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Assay Detail

CHEMBL3269820

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in rat brain membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

In Vitro Membrane Permeation Studies and in Vivo Antinociception of Glycosylated Dmt(1)-DALDA Analogues.
Ballet S, Betti C, Novoa A, Tömböly C, Nielsen CU, Helms HC, Lesniak A, Kleczkowska P, Chung NN, Lipkowski AW, Brodin B, Tourwé D, Schiller PW.
ACS Med Chem Lett (2014) 5 : 352 -357
PubMed 24839540 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 9.27 9.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3264361 1 9.95
CHEMBL2181202 1 9.85
CHEMBL3264360 1 9.69
CHEMBL3264359 1 9.65
CHEMBL3264362 1 9.54
CHEMBL60444 1 8.77
CHEMBL3264358 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3264361 Ki = 0.112 nM 9.95
CHEMBL2181202 Ki = 0.143 nM 9.85
CHEMBL3264360 Ki = 0.203 nM 9.69
CHEMBL3264359 Ki = 0.222 nM 9.65
CHEMBL3264362 Ki = 0.286 nM 9.54
CHEMBL60444 Ki = 1.69 nM 8.77
CHEMBL3264358 Ki = 38.4 nM 7.42