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Assay Detail

CHEMBL4009967

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

Binding
Activity at DAT in rat synaptosomes assessed as release of [3H]DA after 5 mins by liquid scintillation counting method
12
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 Autocuration

Target

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

Publication

The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.
Glennon RA.
J Med Chem (2017) 60 : 2605 -2628
PubMed 28244748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 6.59 7.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4084187 1 7.83
CHEMBL612 DEXTROAMPHETAMINE 4.0 1 7.60
CHEMBL3330645 1 7.19
CHEMBL1788307 1 7.01
CHEMBL195390 1 6.85
CHEMBL6731 TENAMFETAMINE 2.0 1 6.72
CHEMBL43048 MIDOMAFETAMINE 3.0 1 6.56
CHEMBL1927025 1 6.05
CHEMBL3330646 1 6.05
CHEMBL4104749 1 6.00
CHEMBL4086874 1 5.80
CHEMBL382757 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4084187 EC50 = 14.8 nM 7.83
CHEMBL612 DEXTROAMPHETAMINE EC50 = 25.0 nM 7.60
CHEMBL3330645 EC50 = 64.0 nM 7.19
CHEMBL1788307 EC50 = 98.0 nM 7.01
CHEMBL195390 EC50 = 142.0 nM 6.85
CHEMBL6731 TENAMFETAMINE EC50 = 190.0 nM 6.72
CHEMBL43048 MIDOMAFETAMINE EC50 = 278.0 nM 6.56
CHEMBL1927025 EC50 = 900.0 nM 6.05
CHEMBL3330646 EC50 = 900.0 nM 6.05
CHEMBL4104749 EC50 = 1000.0 nM 6.00
CHEMBL4086874 EC50 = 1600.0 nM 5.80
CHEMBL382757 EC50 = 3700.0 nM 5.43