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Assay Detail

CHEMBL2186560

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

Binding
Displacement of [3H]di-o-tolylguanidine from Sigma2 receptor in rat liver homogenate
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

New positron emission tomography (PET) radioligand for imaging σ-1 receptors in living subjects.
James ML, Shen B, Zavaleta CL, Nielsen CH, Mesangeau C, Vuppala PK, Chan C, Avery BA, Fishback JA, Matsumoto RR, Gambhir SS, McCurdy CR, Chin FT.
J Med Chem (2012) 55 : 8272 -8282
PubMed 22853801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.73 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 7.24
CHEMBL272899 1 6.61
CHEMBL2181924 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 57.2 nM 7.24
CHEMBL272899 Ki = 247.0 nM 6.61
CHEMBL2181924 Ki = 467.0 nM 6.33