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Assay Detail

CHEMBL3270915

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Functional
Agonist activity at human mu opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL233)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP-receptor selective scaffolds. Part II.
Journigan VB, Polgar WE, Khroyan TV, Zaveri NT.
Bioorg Med Chem (2014) 22 : 2508 -2516
PubMed 24657054 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 6.95 7.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3262547 1 7.65
CHEMBL3262548 1 7.63
CHEMBL3262546 1 7.54
CHEMBL38874 DAMGO 1 7.49
CHEMBL3262549 1 7.40
CHEMBL3262544 1 7.25
CHEMBL3262545 1 7.09
CHEMBL3262542 1 6.39
CHEMBL3262551 1 6.17
CHEMBL3262543 1 6.13
CHEMBL3262552 1 5.68
CHEMBL3262550 1 -
CHEMBL3262553 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3262547 EC50 = 22.3 nM 7.65
CHEMBL3262548 EC50 = 23.4 nM 7.63
CHEMBL3262546 EC50 = 28.7 nM 7.54
CHEMBL38874 DAMGO EC50 = 32.6 nM 7.49
CHEMBL3262549 EC50 = 39.5 nM 7.40
CHEMBL3262544 EC50 = 56.9 nM 7.25
CHEMBL3262545 EC50 = 81.4 nM 7.09
CHEMBL3262542 EC50 = 409.0 nM 6.39
CHEMBL3262551 EC50 = 673.0 nM 6.17
CHEMBL3262543 EC50 = 745.0 nM 6.13
CHEMBL3262552 EC50 = 2110.0 nM 5.68
CHEMBL3262550 EC50 > 10000.0 nM -
CHEMBL3262553 EC50 > 10000.0 nM -