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Assay Detail

CHEMBL905185

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Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay
20
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 20 8.07 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200199 BIPHALIN 2 8.96
CHEMBL31421 2 8.80
CHEMBL229280 2 8.74
CHEMBL389652 2 8.54
CHEMBL439019 2 8.40
CHEMBL389651 2 8.09
CHEMBL2371978 2 7.78
CHEMBL2371977 2 7.68
CHEMBL426363 2 7.30
CHEMBL387670 2 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200199 BIPHALIN EC50 = 1.1 nM 8.96
CHEMBL200199 BIPHALIN EC50 = 1.122 nM 8.95
CHEMBL31421 EC50 = 1.585 nM 8.80
CHEMBL31421 EC50 = 1.6 nM 8.80
CHEMBL229280 EC50 = 1.8 nM 8.74
CHEMBL229280 EC50 = 1.862 nM 8.73
CHEMBL389652 EC50 = 2.884 nM 8.54
CHEMBL389652 EC50 = 2.9 nM 8.54
CHEMBL439019 EC50 = 3.981 nM 8.40
CHEMBL439019 EC50 = 4.0 nM 8.40
CHEMBL389651 EC50 = 8.128 nM 8.09
CHEMBL389651 EC50 = 9.6 nM 8.02
CHEMBL2371978 EC50 = 16.6 nM 7.78
CHEMBL2371978 EC50 = 17.0 nM 7.77
CHEMBL2371977 EC50 = 21.0 nM 7.68
CHEMBL2371977 EC50 = 20.89 nM 7.68
CHEMBL426363 EC50 = 50.12 nM 7.30
CHEMBL426363 EC50 = 50.0 nM 7.30
CHEMBL387670 EC50 = 360.0 nM 6.44
CHEMBL387670 EC50 = 363.08 nM 6.44