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Assay Detail

CHEMBL992474

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

Binding
Displacement of [3H]5-HT from SERT in rat cerebral cortex synaptosome membrane
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

The molecular interactions of buspirone analogues with the serotonin transporter.
Jarończyk M, Chilmonczyk Z, Mazurek AP, Nowak G, Ravna AW, Kristiansen K, Sylte I.
Bioorg Med Chem (2008) 16 : 9283 -9294
PubMed 18812261 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.08 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL485540 1 7.48
CHEMBL485542 1 7.12
CHEMBL483176 1 7.02
CHEMBL299638 1 6.95
CHEMBL297702 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL485540 IC50 = 33.0 nM 7.48
CHEMBL485542 IC50 = 75.0 nM 7.12
CHEMBL483176 IC50 = 95.0 nM 7.02
CHEMBL299638 IC50 = 112.0 nM 6.95
CHEMBL297702 IC50 = 146.0 nM 6.84