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Assay Detail

CHEMBL885075

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

Binding
In vitro inhibitory activity towards [3H]cocaine binding to rat striatal tissue
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
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-carbamoylecgonine methyl ester analogues as inhibitors of cocaine binding and dopamine uptake.
Kline RH, Wright J, Eshleman AJ, Fox KM, Eldefrawi ME.
J Med Chem (1991) 34 : 702 -705
PubMed 1995895 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.95 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL159325 1 7.43
CHEMBL370805 COCAINE 4.0 1 7.19
CHEMBL163614 1 5.96
CHEMBL350155 1 5.68
CHEMBL164409 1 5.25
CHEMBL348799 1 4.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL159325 IC50 = 37.0 nM 7.43
CHEMBL370805 COCAINE IC50 = 65.0 nM 7.19
CHEMBL163614 IC50 = 1090.0 nM 5.96
CHEMBL350155 IC50 = 2070.0 nM 5.68
CHEMBL164409 IC50 = 5600.0 nM 5.25
CHEMBL348799 IC50 = 63300.0 nM 4.20