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Assay Detail

CHEMBL740206

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Binding
Tested in vitro for dopamine(DA) neuronal uptake inhibition
29
Total Activities
27
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 dopamine transporter (CHEMBL2799)
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 29 6.91 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285506 1 9.00
CHEMBL330666 1 8.59
CHEMBL96362 1 8.49
CHEMBL35184 1 7.95
CHEMBL327790 3 7.63
CHEMBL94535 1 7.56
CHEMBL95153 1 7.36
CHEMBL555462 1 7.24
CHEMBL329216 1 7.08
CHEMBL539803 1 7.08
CHEMBL328818 1 7.07
CHEMBL555655 1 6.99
CHEMBL94508 1 6.96
CHEMBL94738 1 6.89
CHEMBL94665 1 6.73
CHEMBL94711 1 6.56
CHEMBL554191 1 6.54
CHEMBL490 PAROXETINE 4.0 1 6.34
CHEMBL541308 1 6.19
CHEMBL94739 FEMOXETINE 2.0 1 5.99
CHEMBL284305 1 5.76
CHEMBL93035 1 5.68
CHEMBL545724 1 5.55
CHEMBL96615 1 5.21
CHEMBL11 IMIPRAMINE 4.0 1 -
CHEMBL41 FLUOXETINE 4.0 1 -
CHEMBL549 CITALOPRAM 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285506 Ki = 0.99 nM 9.00
CHEMBL330666 Ki = 2.6 nM 8.59
CHEMBL96362 Ki = 3.2 nM 8.49
CHEMBL35184 Ki = 11.3 nM 7.95
CHEMBL327790 Ki = 23.5 nM 7.63
CHEMBL94535 Ki = 27.4 nM 7.56
CHEMBL327790 Ki = 36.8 nM 7.43
CHEMBL95153 Ki = 43.7 nM 7.36
CHEMBL555462 Ki = 57.7 nM 7.24
CHEMBL329216 Ki = 83.0 nM 7.08
CHEMBL539803 Ki = 83.9 nM 7.08
CHEMBL328818 Ki = 84.5 nM 7.07
CHEMBL555655 Ki = 103.0 nM 6.99
CHEMBL94508 Ki = 111.0 nM 6.96
CHEMBL94738 Ki = 128.0 nM 6.89
CHEMBL94665 Ki = 187.0 nM 6.73
CHEMBL94711 Ki = 278.0 nM 6.56
CHEMBL554191 Ki = 290.0 nM 6.54
CHEMBL490 PAROXETINE Ki = 460.0 nM 6.34
CHEMBL541308 Ki = 652.0 nM 6.19
CHEMBL94739 FEMOXETINE Ki = 1035.0 nM 5.99
CHEMBL327790 Ki = 1450.0 nM 5.84
CHEMBL284305 Ki = 1740.0 nM 5.76
CHEMBL93035 Ki = 2110.0 nM 5.68
CHEMBL545724 Ki = 2800.0 nM 5.55
CHEMBL96615 Ki = 6180.0 nM 5.21
CHEMBL11 IMIPRAMINE Ki > 10000.0 nM -
CHEMBL41 FLUOXETINE Ki > 2000.0 nM -
CHEMBL549 CITALOPRAM Ki > 10000.0 nM -