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Assay Detail

CHEMBL884138

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

Functional
Competitive inhibition against [3H]dopamine uptake in bovine striatal tissue
7
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Bos taurus
Tissue Striatum
Confidence 1 — Organism
Curated By Intermediate

Target

Bos taurus (CHEMBL613489)
Type ORGANISM
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 5.95 6.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1790051 2 6.88
CHEMBL302855 1 6.25
CHEMBL60609 2 6.21
CHEMBL370805 COCAINE 4.0 1 6.07
CHEMBL62608 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1790051 IC50 = 133.0 nM 6.88
CHEMBL302855 IC50 = 557.0 nM 6.25
CHEMBL60609 IC50 = 616.0 nM 6.21
CHEMBL370805 COCAINE IC50 = 843.0 nM 6.07
CHEMBL60609 IC50 = 903.0 nM 6.04
CHEMBL1790051 IC50 = 2100.0 nM 5.68
CHEMBL62608 IC50 = 30000.0 nM 4.52