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Assay Detail

CHEMBL2412192

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 human/mouse HN9.10 cell membranes after 3 hrs by liquid scintillation counting analysis
18
Total Activities
11
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

Chiral Effect of a Phe Residue in Position 3 of the Dmt(1)-L(or D)-Tic(2) Analogues on Opioid Functional Activities.
Lee YS, Qu HC, Davis P, Ma SW, Vardanyan R, Lai J, Porreca F, Hruby VJ.
ACS Med Chem Lett (2013) 4 : 656 -659
PubMed 24648867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.50 9.92
IC50 7 7.97 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL538700 1 9.92
CHEMBL2408011 2 9.70
CHEMBL2408013 1 9.42
CHEMBL2408012 2 9.37
CHEMBL2408014 2 9.12
CHEMBL2408019 1 8.92
CHEMBL2408015 2 8.26
CHEMBL2408016 2 8.03
CHEMBL2408010 1 7.24
CHEMBL2408017 2 6.89
CHEMBL2408018 2 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL538700 Ki = 0.12 nM 9.92
CHEMBL2408011 Ki = 0.2 nM 9.70
CHEMBL2408013 Ki = 0.38 nM 9.42
CHEMBL2408012 Ki = 0.43 nM 9.37
CHEMBL2408011 IC50 = 0.4266 nM 9.37
CHEMBL2408012 IC50 = 0.6761 nM 9.17
CHEMBL2408014 Ki = 0.76 nM 9.12
CHEMBL2408019 Ki = 1.2 nM 8.92
CHEMBL2408014 IC50 = 1.585 nM 8.80
CHEMBL2408015 Ki = 5.5 nM 8.26
CHEMBL2408016 Ki = 9.3 nM 8.03
CHEMBL2408015 IC50 = 11.75 nM 7.93
CHEMBL2408016 IC50 = 20.42 nM 7.69
CHEMBL2408010 Ki = 57.0 nM 7.24
CHEMBL2408017 Ki = 130.0 nM 6.89
CHEMBL2408018 Ki = 250.0 nM 6.60
CHEMBL2408017 IC50 = 275.42 nM 6.56
CHEMBL2408018 IC50 = 524.81 nM 6.28