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Assay Detail

CHEMBL1826107

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

Binding
Displacement of [3H]-pentazocine from sigma 1 receptor from guinea pig brain membrane
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Fluorescent derivatives of σ receptor ligand 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) as a tool for uptake and cellular localization studies in pancreatic tumor cells.
Abate C, Hornick JR, Spitzer D, Hawkins WG, Niso M, Perrone R, Berardi F.
J Med Chem (2011) 54 : 5858 -5867
PubMed 21744858 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.64 9.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53325 1 9.42
CHEMBL60542 (+)-PENTAZOCINE 1 8.58
CHEMBL1822599 1 8.04
CHEMBL1822600 1 7.70
CHEMBL1822597 1 7.10
CHEMBL1822598 1 7.02
CHEMBL1822595 1 5.59
CHEMBL1822596 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53325 Ki = 0.38 nM 9.42
CHEMBL60542 (+)-PENTAZOCINE Ki = 2.62 nM 8.58
CHEMBL1822599 Ki = 9.08 nM 8.04
CHEMBL1822600 Ki = 19.8 nM 7.70
CHEMBL1822597 Ki = 78.7 nM 7.10
CHEMBL1822598 Ki = 96.2 nM 7.02
CHEMBL1822595 Ki = 2570.0 nM 5.59
CHEMBL1822596 Ki > 5000.0 nM -