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Assay Detail

CHEMBL839593

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

Binding
Inhibition of [3H]WIN-35428 binding to rat dopamine transporter
13
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium-dependent dopamine transporter (CHEMBL338)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological evaluation of meperidine analogues at monoamine transporters.
Lomenzo SA, Rhoden JB, Izenwasser S, Wade D, Kopajtic T, Katz JL, Trudell ML.
J Med Chem (2005) 48 : 1336 -1343
PubMed 15743177 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 5.39 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL541124 1 6.90
CHEMBL536952 1 5.94
CHEMBL536265 1 5.63
CHEMBL557576 1 5.57
CHEMBL536264 1 5.49
CHEMBL539076 1 5.39
CHEMBL536037 1 5.08
CHEMBL539845 1 4.97
CHEMBL539075 1 4.91
CHEMBL1701 MEPERIDINE HYDROCHLORIDE 4.0 1 4.75
CHEMBL540360 1 4.66
CHEMBL370805 COCAINE 4.0 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL541124 Ki = 125.0 nM 6.90
CHEMBL536952 Ki = 1140.0 nM 5.94
CHEMBL536265 Ki = 2360.0 nM 5.63
CHEMBL557576 Ki = 2670.0 nM 5.57
CHEMBL536264 Ki = 3250.0 nM 5.49
CHEMBL539076 Ki = 4100.0 nM 5.39
CHEMBL536037 Ki = 8340.0 nM 5.08
CHEMBL539845 Ki = 10700.0 nM 4.97
CHEMBL539075 Ki = 12400.0 nM 4.91
CHEMBL1701 MEPERIDINE HYDROCHLORIDE Ki = 17800.0 nM 4.75
CHEMBL540360 Ki = 22000.0 nM 4.66
CHEMBL370805 COCAINE Ki = 32000.0 nM -
CHEMBL370805 COCAINE Ki = 388000.0 nM -