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Assay Detail

CHEMBL675003

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

Binding
Inhibitory potency against dopamine (DA) transporter using [3H]WIN-35428 (WIN-) binding assay.
18
Total Activities
8
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

Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-substituted-6-amino-5-phenylbicyclo[2.2.2]octanes.
Javanmard S, Deutsch HM, Collard DM, Kuhar MJ, Schweri MM.
J Med Chem (1999) 42 : 4836 -4843
PubMed 10579846 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.84 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL358368 1 7.85
CHEMBL2079586 1 7.69
CHEMBL827 DEXMETHYLPHENIDATE 4.0 1 7.08
CHEMBL370805 COCAINE 4.0 1 6.80
CHEMBL357443 4 6.57
CHEMBL436211 4 5.75
CHEMBL145534 2 5.40
CHEMBL145732 4 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL358368 IC50 = 14.2 nM 7.85
CHEMBL2079586 IC50 = 20.4 nM 7.69
CHEMBL827 DEXMETHYLPHENIDATE IC50 = 83.0 nM 7.08
CHEMBL370805 COCAINE IC50 = 160.0 nM 6.80
CHEMBL357443 IC50 = 270.0 nM 6.57
CHEMBL357443 IC50 = 358.0 nM 6.45
CHEMBL436211 IC50 = 1770.0 nM 5.75
CHEMBL436211 IC50 = 2040.0 nM 5.69
CHEMBL357443 IC50 = 2200.0 nM 5.66
CHEMBL357443 IC50 = 2270.0 nM 5.64
CHEMBL145534 IC50 = 4010.0 nM 5.40
CHEMBL145732 IC50 = 5330.0 nM 5.27
CHEMBL436211 IC50 = 7040.0 nM 5.15
CHEMBL436211 IC50 = 9920.0 nM 5.00
CHEMBL145534 IC50 = 10300.0 nM 4.99
CHEMBL145732 IC50 = 12200.0 nM 4.91
CHEMBL145732 IC50 = 13600.0 nM 4.87
CHEMBL145732 IC50 = 45600.0 nM 4.34