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Assay Detail

CHEMBL805614

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

Binding
Opioid activity in terms of inhibition of [3H]dihydromorphine binding to opioid receptor mu in rat brain membrane.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

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 7 7.78 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20768 1 8.17
CHEMBL293952 1 8.08
CHEMBL53170 1 8.02
CHEMBL20807 1 7.98
CHEMBL54808 1 7.57
CHEMBL282433 DITOLYLGUANIDINE 1 7.54
CHEMBL276500 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20768 Ki = 6.8 nM 8.17
CHEMBL293952 Ki = 8.3 nM 8.08
CHEMBL53170 Ki = 9.5 nM 8.02
CHEMBL20807 Ki = 10.4 nM 7.98
CHEMBL54808 Ki = 27.1 nM 7.57
CHEMBL282433 DITOLYLGUANIDINE Ki = 28.8 nM 7.54
CHEMBL276500 Ki = 78.5 nM 7.11