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Assay Detail

CHEMBL804967

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Binding
Inhibition of [3H]DTG binding to Sigma opioid receptor
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Binding of substituted and conformationally restricted derivatives of N-(3-phenyl-n-propyl)-1-phenyl-2-aminopropane at sigma-receptors.
Glennon RA, Ismaiel AM, Smith JD, Yousif M, el-Ashmawy M, Herndon JL, Fischer JB, Howie KJ, Server AC.
J Med Chem (1991) 34 : 1855 -1859
PubMed 1648139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.92 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19841 1 8.41
CHEMBL54 HALOPERIDOL 4.0 1 8.30
CHEMBL281619 1 8.22
CHEMBL53253 1 8.21
CHEMBL19541 1 8.20
CHEMBL296601 1 8.10
CHEMBL19802 1 8.06
CHEMBL298758 1 7.92
CHEMBL19082 1 7.75
CHEMBL25858 1 7.70
CHEMBL20337 1 7.66
CHEMBL20626 1 7.66
CHEMBL55317 1 7.56
CHEMBL55318 1 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19841 Ki = 3.9 nM 8.41
CHEMBL54 HALOPERIDOL Ki = 5.0 nM 8.30
CHEMBL281619 Ki = 6.0 nM 8.22
CHEMBL53253 Ki = 6.2 nM 8.21
CHEMBL19541 Ki = 6.3 nM 8.20
CHEMBL296601 Ki = 7.9 nM 8.10
CHEMBL19802 Ki = 8.8 nM 8.06
CHEMBL298758 Ki = 12.0 nM 7.92
CHEMBL19082 Ki = 17.6 nM 7.75
CHEMBL25858 Ki = 20.0 nM 7.70
CHEMBL20337 Ki = 22.0 nM 7.66
CHEMBL20626 Ki = 21.8 nM 7.66
CHEMBL55317 Ki = 27.4 nM 7.56
CHEMBL55318 Ki = 83.2 nM 7.08