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Assay Detail

CHEMBL753818

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Binding
Tested for the binding affinity against the Delta opioid receptor in guinea pig brain using [3H]DPDPE
15
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

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol.
Nelson TD, Davis RD, Nelson WL.
J Med Chem (1994) 37 : 4270 -4277
PubMed 7996538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.70 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2111914 1 8.85
CHEMBL2112732 1 8.54
CHEMBL2112740 1 8.26
CHEMBL2111912 1 8.18
CHEMBL19019 NALTREXONE 4.0 1 8.00
CHEMBL2112730 1 7.96
CHEMBL2111913 1 7.72
CHEMBL2111911 1 7.70
CHEMBL2112729 1 7.60
CHEMBL140278 2 7.58
CHEMBL423341 1 7.52
CHEMBL2111916 1 7.44
CHEMBL2112736 1 7.32
CHEMBL31421 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2111914 IC50 = 1.4 nM 8.85
CHEMBL2112732 IC50 = 2.9 nM 8.54
CHEMBL2112740 IC50 = 5.5 nM 8.26
CHEMBL2111912 IC50 = 6.6 nM 8.18
CHEMBL19019 NALTREXONE IC50 = 10.0 nM 8.00
CHEMBL2112730 IC50 = 11.0 nM 7.96
CHEMBL2111913 IC50 = 19.0 nM 7.72
CHEMBL2111911 IC50 = 20.0 nM 7.70
CHEMBL2112729 IC50 = 25.0 nM 7.60
CHEMBL140278 IC50 = 26.0 nM 7.58
CHEMBL423341 IC50 = 30.0 nM 7.52
CHEMBL140278 IC50 = 32.0 nM 7.50
CHEMBL2111916 IC50 = 36.0 nM 7.44
CHEMBL2112736 IC50 = 48.0 nM 7.32
CHEMBL31421 IC50 = 5000.0 nM 5.30