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Assay Detail

CHEMBL755204

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

Binding
Inhibition of [3H]-DPDPE binding to Opioid receptor delta 1 of rat brain membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

Delta-type opioid receptor (CHEMBL269)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for mu opioid receptors.
Pelton JT, Kazmierski W, Gulya K, Yamamura HI, Hruby VJ.
J Med Chem (1986) 29 : 2370 -2375
PubMed 2878079 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.08 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1790572 1 5.70
CHEMBL1823872 SOMATOSTATIN 3.0 1 5.70
CHEMBL384284 1 5.55
CHEMBL413950 1 5.35
CHEMBL414987 1 5.25
CHEMBL437283 1 5.08
CHEMBL507214 1 4.87
CHEMBL274298 1 4.56
CHEMBL440061 1 4.50
CHEMBL263342 1 4.24
CHEMBL274400 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1790572 IC50 = 2000.0 nM 5.70
CHEMBL1823872 SOMATOSTATIN IC50 = 2000.0 nM 5.70
CHEMBL384284 IC50 = 2800.0 nM 5.55
CHEMBL413950 IC50 = 4500.0 nM 5.35
CHEMBL414987 IC50 = 5600.0 nM 5.25
CHEMBL437283 IC50 = 8400.0 nM 5.08
CHEMBL507214 IC50 = 13500.0 nM 4.87
CHEMBL274298 IC50 = 27500.0 nM 4.56
CHEMBL440061 IC50 = 32000.0 nM 4.50
CHEMBL263342 IC50 = 58000.0 nM 4.24
CHEMBL274400 IC50 > 70000.0 nM -