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Assay Detail

CHEMBL751922

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

Functional
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 16 8.63 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113383 1 9.48
CHEMBL2113378 1 9.06
CHEMBL2113382 1 9.02
CHEMBL2113379 1 8.92
CHEMBL31421 1 8.89
CHEMBL2113373 1 8.85
CHEMBL2113381 1 8.48
CHEMBL2113377 1 8.33
CHEMBL2113380 1 8.12
CHEMBL2113376 1 8.07
CHEMBL2113372 1 7.72
CHEMBL38874 DAMGO 1 -
CHEMBL440765 U-69593 1 -
CHEMBL573214 NORBINALTORPHIMINE 1 -
CHEMBL19019 NALTREXONE 4.0 1 -
CHEMBL567175 NALTRINDOLE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113383 EC50 = 0.33 nM 9.48
CHEMBL2113378 EC50 = 0.87 nM 9.06
CHEMBL2113382 EC50 = 0.95 nM 9.02
CHEMBL2113379 EC50 = 1.2 nM 8.92
CHEMBL31421 EC50 = 1.3 nM 8.89
CHEMBL2113373 EC50 = 1.4 nM 8.85
CHEMBL2113381 EC50 = 3.3 nM 8.48
CHEMBL2113377 EC50 = 4.71 nM 8.33
CHEMBL2113380 EC50 = 7.53 nM 8.12
CHEMBL2113376 EC50 = 8.6 nM 8.07
CHEMBL2113372 EC50 = 19.0 nM 7.72
CHEMBL38874 DAMGO EC50 > 10000.0 nM -
CHEMBL440765 U-69593 EC50 > 10000.0 nM -
CHEMBL573214 NORBINALTORPHIMINE EC50 = 4.42 Ke nM-1 -
CHEMBL19019 NALTREXONE EC50 = 5.44 Ke nM-1 -
CHEMBL567175 NALTRINDOLE EC50 = 0.11 Ke nM-1 -