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Assay Detail

CHEMBL4158770

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Binding
Displacement of [3H]-DTG from sigma2 receptor in rat liver membranes
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sigma intracellular receptor 2 (CHEMBL4105864)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic σ Receptor Ligands with Exocyclic Amino Moiety.
Bergkemper M, Kronenberg E, Thum S, Börgel F, Daniliuc C, Schepmann D, Nieto FR, Brust P, Reinoso RF, Alvarez I, Wünsch B.
J Med Chem (2018) 61 : 9666 -9690
PubMed 30350997 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 9.06 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL61479 SIRAMESINE 2.0 1 9.92
CHEMBL53325 1 9.17
CHEMBL291439 1 8.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL61479 SIRAMESINE Ki = 0.12 nM 9.92
CHEMBL53325 Ki = 0.68 nM 9.17
CHEMBL291439 Ki = 8.2 nM 8.09