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Assay Detail

CHEMBL1693939

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

Binding
Displacement of [3H]-paroxetine from SERT in rabbit cortical membrane
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis, molecular docking and binding studies of selective serotonin transporter inhibitors.
Nencetti S, Mazzoni MR, Ortore G, Lapucci A, Giuntini J, Orlandini E, Banti I, Nuti E, Lucacchini A, Giannaccini G, Rossello A.
Eur J Med Chem (2011) 46 : 825 -834
PubMed 21272963 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.40 9.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL490 PAROXETINE 4.0 1 9.51
CHEMBL153036 R-FLUOXETINE 1 8.24
CHEMBL1689299 1 7.99
CHEMBL1689295 1 7.65
CHEMBL1689291 1 7.54
CHEMBL1689296 1 7.09
CHEMBL1689293 1 7.01
CHEMBL1689297 1 7.01
CHEMBL1689300 1 7.01
CHEMBL1689294 1 6.86
CHEMBL1689292 1 6.51
CHEMBL1689298 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL490 PAROXETINE Ki = 0.31 nM 9.51
CHEMBL153036 R-FLUOXETINE Ki = 5.8 nM 8.24
CHEMBL1689299 Ki = 10.28 nM 7.99
CHEMBL1689295 Ki = 22.6 nM 7.65
CHEMBL1689291 Ki = 28.74 nM 7.54
CHEMBL1689296 Ki = 81.07 nM 7.09
CHEMBL1689293 Ki = 98.42 nM 7.01
CHEMBL1689297 Ki = 96.82 nM 7.01
CHEMBL1689300 Ki = 96.58 nM 7.01
CHEMBL1689294 Ki = 138.61 nM 6.86
CHEMBL1689292 Ki = 305.9 nM 6.51
CHEMBL1689298 Ki = 396.5 nM 6.40