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Assay Detail

CHEMBL1769552

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 mouse HN9.10 cells
11
Total Activities
6
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

Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.
Yamamoto T, Nair P, Largent-Milnes TM, Jacobsen NE, Davis P, Ma SW, Yamamura HI, Vanderah TW, Porreca F, Lai J, Hruby VJ.
J Med Chem (2011) 54 : 2029 -2038
PubMed 21366266 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.97 9.82
IC50 5 8.72 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1766207 2 9.82
CHEMBL1766208 2 9.74
CHEMBL1766205 2 9.34
CHEMBL200199 BIPHALIN 1 8.59
CHEMBL1766206 2 8.39
CHEMBL1766204 2 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1766207 Ki = 0.15 nM 9.82
CHEMBL1766208 Ki = 0.18 nM 9.74
CHEMBL1766207 IC50 = 0.3162 nM 9.50
CHEMBL1766208 IC50 = 0.3802 nM 9.42
CHEMBL1766205 Ki = 0.46 nM 9.34
CHEMBL1766205 IC50 = 0.9772 nM 9.01
CHEMBL200199 BIPHALIN Ki = 2.6 nM 8.59
CHEMBL1766206 Ki = 4.1 nM 8.39
CHEMBL1766206 IC50 = 8.511 nM 8.07
CHEMBL1766204 Ki = 11.0 nM 7.96
CHEMBL1766204 IC50 = 23.99 nM 7.62