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Assay Detail

CHEMBL3744508

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

Binding
Displacement of [3H]8-OH-DPAT from human recombinant 5-HT1A receptor expressed in HeLa cell membrane after 30 mins by liquid scintillation counting
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Enantiomeric resolution of [(2,2-diphenyl-1,3-dioxolan-4-yl)methyl](2-phenoxyethyl)amine, a potent 1and 5-HT1Areceptor ligand: an in vitro and computational study
Franchini S, Baraldi A, Sorbi C, Pellati F, Cichero E, Battisti UM, Angeli P, Cilia A, Brasili L
Medchemcomm (2015) 6 : 677 -690
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.28 8.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3741808 1 8.61
CHEMBL3739897 1 8.52
CHEMBL37883 1 8.45
CHEMBL3739932 1 8.42
CHEMBL3740374 1 7.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3741808 Ki = 2.455 nM 8.61
CHEMBL3739897 Ki = 3.02 nM 8.52
CHEMBL37883 Ki = 3.548 nM 8.45
CHEMBL3739932 Ki = 3.802 nM 8.42
CHEMBL3740374 Ki = 40.74 nM 7.39