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Assay Detail

CHEMBL846630

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

Binding
Binding affinity against sigma receptor from guinea pig brain, using [3H](+)-pentazocine as radioligand.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL287)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and receptor binding properties of fluoro- and iodo-substituted high affinity sigma receptor ligands: identification of potential PET and SPECT sigma receptor imaging agents.
de Costa B, Radesca L, Dominguez C, Di Paolo L, Bowen WD.
J Med Chem (1992) 35 : 2221 -2230
PubMed 1319493 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.60 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70540 1 9.41
CHEMBL312766 1 9.28
CHEMBL420557 1 8.92
CHEMBL71049 1 8.91
CHEMBL70861 1 8.29
CHEMBL324392 1 7.98
CHEMBL2368719 1 7.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70540 Ki = 0.39 nM 9.41
CHEMBL312766 Ki = 0.52 nM 9.28
CHEMBL420557 Ki = 1.19 nM 8.92
CHEMBL71049 Ki = 1.23 nM 8.91
CHEMBL70861 Ki = 5.07 nM 8.29
CHEMBL324392 Ki = 10.5 nM 7.98
CHEMBL2368719 Ki = 38.9 nM 7.41