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Assay Detail

CHEMBL670038

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

Binding
Inhibition of [3H]WIN-35428l binding to Dopamine transporter
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Isopropyl and phenyl esters of 3 beta-(4-substituted phenyl)tropan-2 beta-carboxylic acids. Potent and selective compounds for the dopamine transporter.
Carroll FI, Abraham P, Lewin AH, Parham KA, Boja JW, Kuhar M.
J Med Chem (1992) 35 : 2497 -2500
PubMed 1619622 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.14 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL82946 1 9.37
CHEMBL610897 1 8.93
CHEMBL311347 1 8.90
CHEMBL82093 1 8.85
CHEMBL313038 1 8.82
CHEMBL312037 1 8.77
CHEMBL310573 1 8.70
CHEMBL86165 1 8.48
CHEMBL309635 1 8.28
CHEMBL2079586 1 7.80
CHEMBL83729 1 7.64
CHEMBL370805 COCAINE 4.0 1 6.99
CHEMBL314464 1 6.95
CHEMBL310131 1 6.89
CHEMBL314465 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL82946 IC50 = 0.43 nM 9.37
CHEMBL610897 IC50 = 1.17 nM 8.93
CHEMBL311347 IC50 = 1.26 nM 8.90
CHEMBL82093 IC50 = 1.41 nM 8.85
CHEMBL313038 IC50 = 1.51 nM 8.82
CHEMBL312037 IC50 = 1.71 nM 8.77
CHEMBL310573 IC50 = 1.99 nM 8.70
CHEMBL86165 IC50 = 3.27 nM 8.48
CHEMBL309635 IC50 = 5.29 nM 8.28
CHEMBL2079586 IC50 = 15.7 nM 7.80
CHEMBL83729 IC50 = 23.0 nM 7.64
CHEMBL370805 COCAINE IC50 = 102.0 nM 6.99
CHEMBL314464 IC50 = 112.0 nM 6.95
CHEMBL310131 IC50 = 130.0 nM 6.89
CHEMBL314465 IC50 = 211.0 nM 6.68