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Assay Detail

CHEMBL837592

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Functional
Inhibitory concentration against [3H]-DA uptake in rat brain tissue
3
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Brain
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
IC50 3 5.56 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1701 MEPERIDINE HYDROCHLORIDE 4.0 2 6.21
CHEMBL370805 COCAINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1701 MEPERIDINE HYDROCHLORIDE IC50 = 610.0 nM 6.21
CHEMBL1701 MEPERIDINE HYDROCHLORIDE IC50 = 12600.0 nM 4.90
CHEMBL370805 COCAINE IC50 = 405000.0 nM -