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Assay Detail

CHEMBL805176

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Binding
Binding affinity for serotonin transporter is assessed from the ability to displace [3H]citalopram from rat brain.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and biological evaluation of 2-substituted 3beta-tolyltropane derivatives at dopamine, serotonin, and norepinephrine transporters.
Xu L, Izenwasser S, Katz JL, Kopajtic T, Klein-Stevens C, Zhu N, Lomenzo SA, Winfield L, Trudell ML.
J Med Chem (2002) 45 : 1203 -1210
PubMed 11881989 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.38 7.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2079577 1 7.18
CHEMBL2112763 1 7.16
CHEMBL2112762 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2079577 Ki = 66.0 nM 7.18
CHEMBL2112763 Ki = 70.0 nM 7.16
CHEMBL2112762 Ki = 16000.0 nM 4.80