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Assay Detail

CHEMBL4158769

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

Binding
Displacement of [3H](+)-pentazocine from sigma1 receptor in quinea pig brain membranes
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL4153)
Type SINGLE PROTEIN
Organism Cavia porcellus

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 7.36 9.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53325 1 9.42
CHEMBL61479 SIRAMESINE 2.0 1 7.77
CHEMBL291439 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53325 Ki = 0.38 nM 9.42
CHEMBL61479 SIRAMESINE Ki = 17.0 nM 7.77
CHEMBL291439 Ki = 12900.0 nM 4.89