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Assay Detail

CHEMBL873626

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

Binding
The compound was tested for binding affinity against opioid receptor in rat brain membranes, using [3H]dihydromorphine as the radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Brain membranes
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Opioid receptor (CHEMBL2094129)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Irreversible blockage of opioid receptor types by ester homologues of beta-funaltrexamine.
Schoenecker JW, Takemori AE, Portoghese PS.
J Med Chem (1986) 29 : 1868 -1871
PubMed 3020246 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 9.35 10.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL293967 1 10.82
CHEMBL53563 1 9.52
CHEMBL301654 1 9.19
CHEMBL473136 1 8.99
CHEMBL54820 1 8.81
CHEMBL293145 1 8.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL293967 IC50 = 0.015 nM 10.82
CHEMBL53563 IC50 = 0.3 nM 9.52
CHEMBL301654 IC50 = 0.64 nM 9.19
CHEMBL473136 IC50 = 1.03 nM 8.99
CHEMBL54820 IC50 = 1.56 nM 8.81
CHEMBL293145 IC50 = 1.65 nM 8.78