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Assay Detail

CHEMBL5033453

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

Functional
Agonist activity at human MOR expressed in CHO-K1 cells assessed as reduction in forskolin-induced cAMP production incubated for 45 mins by by HTRF assay
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Propionamide Derivatives as Dual μ-Opioid Receptor Agonists and σ<sub>1</sub> Receptor Antagonists for the Treatment of Pain.
García M, Llorente V, Garriga L, Christmann U, Rodríguez-Escrich S, Virgili M, Fernández B, Bordas M, Ayet E, Burgueño J, Pujol M, Dordal A, Portillo-Salido E, Gris G, Vela JM, Almansa C.
J Med Chem (2021) 64 : 10139 -10154
PubMed 34236190 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 46 6.93 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5089000 1 8.40
CHEMBL5090595 1 8.22
CHEMBL5081133 1 8.22
CHEMBL5084344 1 8.05
CHEMBL5094899 1 7.92
CHEMBL656 OXYCODONE 4.0 1 7.77
CHEMBL5083736 1 7.62
CHEMBL5070613 1 7.58
CHEMBL5073189 1 7.55
CHEMBL5087458 1 7.52
CHEMBL5087472 1 7.47
CHEMBL5089489 1 7.46
CHEMBL5076404 1 7.41
CHEMBL5089766 1 7.28
CHEMBL5075502 1 7.14
CHEMBL5089365 1 7.08
CHEMBL5080761 1 7.07
CHEMBL5092587 1 6.88
CHEMBL5085771 1 6.85
CHEMBL5077829 1 6.80
CHEMBL5093051 1 6.75
CHEMBL5086571 1 6.74
CHEMBL5090993 1 6.68
CHEMBL5080086 1 6.60
CHEMBL5084697 1 6.52
CHEMBL5084395 1 6.50
CHEMBL5076707 1 6.29
CHEMBL5083271 1 6.29
CHEMBL5081159 1 6.22
CHEMBL5079087 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5089000 EC50 = 4.0 nM 8.40
CHEMBL5090595 EC50 = 6.0 nM 8.22
CHEMBL5081133 EC50 = 6.0 nM 8.22
CHEMBL5084344 EC50 = 9.0 nM 8.05
CHEMBL5094899 EC50 = 12.0 nM 7.92
CHEMBL656 OXYCODONE EC50 = 17.0 nM 7.77
CHEMBL5083736 EC50 = 24.0 nM 7.62
CHEMBL5070613 EC50 = 26.0 nM 7.58
CHEMBL5073189 EC50 = 28.0 nM 7.55
CHEMBL5087458 EC50 = 30.0 nM 7.52
CHEMBL5087472 EC50 = 34.0 nM 7.47
CHEMBL5089489 EC50 = 35.0 nM 7.46
CHEMBL5076404 EC50 = 39.0 nM 7.41
CHEMBL5089766 EC50 = 53.0 nM 7.28
CHEMBL5075502 EC50 = 73.0 nM 7.14
CHEMBL5089365 EC50 = 84.0 nM 7.08
CHEMBL5080761 EC50 = 86.0 nM 7.07
CHEMBL5092587 EC50 = 133.0 nM 6.88
CHEMBL5085771 EC50 = 142.0 nM 6.85
CHEMBL5077829 EC50 = 158.0 nM 6.80
CHEMBL5093051 EC50 = 180.0 nM 6.75
CHEMBL5086571 EC50 = 183.0 nM 6.74
CHEMBL5090993 EC50 = 210.0 nM 6.68
CHEMBL5080086 EC50 = 253.0 nM 6.60
CHEMBL5084697 EC50 = 299.0 nM 6.52
CHEMBL5084395 EC50 = 314.0 nM 6.50
CHEMBL5076707 EC50 = 515.0 nM 6.29
CHEMBL5083271 EC50 = 510.0 nM 6.29
CHEMBL5081159 EC50 = 598.0 nM 6.22
CHEMBL5079087 EC50 = 720.0 nM 6.14
CHEMBL5081183 EC50 = 738.0 nM 6.13
CHEMBL5079310 EC50 = 869.0 nM 6.06
CHEMBL5093833 EC50 = 972.0 nM 6.01
CHEMBL5082661 EC50 = 1167.0 nM 5.93
CHEMBL5082031 EC50 = 1237.0 nM 5.91
CHEMBL5075152 EC50 = 1468.0 nM 5.83
CHEMBL5085710 EC50 = 4527.0 nM 5.34
CHEMBL5091094 EC50 > 10000.0 nM -
CHEMBL5072099 EC50 > 10000.0 nM -
CHEMBL5078587 EC50 > 1000.0 nM -
CHEMBL5079816 EC50 > 10000.0 nM -
CHEMBL5074927 EC50 > 1000.0 nM -
CHEMBL5094913 EC50 > 10000.0 nM -
CHEMBL5070185 EC50 > 10000.0 nM -
CHEMBL5077038 EC50 > 10000.0 nM -
CHEMBL2170062 EC50 > 10000.0 nM -