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Assay Detail

CHEMBL2412191

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

Binding
Displacement of [3H]DAMGO from rat mu 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 Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 8.13 9.35
IC50 7 7.94 9.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2408014 2 9.35
CHEMBL538700 1 8.92
CHEMBL2408016 2 8.72
CHEMBL2408010 1 8.42
CHEMBL2408018 2 8.19
CHEMBL2408011 2 8.02
CHEMBL2408017 2 7.92
CHEMBL2408015 2 7.85
CHEMBL2408012 2 7.82
CHEMBL2408013 1 7.66
CHEMBL2408019 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2408014 Ki = 0.45 nM 9.35
CHEMBL2408014 IC50 = 0.955 nM 9.02
CHEMBL538700 Ki = 1.2 nM 8.92
CHEMBL2408016 Ki = 1.9 nM 8.72
CHEMBL2408010 Ki = 3.8 nM 8.42
CHEMBL2408016 IC50 = 4.074 nM 8.39
CHEMBL2408018 Ki = 6.4 nM 8.19
CHEMBL2408011 Ki = 9.5 nM 8.02
CHEMBL2408017 Ki = 12.0 nM 7.92
CHEMBL2408018 IC50 = 13.49 nM 7.87
CHEMBL2408015 Ki = 14.0 nM 7.85
CHEMBL2408012 Ki = 15.0 nM 7.82
CHEMBL2408011 IC50 = 19.95 nM 7.70
CHEMBL2408013 Ki = 22.0 nM 7.66
CHEMBL2408017 IC50 = 25.12 nM 7.60
CHEMBL2408015 IC50 = 28.84 nM 7.54
CHEMBL2408012 IC50 = 32.36 nM 7.49
CHEMBL2408019 Ki = 280.0 nM 6.55