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Assay Detail

CHEMBL808143

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

Binding
In vitro ability of compound to inhibit 5-HT re-uptake of radiolabeled [3H]-tritium transmitter into synaptosome
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

Sodium-dependent serotonin transporter (CHEMBL228)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bicyclo[2.2.1]heptanes as novel triple re-uptake inhibitors for the treatment of depression.
Axford L, Boot JR, Hotten TM, Keenan M, Martin FM, Milutinovic S, Moore NA, O'Neill MF, Pullar IA, Tupper DE, Van Belle KR, Vivien V.
Bioorg Med Chem Lett (2003) 13 : 3277 -3280
PubMed 12951108 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.40 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL111128 1 8.05
CHEMBL326466 1 8.05
CHEMBL109571 1 8.00
CHEMBL109517 1 7.70
CHEMBL331799 1 7.30
CHEMBL323447 1 7.03
CHEMBL322067 1 6.57
CHEMBL113136 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL111128 IC50 = 9.0 nM 8.05
CHEMBL326466 IC50 = 9.0 nM 8.05
CHEMBL109571 IC50 = 10.0 nM 8.00
CHEMBL109517 IC50 = 20.0 nM 7.70
CHEMBL331799 IC50 = 50.0 nM 7.30
CHEMBL323447 IC50 = 93.0 nM 7.03
CHEMBL322067 IC50 = 270.0 nM 6.57
CHEMBL113136 IC50 = 303.0 nM 6.52