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Assay Detail

CHEMBL1024696

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 mouse HN9.10 cell membrane by liquid scintillation counting
7
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
Yamamoto T, Nair P, Jacobsen NE, Davis P, Ma SW, Navratilova E, Moye S, Lai J, Yamamura HI, Vanderah TW, Porreca F, Hruby VJ.
J Med Chem (2008) 51 : 6334 -6347
PubMed 18821747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.92 9.36
IC50 3 8.70 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL448998 2 9.36
CHEMBL507340 2 9.18
CHEMBL200199 BIPHALIN 1 8.59
CHEMBL389652 2 8.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL448998 Ki = 0.44 nM 9.36
CHEMBL507340 Ki = 0.66 nM 9.18
CHEMBL448998 IC50 = 0.7943 nM 9.10
CHEMBL507340 IC50 = 1.585 nM 8.80
CHEMBL200199 BIPHALIN Ki = 2.6 nM 8.59
CHEMBL389652 Ki = 2.8 nM 8.55
CHEMBL389652 IC50 = 6.31 nM 8.20