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Assay Detail

CHEMBL1045633

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Functional
Agonist activity at human delta opioid receptor expressed in HN9.10 cells assessed as stimulation of [35S]GTPgammaS binding
12
Total Activities
6
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 biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.
Yamamoto T, Nair P, Ma SW, Davis P, Yamamura HI, Vanderah TW, Porreca F, Lai J, Hruby VJ.
Bioorg Med Chem (2009) 17 : 7337 -7343
PubMed 19762245 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 8.32 10.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL611926 2 10.76
CHEMBL200199 BIPHALIN 2 8.96
CHEMBL507340 2 8.07
CHEMBL592969 2 7.89
CHEMBL611924 2 7.29
CHEMBL611925 2 7.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL611926 EC50 = 0.01738 nM 10.76
CHEMBL611926 EC50 = 0.02 nM 10.70
CHEMBL200199 BIPHALIN EC50 = 1.1 nM 8.96
CHEMBL200199 BIPHALIN EC50 = 1.122 nM 8.95
CHEMBL507340 EC50 = 8.511 nM 8.07
CHEMBL507340 EC50 = 8.6 nM 8.07
CHEMBL592969 EC50 = 13.0 nM 7.89
CHEMBL592969 EC50 = 13.18 nM 7.88
CHEMBL611924 EC50 = 51.29 nM 7.29
CHEMBL611924 EC50 = 51.0 nM 7.29
CHEMBL611925 EC50 = 97.72 nM 7.01
CHEMBL611925 EC50 = 98.0 nM 7.01