8.16
CHEMBL4788250 Ki = 11.4 nM 7.94
CHEMBL4750581 Ki - -
CHEMBL4744490 Ki - -
CHEMBL4761198 Ki - -