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Assay Detail

CHEMBL751253

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

Binding
Displacement of [3H]C1-DPDPE from human recombinant Opioid receptor delta 1 on CHO cell membranes.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
Grundt P, Jales AR, Traynor JR, Lewis JW, Husbands SM.
J Med Chem (2003) 46 : 1563 -1566
PubMed 12672258 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.45 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL567175 NALTRINDOLE 1 9.70
CHEMBL2113383 1 9.14
CHEMBL2113382 1 8.96
CHEMBL401093 OXYMORPHINDOLE 1 8.89
CHEMBL2113377 1 8.86
CHEMBL31421 1 8.77
CHEMBL2113378 1 8.71
CHEMBL2113381 1 8.68
CHEMBL2113376 1 8.54
CHEMBL2113373 1 8.37
CHEMBL573214 NORBINALTORPHIMINE 1 8.24
CHEMBL2113379 1 8.18
CHEMBL2113372 1 7.99
CHEMBL19019 NALTREXONE 4.0 1 7.97
CHEMBL2113380 1 7.63
CHEMBL38874 DAMGO 1 6.52
CHEMBL440765 U-69593 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL567175 NALTRINDOLE Ki = 0.2 nM 9.70
CHEMBL2113383 Ki = 0.73 nM 9.14
CHEMBL2113382 Ki = 1.1 nM 8.96
CHEMBL401093 OXYMORPHINDOLE Ki = 1.28 nM 8.89
CHEMBL2113377 Ki = 1.39 nM 8.86
CHEMBL31421 Ki = 1.7 nM 8.77
CHEMBL2113378 Ki = 1.95 nM 8.71
CHEMBL2113381 Ki = 2.07 nM 8.68
CHEMBL2113376 Ki = 2.88 nM 8.54
CHEMBL2113373 Ki = 4.23 nM 8.37
CHEMBL573214 NORBINALTORPHIMINE Ki = 5.7 nM 8.24
CHEMBL2113379 Ki = 6.55 nM 8.18
CHEMBL2113372 Ki = 10.3 nM 7.99
CHEMBL19019 NALTREXONE Ki = 10.8 nM 7.97
CHEMBL2113380 Ki = 23.6 nM 7.63
CHEMBL38874 DAMGO Ki = 300.0 nM 6.52
CHEMBL440765 U-69593 Ki > 10000.0 nM -