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Assay Detail

CHEMBL905182

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
10
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, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
Yamamoto T, Nair P, Davis P, Ma SW, Navratilova E, Moye S, Tumati S, Lai J, Vanderah TW, Yamamura HI, Porreca F, Hruby VJ.
J Med Chem (2007) 50 : 2779 -2786
PubMed 17516639 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.08 8.89
IC50 8 7.58 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL340032 DADLE 1 8.89
CHEMBL439019 2 8.74
CHEMBL200199 BIPHALIN 1 8.59
CHEMBL389652 2 8.55
CHEMBL229280 2 8.32
CHEMBL389651 2 8.30
CHEMBL2371977 2 7.82
CHEMBL426363 2 7.44
CHEMBL387670 2 7.11
CHEMBL2371978 2 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL340032 DADLE Ki = 1.3 nM 8.89
CHEMBL439019 Ki = 1.8 nM 8.74
CHEMBL200199 BIPHALIN Ki = 2.6 nM 8.59
CHEMBL389652 Ki = 2.8 nM 8.55
CHEMBL439019 IC50 = 3.802 nM 8.42
CHEMBL229280 Ki = 4.8 nM 8.32
CHEMBL389651 Ki = 5.0 nM 8.30
CHEMBL389652 IC50 = 6.026 nM 8.22
CHEMBL389651 IC50 = 10.72 nM 7.97
CHEMBL229280 IC50 = 12.02 nM 7.92
CHEMBL2371977 Ki = 15.0 nM 7.82
CHEMBL2371977 IC50 = 31.62 nM 7.50
CHEMBL426363 Ki = 36.0 nM 7.44
CHEMBL426363 IC50 = 77.62 nM 7.11
CHEMBL387670 Ki = 77.0 nM 7.11
CHEMBL2371978 Ki = 93.0 nM 7.03
CHEMBL387670 IC50 = 162.18 nM 6.79
CHEMBL2371978 IC50 = 199.53 nM 6.70