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Assay Detail

CHEMBL2445161

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in CD1 mouse brain membranes after 1 hr by liquid scintillation counting
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mu-type opioid receptor (CHEMBL2858)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

N-Alkyl dien- and trienamides from the roots of Otanthus maritimus with binding affinity for opioid and cannabinoid receptors.
Ruiu S, Anzani N, Orrù A, Floris C, Caboni P, Maccioni E, Distinto S, Alcaro S, Cottiglia F.
Bioorg Med Chem (2013) 21 : 7074 -7082
PubMed 24095014 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 5.17 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL556578 MORPHINE HYDROCHLORIDE 3.0 1 8.92
CHEMBL2442642 1 5.24
CHEMBL2442643 1 5.13
CHEMBL2442641 1 5.12
CHEMBL426912 1 5.09
CHEMBL2442635 1 5.09
CHEMBL2442645 1 5.05
CHEMBL2442637 1 4.89
CHEMBL2442638 1 4.54
CHEMBL2442639 1 4.38
CHEMBL2442640 1 4.29
CHEMBL2442636 1 4.28
CHEMBL2442644 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL556578 MORPHINE HYDROCHLORIDE Ki = 1.2 nM 8.92
CHEMBL2442642 Ki = 5750.0 nM 5.24
CHEMBL2442643 Ki = 7400.0 nM 5.13
CHEMBL2442641 Ki = 7500.0 nM 5.12
CHEMBL426912 Ki = 8200.0 nM 5.09
CHEMBL2442635 Ki = 8100.0 nM 5.09
CHEMBL2442645 Ki = 9000.0 nM 5.05
CHEMBL2442637 Ki = 12800.0 nM 4.89
CHEMBL2442638 Ki = 29000.0 nM 4.54
CHEMBL2442639 Ki = 41500.0 nM 4.38
CHEMBL2442640 Ki = 51000.0 nM 4.29
CHEMBL2442636 Ki = 52000.0 nM 4.28
CHEMBL2442644 Ki > 50000.0 nM -