Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL660857

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

Binding
Competitive inhibition against [3H]cocaine binding to cocaine receptor in bovine striatal tissue
7
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Sodium-dependent dopamine transporter (CHEMBL2986)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Synthesis of 3-arylecgonine analogues as inhibitors of cocaine binding and dopamine uptake.
Kline RH, Wright J, Fox KM, Eldefrawi ME.
J Med Chem (1990) 33 : 2024 -2028
PubMed 2362282 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.52 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1790051 2 7.66
CHEMBL60609 2 6.86
CHEMBL370805 COCAINE 4.0 1 6.86
CHEMBL302855 1 6.72
CHEMBL62608 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1790051 IC50 = 22.0 nM 7.66
CHEMBL60609 IC50 = 137.0 nM 6.86
CHEMBL370805 COCAINE IC50 = 139.0 nM 6.86
CHEMBL302855 IC50 = 192.0 nM 6.72
CHEMBL60609 IC50 = 213.0 nM 6.67
CHEMBL1790051 IC50 = 1200.0 nM 5.92
CHEMBL62608 IC50 = 11000.0 nM 4.96