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Assay Detail

CHEMBL861290

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Functional
Inhibition of [35S]GTP-gamma-S binding to human delta opioid receptor expressed in CHO cells
33
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
Lee YS, Agnes RS, Badghisi H, Davis P, Ma SW, Lai J, Porreca F, Hruby VJ.
J Med Chem (2006) 49 : 1773 -1780
PubMed 16509592 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 8.12 9.28
Emax 11 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL408889 3 9.28
CHEMBL200199 BIPHALIN 3 8.96
CHEMBL412331 3 8.89
CHEMBL31421 3 8.80
CHEMBL438739 3 8.25
CHEMBL375412 3 8.03
CHEMBL374325 3 7.60
CHEMBL405192 3 7.57
CHEMBL408832 3 7.57
CHEMBL442483 3 7.27
CHEMBL413644 3 7.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL408889 EC50 = 0.53 nM 9.28
CHEMBL408889 EC50 = 0.5248 nM 9.28
CHEMBL200199 BIPHALIN EC50 = 1.1 nM 8.96
CHEMBL200199 BIPHALIN EC50 = 1.122 nM 8.95
CHEMBL412331 EC50 = 1.3 nM 8.89
CHEMBL412331 EC50 = 1.318 nM 8.88
CHEMBL31421 EC50 = 1.585 nM 8.80
CHEMBL31421 EC50 = 1.6 nM 8.80
CHEMBL438739 EC50 = 5.6 nM 8.25
CHEMBL438739 EC50 = 5.623 nM 8.25
CHEMBL375412 EC50 = 9.4 nM 8.03
CHEMBL375412 EC50 = 9.333 nM 8.03
CHEMBL374325 EC50 = 25.12 nM 7.60
CHEMBL374325 EC50 = 26.0 nM 7.58
CHEMBL408832 EC50 = 27.0 nM 7.57
CHEMBL405192 EC50 = 26.92 nM 7.57
CHEMBL405192 EC50 = 27.0 nM 7.57
CHEMBL408832 EC50 = 27.54 nM 7.56
CHEMBL442483 EC50 = 54.0 nM 7.27
CHEMBL442483 EC50 = 54.95 nM 7.26
CHEMBL413644 EC50 = 74.0 nM 7.13
CHEMBL413644 EC50 = 74.13 nM 7.13
CHEMBL408832 Emax = 25.0 % -
CHEMBL413644 Emax = 100.0 % -
CHEMBL438739 Emax = 61.0 % -
CHEMBL200199 BIPHALIN Emax = 83.0 % -
CHEMBL31421 Emax = 69.0 % -
CHEMBL375412 Emax = 65.0 % -
CHEMBL412331 Emax = 81.0 % -
CHEMBL408889 Emax = 70.0 % -
CHEMBL405192 Emax = 54.0 % -
CHEMBL374325 Emax = 120.0 % -
CHEMBL442483 Emax = 72.0 % -