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Assay Detail

CHEMBL1024702

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Functional
Agonist activity at human delta opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay
10
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 10 8.60 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200199 BIPHALIN 2 9.00
CHEMBL31421 2 8.80
CHEMBL448998 2 8.60
CHEMBL389652 2 8.54
CHEMBL507340 2 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200199 BIPHALIN EC50 = 1.0 nM 9.00
CHEMBL200199 BIPHALIN EC50 = 1.1 nM 8.96
CHEMBL31421 EC50 = 1.6 nM 8.80
CHEMBL31421 EC50 = 1.585 nM 8.80
CHEMBL448998 EC50 = 2.512 nM 8.60
CHEMBL448998 EC50 = 2.6 nM 8.59
CHEMBL389652 EC50 = 2.9 nM 8.54
CHEMBL389652 EC50 = 3.162 nM 8.50
CHEMBL507340 EC50 = 7.943 nM 8.10
CHEMBL507340 EC50 = 8.6 nM 8.07