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Assay Detail

CHEMBL892232

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

Binding
Displacement of [3H]citalopram from human 5HT transporter expressed in HEK293 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Naphthyl piperazines with dual activity as 5-HT1D antagonists and 5-HT reuptake inhibitors.
Bueno AB, Gilmore J, Boot J, Broadmore R, Cooper J, Findlay J, Hayhurst L, Marcos A, Montero C, Mitchell S, Timms G, Tomlinson R, Wallace L, Walton L.
Bioorg Med Chem Lett (2007) 17 : 3344 -3348
PubMed 17434731 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.66 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL83617 1 10.00
CHEMBL234447 1 9.10
CHEMBL3706925 1 8.89
CHEMBL3706923 1 8.89
CHEMBL391272 1 8.68
CHEMBL233210 1 8.66
CHEMBL391271 1 8.52
CHEMBL391273 1 8.24
CHEMBL234448 1 8.13
CHEMBL234449 1 8.09
CHEMBL3706924 1 8.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL83617 Ki = 0.1 nM 10.00
CHEMBL234447 Ki = 0.8 nM 9.10
CHEMBL3706925 Ki = 1.3 nM 8.89
CHEMBL3706923 Ki = 1.3 nM 8.89
CHEMBL391272 Ki = 2.1 nM 8.68
CHEMBL233210 Ki = 2.2 nM 8.66
CHEMBL391271 Ki = 3.0 nM 8.52
CHEMBL391273 Ki = 5.7 nM 8.24
CHEMBL234448 Ki = 7.4 nM 8.13
CHEMBL234449 Ki = 8.1 nM 8.09
CHEMBL3706924 Ki = 8.8 nM 8.06