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Assay Detail

CHEMBL670187

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

Binding
Displacement of 0.5 nM [3H]WIN-35248 from Dopamine transporter
13
Total Activities
7
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

3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter.
Blough BE, Holmquist CR, Abraham P, Kuhar MJ, Carroll FI.
Bioorg Med Chem Lett (2000) 10 : 2445 -2447
PubMed 11078197 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.23 9.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL81525 2 9.21
CHEMBL80262 2 9.08
CHEMBL306208 2 8.95
CHEMBL82027 2 8.77
CHEMBL80515 2 8.36
CHEMBL2079586 2 7.80
CHEMBL370805 COCAINE 4.0 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL81525 IC50 = 0.62 nM 9.21
CHEMBL80262 IC50 = 0.84 nM 9.08
CHEMBL306208 IC50 = 1.12 nM 8.95
CHEMBL82027 IC50 = 1.7 nM 8.77
CHEMBL306208 IC50 = 2.4 nM 8.62
CHEMBL81525 IC50 = 3.1 nM 8.51
CHEMBL80515 IC50 = 4.4 nM 8.36
CHEMBL82027 IC50 = 10.2 nM 7.99
CHEMBL2079586 IC50 = 15.7 nM 7.80
CHEMBL2079586 IC50 = 21.0 nM 7.68
CHEMBL80515 IC50 = 32.6 nM 7.49
CHEMBL80262 IC50 = 33.6 nM 7.47
CHEMBL370805 COCAINE IC50 = 89.1 nM 7.05