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Assay Detail

CHEMBL934286

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Functional
Agonist activity at human delta opioid receptor by [35S]GTP-gamma-S binding assay
24
Total Activities
8
Compounds Tested
3
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

A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
Yamamoto T, Nair P, Vagner J, Largent-Milnes T, Davis P, Ma SW, Navratilova E, Moye S, Tumati S, Lai J, Yamamura HI, Vanderah TW, Porreca F, Hruby VJ.
J Med Chem (2008) 51 : 1369 -1376
PubMed 18266313 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Emax 8 - -
EC50 8 7.61 8.96
logEC50 8 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200199 BIPHALIN 3 8.96
CHEMBL31421 3 8.80
CHEMBL271619 3 7.77
CHEMBL261390 3 7.46
CHEMBL438389 3 7.10
CHEMBL261608 3 7.07
CHEMBL406030 3 6.92
CHEMBL272665 3 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200199 BIPHALIN EC50 = 1.1 nM 8.96
CHEMBL31421 EC50 = 1.6 nM 8.80
CHEMBL271619 EC50 = 17.0 nM 7.77
CHEMBL261390 EC50 = 35.0 nM 7.46
CHEMBL438389 EC50 = 80.0 nM 7.10
CHEMBL261608 EC50 = 85.0 nM 7.07
CHEMBL406030 EC50 = 120.0 nM 6.92
CHEMBL272665 EC50 = 150.0 nM 6.82
CHEMBL261390 Emax = 16.0 % -
CHEMBL31421 logEC50 = -8.8 -
CHEMBL406030 Emax = 137.0 % -
CHEMBL406030 logEC50 = -6.9 -
CHEMBL438389 Emax = 161.0 % -
CHEMBL438389 logEC50 = -7.1 -
CHEMBL31421 Emax = 69.0 % -
CHEMBL261390 logEC50 = -7.5 -
CHEMBL272665 logEC50 = -6.8 -
CHEMBL271619 Emax = 56.0 % -
CHEMBL271619 logEC50 = -7.8 -
CHEMBL200199 BIPHALIN logEC50 = -9.0 -
CHEMBL261608 Emax = 131.0 % -
CHEMBL261608 logEC50 = -7.1 -
CHEMBL200199 BIPHALIN Emax = 83.0 % -
CHEMBL272665 Emax = 70.0 % -