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Assay Detail

CHEMBL740208

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Binding
Tested in vitro for serotonin(5-HT) neuronal uptake inhibition
30
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium-dependent serotonin transporter (CHEMBL4642)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Pyrroloisoquinoline antidepressants. 3. A focus on serotonin.
Maryanoff BE, Vaught JL, Shank RP, McComsey DF, Costanzo MJ, Nortey SO.
J Med Chem (1990) 33 : 2793 -2797
PubMed 2213832 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 8.17 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL327790 3 9.41
CHEMBL490 PAROXETINE 4.0 1 9.36
CHEMBL330666 1 9.00
CHEMBL285506 1 8.75
CHEMBL555462 1 8.62
CHEMBL549 CITALOPRAM 4.0 1 8.54
CHEMBL96362 1 8.54
CHEMBL539803 1 8.52
CHEMBL554191 1 8.52
CHEMBL94711 1 8.49
CHEMBL541308 1 8.39
CHEMBL94738 1 8.32
CHEMBL329216 1 8.10
CHEMBL94508 1 8.09
CHEMBL555655 1 8.07
CHEMBL94739 FEMOXETINE 2.0 1 8.04
CHEMBL94535 1 8.01
CHEMBL41 FLUOXETINE 4.0 1 7.97
CHEMBL94665 1 7.90
CHEMBL545724 1 7.83
CHEMBL95153 1 7.81
CHEMBL284305 1 7.78
CHEMBL328818 1 7.72
CHEMBL35184 1 7.63
CHEMBL93035 1 7.54
CHEMBL11 IMIPRAMINE 4.0 1 7.38
CHEMBL96615 1 6.22
CHEMBL555404 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL327790 Ki = 0.39 nM 9.41
CHEMBL490 PAROXETINE Ki = 0.44 nM 9.36
CHEMBL327790 Ki = 0.68 nM 9.17
CHEMBL330666 Ki = 1.01 nM 9.00
CHEMBL285506 Ki = 1.76 nM 8.75
CHEMBL555462 Ki = 2.4 nM 8.62
CHEMBL549 CITALOPRAM Ki = 2.9 nM 8.54
CHEMBL96362 Ki = 2.9 nM 8.54
CHEMBL539803 Ki = 3.0 nM 8.52
CHEMBL554191 Ki = 3.0 nM 8.52
CHEMBL94711 Ki = 3.2 nM 8.49
CHEMBL541308 Ki = 4.1 nM 8.39
CHEMBL94738 Ki = 4.8 nM 8.32
CHEMBL329216 Ki = 7.9 nM 8.10
CHEMBL94508 Ki = 8.1 nM 8.09
CHEMBL555655 Ki = 8.6 nM 8.07
CHEMBL94739 FEMOXETINE Ki = 9.1 nM 8.04
CHEMBL94535 Ki = 9.7 nM 8.01
CHEMBL41 FLUOXETINE Ki = 10.8 nM 7.97
CHEMBL94665 Ki = 12.7 nM 7.90
CHEMBL545724 Ki = 14.7 nM 7.83
CHEMBL95153 Ki = 15.6 nM 7.81
CHEMBL284305 Ki = 16.6 nM 7.78
CHEMBL328818 Ki = 19.1 nM 7.72
CHEMBL35184 Ki = 23.5 nM 7.63
CHEMBL93035 Ki = 29.2 nM 7.54
CHEMBL11 IMIPRAMINE Ki = 42.0 nM 7.38
CHEMBL327790 Ki = 58.4 nM 7.23
CHEMBL96615 Ki = 597.0 nM 6.22
CHEMBL555404 Ki ~ 100.0 nM -