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Assay Detail

CHEMBL616165

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Binding
Concentration of compound required to inhibit cortical 5-hydroxytryptamine 1A receptor binding sites in rat brain was evaluated
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Resolved N,N-dialkylated 2-amino-8-hydroxytetralins: stereoselective interactions with 5-HT1A receptors in the brain.
Björk L, Höök BB, Nelson DL, Andén NE, Hacksell U.
J Med Chem (1989) 32 : 779 -783
PubMed 2522991 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.38 8.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26998 1 8.31
CHEMBL41436 1 8.18
CHEMBL164814 1 8.02
CHEMBL423987 1 7.33
CHEMBL168114 1 7.12
CHEMBL351641 1 6.96
CHEMBL349409 1 6.94
CHEMBL423807 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26998 IC50 = 4.84 nM 8.31
CHEMBL41436 IC50 = 6.54 nM 8.18
CHEMBL164814 IC50 = 9.65 nM 8.02
CHEMBL423987 IC50 = 46.2 nM 7.33
CHEMBL168114 IC50 = 75.0 nM 7.12
CHEMBL351641 IC50 = 108.9 nM 6.96
CHEMBL349409 IC50 = 114.5 nM 6.94
CHEMBL423807 IC50 = 675.0 nM 6.17