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Assay Detail

CHEMBL4673766

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

Binding
Displacement of [3H]-pentazocine from guinea pig brain sigma 1 receptor incubated for 120 mins by liquid scintillation counting method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
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 and sigma receptor affinity of spiro[[2]benzopyran-1,1-cyclohexanes] with an exocyclic amino moiety in the 3-position
Kronenberg, Elisabeth, Weber, Frauke, Schepmann, Dirk, Wunsch, Bernhard
RSC Med Chem (2021) 12 : 237 -244
PubMed 34046612 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.52 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL100116 PENTAZOCINE 4.0 1 8.27
CHEMBL4761627 1 8.27
CHEMBL4792455 1 7.82
CHEMBL282433 DITOLYLGUANIDINE 1 7.15
CHEMBL4797610 1 7.02
CHEMBL4781486 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL100116 PENTAZOCINE Ki = 5.4 nM 8.27
CHEMBL4761627 Ki = 5.4 nM 8.27
CHEMBL4792455 Ki = 15.0 nM 7.82
CHEMBL282433 DITOLYLGUANIDINE Ki = 71.0 nM 7.15
CHEMBL4797610 Ki = 95.0 nM 7.02
CHEMBL4781486 Ki = 278.0 nM 6.56