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Assay Detail

CHEMBL1045629

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 cells
15
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 8 8.59 9.18
IC50 7 8.21 8.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38874 DAMGO 2 9.18
CHEMBL595972 2 9.18
CHEMBL507340 2 9.18
CHEMBL611926 2 8.89
CHEMBL200199 BIPHALIN 1 8.59
CHEMBL611924 2 8.30
CHEMBL611925 2 8.11
CHEMBL592969 2 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38874 DAMGO Ki = 0.66 nM 9.18
CHEMBL595972 Ki = 0.66 nM 9.18
CHEMBL507340 Ki = 0.66 nM 9.18
CHEMBL611926 Ki = 1.3 nM 8.89
CHEMBL595972 IC50 = 1.38 nM 8.86
CHEMBL38874 DAMGO IC50 = 1.445 nM 8.84
CHEMBL507340 IC50 = 1.445 nM 8.84
CHEMBL200199 BIPHALIN Ki = 2.6 nM 8.59
CHEMBL611926 IC50 = 2.692 nM 8.57
CHEMBL611924 Ki = 5.0 nM 8.30
CHEMBL611925 Ki = 7.8 nM 8.11
CHEMBL611925 IC50 = 15.49 nM 7.81
CHEMBL611924 IC50 = 22.39 nM 7.65
CHEMBL592969 Ki = 54.0 nM 7.27
CHEMBL592969 IC50 = 117.49 nM 6.93