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Assay Detail

CHEMBL784304

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Functional
Ability to inhibit [3H]dopamine uptake was measured in a chopped tissue assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Synthesis and biological evaluation of 2-substituted 3beta-tolyltropane derivatives at dopamine, serotonin, and norepinephrine transporters.
Xu L, Izenwasser S, Katz JL, Kopajtic T, Klein-Stevens C, Zhu N, Lomenzo SA, Winfield L, Trudell ML.
J Med Chem (2002) 45 : 1203 -1210
PubMed 11881989 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.87 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19944 1 7.80
CHEMBL279074 1 7.09
CHEMBL19715 1 6.58
CHEMBL276332 1 6.51
CHEMBL370805 COCAINE 4.0 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19944 IC50 = 16.0 nM 7.80
CHEMBL279074 IC50 = 82.0 nM 7.09
CHEMBL19715 IC50 = 266.0 nM 6.58
CHEMBL276332 IC50 = 311.0 nM 6.51
CHEMBL370805 COCAINE IC50 = 405.0 nM 6.39