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Assay Detail

CHEMBL2019953

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

Binding
Displacement of [3H]-pentazocine from sigma 1 opioid receptor in rat liver homogenate by liquid scintillation counting
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL3602)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Homology Model and Docking-Based Virtual Screening for Ligands of the σ1 Receptor.
Laurini E, Col VD, Mamolo MG, Zampieri D, Posocco P, Fermeglia M, Vio L, Pricl S.
ACS Med Chem Lett (2011) 2 : 834 -839
PubMed 24900272 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.89 10.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL372700 FENPROPIMORPH 1 10.96
CHEMBL473783 1 10.01
CHEMBL2017957 1 8.73
CHEMBL559292 1 8.59
CHEMBL472979 1 8.45
CHEMBL54 HALOPERIDOL 4.0 1 8.24
CHEMBL551856 1 8.15
CHEMBL559979 1 7.89
CHEMBL560 1 7.82
CHEMBL557297 1 7.65
CHEMBL2017958 1 7.52
CHEMBL564522 1 6.65
CHEMBL474182 1 5.99
CHEMBL562450 1 5.94
CHEMBL2017959 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL372700 FENPROPIMORPH Ki = 0.011 nM 10.96
CHEMBL473783 Ki = 0.098 nM 10.01
CHEMBL2017957 Ki = 1.87 nM 8.73
CHEMBL559292 Ki = 2.6 nM 8.59
CHEMBL472979 Ki = 3.58 nM 8.45
CHEMBL54 HALOPERIDOL Ki = 5.7 nM 8.24
CHEMBL551856 Ki = 7.1 nM 8.15
CHEMBL559979 Ki = 12.9 nM 7.89
CHEMBL560 Ki = 15.0 nM 7.82
CHEMBL557297 Ki = 22.5 nM 7.65
CHEMBL2017958 Ki = 30.3 nM 7.52
CHEMBL564522 Ki = 223.0 nM 6.65
CHEMBL474182 Ki = 1017.0 nM 5.99
CHEMBL562450 Ki = 1147.0 nM 5.94
CHEMBL2017959 Ki = 1578.0 nM 5.80