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Assay Detail

CHEMBL887073

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

Functional
Agonist activity at human cloned delta opioid receptor assessed as stimulation of [35S]GTP-gamma-S binding
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Dolle RE, Michaut M, Martinez-Teipel B, Belanger S, Graczyk TM, DeHaven RN.
Bioorg Med Chem Lett (2007) 17 : 2656 -2660
PubMed 17350835 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 7.28 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL247758 1 8.60
CHEMBL247760 1 8.46
CHEMBL246739 1 8.39
CHEMBL391580 1 8.28
CHEMBL246956 1 8.00
CHEMBL31421 1 7.68
CHEMBL246572 1 7.62
CHEMBL13786 1 7.33
CHEMBL247363 1 7.13
CHEMBL246479 1 7.01
CHEMBL247064 1 6.82
CHEMBL247368 1 6.52
CHEMBL2372104 1 6.50
CHEMBL247759 1 6.24
CHEMBL393867 1 6.14
CHEMBL246682 1 5.77
CHEMBL246740 1 -
CHEMBL247562 1 -
CHEMBL247163 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL247758 EC50 = 2.5 nM 8.60
CHEMBL247760 EC50 = 3.5 nM 8.46
CHEMBL246739 EC50 = 4.1 nM 8.39
CHEMBL391580 EC50 = 5.2 nM 8.28
CHEMBL246956 EC50 = 10.0 nM 8.00
CHEMBL31421 EC50 = 21.0 nM 7.68
CHEMBL246572 EC50 = 24.0 nM 7.62
CHEMBL13786 EC50 = 47.0 nM 7.33
CHEMBL247363 EC50 = 74.0 nM 7.13
CHEMBL246479 EC50 = 97.0 nM 7.01
CHEMBL247064 EC50 = 150.0 nM 6.82
CHEMBL247368 EC50 = 300.0 nM 6.52
CHEMBL2372104 EC50 = 320.0 nM 6.50
CHEMBL247759 EC50 = 580.0 nM 6.24
CHEMBL393867 EC50 = 730.0 nM 6.14
CHEMBL246682 EC50 = 1700.0 nM 5.77
CHEMBL246740 EC50 - -
CHEMBL247562 EC50 - -
CHEMBL247163 EC50 - -