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Assay Detail

CHEMBL950319

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membrane
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis of a potent and selective (18)F-labeled delta-opioid receptor antagonist derived from the Dmt-Tic pharmacophore for positron emission tomography imaging.
Ryu EK, Wu Z, Chen K, Lazarus LH, Marczak ED, Sasaki Y, Ambo A, Salvadori S, Ren C, Zhao H, Balboni G, Chen X.
J Med Chem (2008) 51 : 1817 -1823
PubMed 18311909 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.94 8.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL270984 1 8.56
CHEMBL269842 1 7.88
CHEMBL244265 1 7.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL270984 Ki = 2.75 nM 8.56
CHEMBL269842 Ki = 13.2 nM 7.88
CHEMBL244265 Ki = 41.2 nM 7.38