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Assay Detail

CHEMBL1833366

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

Binding
Displacement of (-)-[3H]pentazocine from sigma 1 receptor in rat brain membrane after 120 mins
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and pharmacological evaluation of indole-based sigma receptor ligands.
Mésangeau C, Amata E, Alsharif W, Seminerio MJ, Robson MJ, Matsumoto RR, Poupaert JH, McCurdy CR.
Eur J Med Chem (2011) 46 : 5154 -5161
PubMed 21899931 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.21 8.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1831159 1 8.67
CHEMBL1830149 1 8.48
CHEMBL54 HALOPERIDOL 4.0 1 8.47
CHEMBL270341 1 8.38
CHEMBL1831158 1 8.27
CHEMBL1831160 1 7.84
CHEMBL1831167 1 7.46
CHEMBL1831156 1 7.15
CHEMBL1831164 1 7.04
CHEMBL1831161 1 7.03
CHEMBL1831157 1 6.85
CHEMBL1831162 1 6.65
CHEMBL1831168 1 6.55
CHEMBL1831169 1 6.21
CHEMBL1831163 1 6.15
CHEMBL1831165 1 5.92
CHEMBL1831166 1 5.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1831159 Ki = 2.13 nM 8.67
CHEMBL1830149 Ki = 3.28 nM 8.48
CHEMBL54 HALOPERIDOL Ki = 3.35 nM 8.47
CHEMBL270341 Ki = 4.17 nM 8.38
CHEMBL1831158 Ki = 5.33 nM 8.27
CHEMBL1831160 Ki = 14.55 nM 7.84
CHEMBL1831167 Ki = 34.5 nM 7.46
CHEMBL1831156 Ki = 71.5 nM 7.15
CHEMBL1831164 Ki = 90.87 nM 7.04
CHEMBL1831161 Ki = 92.43 nM 7.03
CHEMBL1831157 Ki = 140.7 nM 6.85
CHEMBL1831162 Ki = 222.33 nM 6.65
CHEMBL1831168 Ki = 279.0 nM 6.55
CHEMBL1831169 Ki = 613.66 nM 6.21
CHEMBL1831163 Ki = 713.5 nM 6.15
CHEMBL1831165 Ki = 1202.0 nM 5.92
CHEMBL1831166 Ki = 2948.4 nM 5.53