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Assay Detail

CHEMBL3583976

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membranes after 120 mins by scintillation counting analysis
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 Autocuration

Target

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

Publication

Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.
Piekielna J, Perlikowska R, do-Rego JC, do-Rego JL, Cerlesi MC, Calo G, Kluczyk A, Łapiński K, Tömböly C, Janecka A.
ACS Med Chem Lett (2015) 6 : 579 -583
PubMed 26005537 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 9.15 9.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3580743 1 9.38
CHEMBL3580749 1 9.31
CHEMBL3580746 1 9.27
CHEMBL3580745 1 9.26
CHEMBL3580748 1 9.21
CHEMBL3582485 1 9.16
CHEMBL3582484 1 9.14
CHEMBL333357 ENDOMORPHIN 2 1 9.10
CHEMBL3580750 1 9.04
CHEMBL3582487 1 9.01
CHEMBL3580744 1 8.80
CHEMBL3580747 1 -
CHEMBL3582486 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3580743 IC50 = 0.42 nM 9.38
CHEMBL3580749 IC50 = 0.49 nM 9.31
CHEMBL3580746 IC50 = 0.54 nM 9.27
CHEMBL3580745 IC50 = 0.55 nM 9.26
CHEMBL3580748 IC50 = 0.61 nM 9.21
CHEMBL3582485 IC50 = 0.69 nM 9.16
CHEMBL3582484 IC50 = 0.72 nM 9.14
CHEMBL333357 ENDOMORPHIN 2 IC50 = 0.79 nM 9.10
CHEMBL3580750 IC50 = 0.92 nM 9.04
CHEMBL3582487 IC50 = 0.98 nM 9.01
CHEMBL3580744 IC50 = 1.6 nM 8.80
CHEMBL3580747 IC50 > 1000.0 nM -
CHEMBL3582486 IC50 > 1000.0 nM -