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Assay Detail

CHEMBL1291963

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

Binding
Selectivity ratio of Ki for dopamine transporter in Sprague-Dawley rat brain to Ki for serotonin transporter in Sprague-Dawley rat brain
31
Total Activities
31
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
Selectivity ratio 29 - -
Ki 2 6.06 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1201082 FLUOXETINE HYDROCHLORIDE 4.0 1 6.41
CHEMBL6067650 PAROXETINE HYDROCHLORIDE 4.0 1 5.70
CHEMBL541124 1 -
CHEMBL536264 1 -
CHEMBL536952 1 -
CHEMBL1290622 1 -
CHEMBL1290741 1 -
CHEMBL1288490 1 -
CHEMBL1290742 1 -
CHEMBL1289072 1 -
CHEMBL1289073 1 -
CHEMBL1289190 1 -
CHEMBL1289191 1 -
CHEMBL1289302 1 -
CHEMBL1289303 1 -
CHEMBL1289420 1 -
CHEMBL1289421 1 -
CHEMBL1289533 1 -
CHEMBL1289534 1 -
CHEMBL1289642 1 -
CHEMBL1289643 1 -
CHEMBL1289747 1 -
CHEMBL1289748 1 -
CHEMBL1289854 1 -
CHEMBL1289855 1 -
CHEMBL1289972 1 -
CHEMBL1289973 1 -
CHEMBL1290067 1 -
CHEMBL1290068 1 -
CHEMBL1290174 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1201082 FLUOXETINE HYDROCHLORIDE Ki = 392.0 nM 6.41
CHEMBL6067650 PAROXETINE HYDROCHLORIDE Ki = 2000.0 nM 5.70
CHEMBL1701 MEPERIDINE HYDROCHLORIDE Selectivity ratio = 43.0 -
CHEMBL541124 Selectivity ratio = 6.7 -
CHEMBL536264 Selectivity ratio = 150.0 -
CHEMBL536952 Selectivity ratio = 160.0 -
CHEMBL1290622 Selectivity ratio = 159.0 -
CHEMBL1290741 Selectivity ratio = 980.0 -
CHEMBL1288490 Selectivity ratio = 1400.0 -
CHEMBL1290742 Selectivity ratio = 51.0 -
CHEMBL1289072 Selectivity ratio = 760.0 -
CHEMBL1289073 Selectivity ratio = 1600.0 -
CHEMBL1289190 Selectivity ratio = 1500.0 -
CHEMBL1289191 Selectivity ratio = 1200.0 -
CHEMBL1289302 Selectivity ratio = 370.0 -
CHEMBL1289303 Selectivity ratio = 260.0 -
CHEMBL1289420 Selectivity ratio = 520.0 -
CHEMBL1289421 Selectivity ratio = 47.0 -
CHEMBL1289533 Selectivity ratio = 100.0 -
CHEMBL1289534 Selectivity ratio = 110.0 -
CHEMBL1289642 Selectivity ratio = 227.0 -
CHEMBL1289643 Selectivity ratio = 96.0 -
CHEMBL1289747 Selectivity ratio = 48.0 -
CHEMBL1289748 Selectivity ratio = 560.0 -
CHEMBL1289854 Selectivity ratio = 4900.0 -
CHEMBL1289855 Selectivity ratio = 300.0 -
CHEMBL1289972 Selectivity ratio = 740.0 -
CHEMBL1289973 Selectivity ratio = 310.0 -
CHEMBL1290067 Selectivity ratio = 370.0 -
CHEMBL1290068 Selectivity ratio = 120.0 -
CHEMBL1290174 Selectivity ratio = 500.0 -