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Assay Detail

CHEMBL867594

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor expressed in rat brain synaptosomal membranes
13
Total Activities
13
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 Expert

Target

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

Publication

Potent Dmt-Tic pharmacophoric delta- and mu-opioid receptor antagonists.
Li T, Fujita Y, Shiotani K, Miyazaki A, Tsuda Y, Ambo A, Sasaki Y, Jinsmaa Y, Marczak E, Bryant SD, Salvadori S, Lazarus LH, Okada Y.
J Med Chem (2005) 48 : 8035 -8044
PubMed 16335927 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.37 8.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196774 1 8.86
CHEMBL198646 1 8.81
CHEMBL261905 1 8.78
CHEMBL373668 1 8.76
CHEMBL197185 1 8.75
CHEMBL370399 1 8.66
CHEMBL370398 1 8.64
CHEMBL198800 1 8.55
CHEMBL381874 1 8.51
CHEMBL200890 1 8.43
CHEMBL373192 1 8.31
CHEMBL370197 1 8.24
CHEMBL571492 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196774 Ki = 1.37 nM 8.86
CHEMBL198646 Ki = 1.56 nM 8.81
CHEMBL261905 Ki = 1.68 nM 8.78
CHEMBL373668 Ki = 1.74 nM 8.76
CHEMBL197185 Ki = 1.79 nM 8.75
CHEMBL370399 Ki = 2.21 nM 8.66
CHEMBL370398 Ki = 2.28 nM 8.64
CHEMBL198800 Ki = 2.83 nM 8.55
CHEMBL381874 Ki = 3.08 nM 8.51
CHEMBL200890 Ki = 3.76 nM 8.43
CHEMBL373192 Ki = 4.86 nM 8.31
CHEMBL370197 Ki = 5.72 nM 8.24
CHEMBL571492 Ki = 3320.0 nM 5.48