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Assay Detail

CHEMBL3286059

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

Binding
Inhibition of [3H]dopamine uptake at dopamine transporter expressed in rat striatal homogenate after 5 mins by scintillation counting analysis
5
Total Activities
2
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 dopamine transporter (CHEMBL338)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Conformationally rigid amphetamine analogs as inhibitors of monoamine uptake by brain synaptosomes.
Tuomisto J, Tuomisto L, Pazdernik TL.
J Med Chem (1976) 19 : 725 -727
PubMed 1271416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.24 6.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL405 AMPHETAMINE 4.0 1 6.02
CHEMBL3278291 4 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL405 AMPHETAMINE IC50 = 960.0 nM 6.02
CHEMBL3278291 IC50 = 3800.0 nM 5.42
CHEMBL3278291 IC50 = 7000.0 nM 5.16
CHEMBL3278291 IC50 = 12000.0 nM 4.92
CHEMBL3278291 IC50 = 20000.0 nM 4.70