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Assay Detail

CHEMBL1291960

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

Binding
Displacement of [3H]citalopram from serotonin transporter in Sprague-Dawley rat brain after 1 hr by liquid scintillation counting
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands.
Gu X, Izenwasser S, Wade D, Housman A, Gulasey G, Rhoden JB, Savoie CD, Mobley DL, Lomenzo SA, Trudell ML.
Bioorg Med Chem (2010) 18 : 8356 -8364
PubMed 20980153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 8.18 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6067650 PAROXETINE HYDROCHLORIDE 4.0 1 10.30
CHEMBL1289854 1 9.22
CHEMBL1289190 1 9.00
CHEMBL1289073 1 8.77
CHEMBL1289748 1 8.70
CHEMBL1290067 1 8.70
CHEMBL1201082 FLUOXETINE HYDROCHLORIDE 4.0 1 8.70
CHEMBL1288490 1 8.60
CHEMBL1289973 1 8.54
CHEMBL1290741 1 8.48
CHEMBL1289072 1 8.41
CHEMBL1289191 1 8.37
CHEMBL1289972 1 8.23
CHEMBL1289855 1 8.23
CHEMBL1289642 1 8.19
CHEMBL1289302 1 8.15
CHEMBL536952 1 8.14
CHEMBL1289533 1 8.04
CHEMBL1290174 1 8.00
CHEMBL1289534 1 7.99
CHEMBL1289420 1 7.96
CHEMBL1289303 1 7.88
CHEMBL1290742 1 7.85
CHEMBL541124 1 7.73
CHEMBL536264 1 7.68
CHEMBL1290622 1 7.67
CHEMBL1290068 1 7.58
CHEMBL1289643 1 7.52
CHEMBL1289747 1 7.33
CHEMBL1289421 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6067650 PAROXETINE HYDROCHLORIDE Ki = 0.05 nM 10.30
CHEMBL1289854 Ki = 0.6 nM 9.22
CHEMBL1289190 Ki = 1.0 nM 9.00
CHEMBL1289073 Ki = 1.7 nM 8.77
CHEMBL1289748 Ki = 2.0 nM 8.70
CHEMBL1290067 Ki = 2.0 nM 8.70
CHEMBL1201082 FLUOXETINE HYDROCHLORIDE Ki = 2.0 nM 8.70
CHEMBL1288490 Ki = 2.5 nM 8.60
CHEMBL1289973 Ki = 2.9 nM 8.54
CHEMBL1290741 Ki = 3.3 nM 8.48
CHEMBL1289072 Ki = 3.9 nM 8.41
CHEMBL1289191 Ki = 4.3 nM 8.37
CHEMBL1289972 Ki = 5.9 nM 8.23
CHEMBL1289855 Ki = 5.9 nM 8.23
CHEMBL1289642 Ki = 6.4 nM 8.19
CHEMBL1289302 Ki = 7.0 nM 8.15
CHEMBL536952 Ki = 7.2 nM 8.14
CHEMBL1289533 Ki = 9.2 nM 8.04
CHEMBL1290174 Ki = 9.9 nM 8.00
CHEMBL1289534 Ki = 10.2 nM 7.99
CHEMBL1289420 Ki = 10.9 nM 7.96
CHEMBL1289303 Ki = 13.2 nM 7.88
CHEMBL1290742 Ki = 14.1 nM 7.85
CHEMBL541124 Ki = 18.7 nM 7.73
CHEMBL536264 Ki = 21.1 nM 7.68
CHEMBL1290622 Ki = 21.6 nM 7.67
CHEMBL1290068 Ki = 26.5 nM 7.58
CHEMBL1289643 Ki = 30.2 nM 7.52
CHEMBL1289747 Ki = 46.7 nM 7.33
CHEMBL1289421 Ki = 49.5 nM 7.30
CHEMBL1701 MEPERIDINE HYDROCHLORIDE Ki = 413.0 nM 6.38