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Assay Detail

CHEMBL907722

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

Binding
Displacement of [3H]citaloporam from SERT in rat brain
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 Expert

Target

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

Publication

Design and synthesis of a novel photoaffinity ligand for the dopamine and serotonin transporters based on 2beta-carbomethoxy-3beta-biphenyltropane.
Newman AH, Cha JH, Cao J, Kopajtic T, Katz JL, Parnas ML, Vaughan R, Lever JR.
J Med Chem (2006) 49 : 6621 -6625
PubMed 17064081 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.33 8.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL218082 1 8.39
CHEMBL385942 1 8.05
CHEMBL214230 1 7.29
CHEMBL273878 1 6.96
CHEMBL217627 1 5.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL218082 Ki = 4.1 nM 8.39
CHEMBL385942 Ki = 8.82 nM 8.05
CHEMBL214230 Ki = 51.0 nM 7.29
CHEMBL273878 Ki = 109.0 nM 6.96
CHEMBL217627 Ki = 1070.0 nM 5.97