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Assay Detail

CHEMBL2037807

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

Binding
Displacement of [3H]Citalopram from human SERT by liquid scintillation counting
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): a search for new dual-acting agents as potential antidepressants.
Zhu XY, Etukala JR, Eyunni SV, Setola V, Roth BL, Ablordeppey SY.
Eur J Med Chem (2012) 53 : 124 -132
PubMed 22520153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.97 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439849 VILAZODONE 4.0 1 9.30
CHEMBL1201082 FLUOXETINE HYDROCHLORIDE 4.0 1 8.96
CHEMBL1946258 1 8.28
CHEMBL1946255 1 7.47
CHEMBL2037531 1 7.19
CHEMBL1946254 1 7.19
CHEMBL1946257 1 7.19
CHEMBL2037528 1 7.09
CHEMBL2037431 1 6.78
CHEMBL2037523 1 6.73
CHEMBL2037527 1 6.62
CHEMBL2037526 1 6.55
CHEMBL2037530 1 6.53
CHEMBL2037524 1 6.31
CHEMBL2037520 1 6.25
CHEMBL2037518 1 6.15
CHEMBL2037432 1 6.04
CHEMBL2037430 1 5.93
CHEMBL2037522 1 5.88
CHEMBL2037519 1 -
CHEMBL2037525 1 -
CHEMBL2037521 1 -
CHEMBL2037529 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439849 VILAZODONE Ki = 0.5 nM 9.30
CHEMBL1201082 FLUOXETINE HYDROCHLORIDE Ki = 1.1 nM 8.96
CHEMBL1946258 Ki = 5.3 nM 8.28
CHEMBL1946255 Ki = 34.0 nM 7.47
CHEMBL2037531 Ki = 64.0 nM 7.19
CHEMBL1946254 Ki = 65.0 nM 7.19
CHEMBL1946257 Ki = 65.0 nM 7.19
CHEMBL2037528 Ki = 81.0 nM 7.09
CHEMBL2037431 Ki = 166.0 nM 6.78
CHEMBL2037523 Ki = 186.0 nM 6.73
CHEMBL2037527 Ki = 237.0 nM 6.62
CHEMBL2037526 Ki = 284.0 nM 6.55
CHEMBL2037530 Ki = 298.0 nM 6.53
CHEMBL2037524 Ki = 491.0 nM 6.31
CHEMBL2037520 Ki = 565.0 nM 6.25
CHEMBL2037518 Ki = 706.0 nM 6.15
CHEMBL2037432 Ki = 922.0 nM 6.04
CHEMBL2037430 Ki = 1184.0 nM 5.93
CHEMBL2037522 Ki = 1325.0 nM 5.88
CHEMBL2037519 Ki - -
CHEMBL2037525 Ki > 10000.0 nM -
CHEMBL2037521 Ki - -
CHEMBL2037529 Ki - -