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Assay Detail

CHEMBL1014663

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

Binding
Displacement of [3H]citalopram from SERT in Sprague-dawley rat frontal cortex by liquid scintillation spectrophotometry
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Frontal cortex
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

1-Naphthyl and 4-indolyl arylalkylamines as selective monoamine reuptake inhibitors.
Manning JR, Sexton T, Childers SR, Davies HM.
Bioorg Med Chem Lett (2009) 19 : 58 -61
PubMed 19038547 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.66 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL513103 1 9.09
CHEMBL453520 1 8.78
CHEMBL461444 1 8.56
CHEMBL509403 1 8.44
CHEMBL502147 1 8.39
CHEMBL1175 DULOXETINE 4.0 1 8.34
CHEMBL460590 1 8.28
CHEMBL336920 (R)-DULOXETINE 1 8.06
CHEMBL459519 1 8.02
CHEMBL508252 1 7.92
CHEMBL450173 1 7.52
CHEMBL468914 1 7.50
CHEMBL459732 1 7.40
CHEMBL41 FLUOXETINE 4.0 1 7.32
CHEMBL460372 1 7.30
CHEMBL468915 1 7.14
CHEMBL468916 1 7.07
CHEMBL511690 1 6.78
CHEMBL512120 1 6.57
CHEMBL295467 NISOXETINE 2.0 1 6.56
CHEMBL641 ATOMOXETINE 4.0 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL513103 Ki = 0.82 nM 9.09
CHEMBL453520 Ki = 1.68 nM 8.78
CHEMBL461444 Ki = 2.72 nM 8.56
CHEMBL509403 Ki = 3.63 nM 8.44
CHEMBL502147 Ki = 4.1 nM 8.39
CHEMBL1175 DULOXETINE Ki = 4.6 nM 8.34
CHEMBL460590 Ki = 5.3 nM 8.28
CHEMBL336920 (R)-DULOXETINE Ki = 8.8 nM 8.06
CHEMBL459519 Ki = 9.5 nM 8.02
CHEMBL508252 Ki = 12.1 nM 7.92
CHEMBL450173 Ki = 30.2 nM 7.52
CHEMBL468914 Ki = 31.9 nM 7.50
CHEMBL459732 Ki = 39.7 nM 7.40
CHEMBL41 FLUOXETINE Ki = 48.0 nM 7.32
CHEMBL460372 Ki = 49.9 nM 7.30
CHEMBL468915 Ki = 72.9 nM 7.14
CHEMBL468916 Ki = 86.0 nM 7.07
CHEMBL511690 Ki = 166.0 nM 6.78
CHEMBL512120 Ki = 271.0 nM 6.57
CHEMBL295467 NISOXETINE Ki = 277.0 nM 6.56
CHEMBL641 ATOMOXETINE Ki = 1500.0 nM 5.82