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Assay Detail

CHEMBL757531

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

Binding
Displacement of [3H]DADLE at delta-opioid receptor
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Delta-type opioid receptor (CHEMBL3222)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.
McLamore S, Ullrich T, Rothman RB, Xu H, Dersch C, Coop A, Davis P, Porreca F, Jacobson AE, Rice KC.
J Med Chem (2001) 44 : 1471 -1474
PubMed 11311071 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.19 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1237164 NALTRINDOLE HYDROCHLORIDE 1 9.66
CHEMBL401093 OXYMORPHINDOLE 1 9.10
CHEMBL611695 1 8.70
CHEMBL608241 1 8.42
CHEMBL611697 1 8.33
CHEMBL611703 1 8.32
CHEMBL611704 1 8.30
CHEMBL611702 1 8.13
CHEMBL611700 1 8.08
CHEMBL611701 1 7.80
CHEMBL611696 1 7.60
CHEMBL611699 1 7.58
CHEMBL611698 1 7.48
CHEMBL611705 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1237164 NALTRINDOLE HYDROCHLORIDE Ki = 0.22 nM 9.66
CHEMBL401093 OXYMORPHINDOLE Ki = 0.8 nM 9.10
CHEMBL611695 Ki = 2.0 nM 8.70
CHEMBL608241 Ki = 3.8 nM 8.42
CHEMBL611697 Ki = 4.7 nM 8.33
CHEMBL611703 Ki = 4.8 nM 8.32
CHEMBL611704 Ki = 5.0 nM 8.30
CHEMBL611702 Ki = 7.4 nM 8.13
CHEMBL611700 Ki = 8.4 nM 8.08
CHEMBL611701 Ki = 16.0 nM 7.80
CHEMBL611696 Ki = 25.0 nM 7.60
CHEMBL611699 Ki = 26.0 nM 7.58
CHEMBL611698 Ki = 33.0 nM 7.48
CHEMBL611705 Ki = 79.0 nM 7.10