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Assay Detail

CHEMBL808105

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

Binding
Inhibition of [3H](+)-DTG binding to Sigma opioid receptor (type 2) of rat liver membranes in the presence of (+)-pentazocine
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 3 — Cell-line / Tissue
Curated By Expert

Publication

Conformationally-flexible benzamide analogues as dopamine D3 and sigma 2 receptor ligands.
Mach RH, Huang Y, Freeman RA, Wu L, Vangveravong S, Luedtke RR.
Bioorg Med Chem Lett (2004) 14 : 195 -202
PubMed 14684327 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.50 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL291439 1 8.09
CHEMBL60048 1 7.99
CHEMBL64261 1 7.91
CHEMBL64260 1 7.88
CHEMBL64176 1 7.79
CHEMBL60139 1 7.75
CHEMBL60140 1 7.67
CHEMBL53038 1 7.60
CHEMBL61789 1 7.58
CHEMBL60133 1 7.32
CHEMBL62638 1 7.16
CHEMBL59713 1 7.12
CHEMBL64751 1 7.05
CHEMBL305366 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL291439 Ki = 8.2 nM 8.09
CHEMBL60048 Ki = 10.3 nM 7.99
CHEMBL64261 Ki = 12.4 nM 7.91
CHEMBL64260 Ki = 13.3 nM 7.88
CHEMBL64176 Ki = 16.4 nM 7.79
CHEMBL60139 Ki = 17.6 nM 7.75
CHEMBL60140 Ki = 21.2 nM 7.67
CHEMBL53038 Ki = 25.0 nM 7.60
CHEMBL61789 Ki = 26.4 nM 7.58
CHEMBL60133 Ki = 47.7 nM 7.32
CHEMBL62638 Ki = 70.0 nM 7.16
CHEMBL59713 Ki = 75.0 nM 7.12
CHEMBL64751 Ki = 89.4 nM 7.05
CHEMBL305366 Ki = 716.5 nM 6.14