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Assay Detail

CHEMBL872697

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

Binding
Binding affinity towards sigma opioid receptor was determined in rat cerebral homogenate using [3H]haloperidol as radioligand
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL3602)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Identification and exploitation of the sigma-opiate pharmacophore.
Glennon RA, Smith JD, Ismaiel AM, el-Ashmawy M, Battaglia G, Fischer JB.
J Med Chem (1991) 34 : 1094 -1098
PubMed 1848295 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.50 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12047 1 8.41
CHEMBL20804 1 8.32
CHEMBL20626 1 7.85
CHEMBL20302 1 7.80
CHEMBL1907648 1 7.50
CHEMBL278585 1 7.34
CHEMBL1907647 1 7.14
CHEMBL1907644 N-BENZYLAMPHETAMINE 1 6.99
CHEMBL1907645 1 6.18
CHEMBL405 AMPHETAMINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12047 Ki = 3.9 nM 8.41
CHEMBL20804 Ki = 4.8 nM 8.32
CHEMBL20626 Ki = 14.0 nM 7.85
CHEMBL20302 Ki = 16.0 nM 7.80
CHEMBL1907648 Ki = 32.0 nM 7.50
CHEMBL278585 Ki = 46.0 nM 7.34
CHEMBL1907647 Ki = 73.0 nM 7.14
CHEMBL1907644 N-BENZYLAMPHETAMINE Ki = 103.0 nM 6.99
CHEMBL1907645 Ki = 664.0 nM 6.18
CHEMBL405 AMPHETAMINE Ki > 50000.0 nM -