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Assay Detail

CHEMBL5133629

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

Binding
Displacement of [3H]-DAMGO from Sprague-Dawley rat brain membrane mu opioid receptor incubated for 45 mins by liquid scintillation counting analysis
11
Total Activities
11
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

Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation.
Dichiara M, Artacho-Cordón A, Turnaturi R, Santos-Caballero M, González-Cano R, Pasquinucci L, Barbaraci C, Rodríguez-Gómez I, Gómez-Guzmán M, Marrazzo A, Cobos EJ, Amata E.
Eur J Med Chem (2022) 230 : 114091 -114091
PubMed 35016113 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.59 8.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38874 DAMGO 1 8.83
CHEMBL5194022 1 6.09
CHEMBL5178450 1 5.84
CHEMBL5194121 1 5.59
CHEMBL3596572 1 -
CHEMBL335258 TEREPHTHALAMIC ACID 1 -
CHEMBL5192985 1 -
CHEMBL5198792 1 -
CHEMBL5205647 1 -
CHEMBL5190377 1 -
CHEMBL5203238 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38874 DAMGO Ki = 1.49 nM 8.83
CHEMBL5194022 Ki = 817.0 nM 6.09
CHEMBL5178450 Ki = 1458.0 nM 5.84
CHEMBL5194121 Ki = 2551.0 nM 5.59
CHEMBL3596572 Ki > 10000.0 nM -
CHEMBL335258 TEREPHTHALAMIC ACID Ki > 10000.0 nM -
CHEMBL5192985 Ki > 10000.0 nM -
CHEMBL5198792 Ki > 10000.0 nM -
CHEMBL5205647 Ki > 10000.0 nM -
CHEMBL5190377 Ki > 10000.0 nM -
CHEMBL5203238 Ki > 10000.0 nM -