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

CHEMBL934064

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

Binding
Displacement of [3H]DTG from opioid sigma2 receptor in rat brain homogenate
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Conversion of a highly selective sigma-1 receptor-ligand to sigma-2 receptor preferring ligands with anticocaine activity.
Mésangeau C, Narayanan S, Green AM, Shaikh J, Kaushal N, Viard E, Xu YT, Fishback JA, Poupaert JH, Matsumoto RR, McCurdy CR.
J Med Chem (2008) 51 : 1482 -1486
PubMed 18278854 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 8.42 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL270341 1 9.41
CHEMBL272603 1 9.26
CHEMBL272854 1 9.11
CHEMBL53325 1 8.96
CHEMBL272608 1 8.83
CHEMBL271772 1 8.74
CHEMBL271975 1 8.65
CHEMBL406081 1 8.61
CHEMBL273084 1 8.52
CHEMBL272610 1 8.51
CHEMBL408003 1 8.42
CHEMBL269876 1 8.27
CHEMBL406082 1 8.23
CHEMBL405925 1 8.06
CHEMBL54 HALOPERIDOL 4.0 1 7.09
CHEMBL272899 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL270341 Ki = 0.39 nM 9.41
CHEMBL272603 Ki = 0.55 nM 9.26
CHEMBL272854 Ki = 0.77 nM 9.11
CHEMBL53325 Ki = 1.11 nM 8.96
CHEMBL272608 Ki = 1.49 nM 8.83
CHEMBL271772 Ki = 1.83 nM 8.74
CHEMBL271975 Ki = 2.25 nM 8.65
CHEMBL406081 Ki = 2.44 nM 8.61
CHEMBL273084 Ki = 3.05 nM 8.52
CHEMBL272610 Ki = 3.06 nM 8.51
CHEMBL408003 Ki = 3.77 nM 8.42
CHEMBL269876 Ki = 5.43 nM 8.27
CHEMBL406082 Ki = 5.89 nM 8.23
CHEMBL405925 Ki = 8.74 nM 8.06
CHEMBL54 HALOPERIDOL Ki = 80.6 nM 7.09
CHEMBL272899 Ki = 830.95 nM 6.08