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Assay Detail

CHEMBL861286

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

Binding
Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 cells
18
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
Lee YS, Agnes RS, Badghisi H, Davis P, Ma SW, Lai J, Porreca F, Hruby VJ.
J Med Chem (2006) 49 : 1773 -1780
PubMed 16509592 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.08 9.38
Ki 9 8.43 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL408832 2 9.64
CHEMBL412331 2 9.32
CHEMBL374325 2 9.09
CHEMBL375412 2 8.85
CHEMBL438739 2 8.47
CHEMBL408889 2 8.28
CHEMBL442483 2 7.64
CHEMBL413644 2 7.35
CHEMBL405192 2 7.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL408832 Ki = 0.23 nM 9.64
CHEMBL408832 IC50 = 0.4169 nM 9.38
CHEMBL412331 Ki = 0.48 nM 9.32
CHEMBL374325 Ki = 0.82 nM 9.09
CHEMBL412331 IC50 = 1.122 nM 8.95
CHEMBL375412 Ki = 1.4 nM 8.85
CHEMBL374325 IC50 = 1.995 nM 8.70
CHEMBL375412 IC50 = 3.236 nM 8.49
CHEMBL438739 Ki = 3.4 nM 8.47
CHEMBL408889 Ki = 5.2 nM 8.28
CHEMBL438739 IC50 = 7.762 nM 8.11
CHEMBL408889 IC50 = 10.72 nM 7.97
CHEMBL442483 Ki = 23.0 nM 7.64
CHEMBL413644 Ki = 45.0 nM 7.35
CHEMBL442483 IC50 = 53.7 nM 7.27
CHEMBL405192 Ki = 59.0 nM 7.23
CHEMBL413644 IC50 = 93.33 nM 7.03
CHEMBL405192 IC50 = 138.04 nM 6.86