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Assay Detail

CHEMBL3405076

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

Functional
Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, syntheses, and pharmacological characterization of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3'-carboxamido)morphinan analogues as opioid receptor ligands.
Yuan Y, Zaidi SA, Stevens DL, Scoggins KL, Mosier PD, Kellogg GE, Dewey WL, Selley DE, Zhang Y.
Bioorg Med Chem (2015) 23 : 1701 -1715
PubMed 25783191 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 8.24 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19019 NALTREXONE 4.0 1 9.80
CHEMBL2417568 1 8.97
CHEMBL2419119 1 8.94
CHEMBL2419122 1 8.91
CHEMBL2419121 1 8.76
CHEMBL2419124 1 8.58
CHEMBL522201 1 8.48
CHEMBL2419116 1 8.48
CHEMBL511142 BUPRENORPHINE 4.0 1 8.44
CHEMBL2419118 1 8.34
CHEMBL3401556 1 8.33
CHEMBL2419123 1 8.22
CHEMBL2419125 1 8.14
CHEMBL3401558 1 7.94
CHEMBL2419120 1 7.85
CHEMBL2419117 1 7.71
CHEMBL3401554 1 7.50
CHEMBL3401555 1 7.37
CHEMBL3401557 1 7.07
CHEMBL70 MORPHINE 4.0 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19019 NALTREXONE EC50 = 0.16 nM 9.80
CHEMBL2417568 EC50 = 1.06 nM 8.97
CHEMBL2419119 EC50 = 1.14 nM 8.94
CHEMBL2419122 EC50 = 1.23 nM 8.91
CHEMBL2419121 EC50 = 1.74 nM 8.76
CHEMBL2419124 EC50 = 2.62 nM 8.58
CHEMBL522201 EC50 = 3.3 nM 8.48
CHEMBL2419116 EC50 = 3.32 nM 8.48
CHEMBL511142 BUPRENORPHINE EC50 = 3.6 nM 8.44
CHEMBL2419118 EC50 = 4.6 nM 8.34
CHEMBL3401556 EC50 = 4.7 nM 8.33
CHEMBL2419123 EC50 = 6.0 nM 8.22
CHEMBL2419125 EC50 = 7.2 nM 8.14
CHEMBL3401558 EC50 = 11.4 nM 7.94
CHEMBL2419120 EC50 = 14.1 nM 7.85
CHEMBL2419117 EC50 = 19.4 nM 7.71
CHEMBL3401554 EC50 = 31.5 nM 7.50
CHEMBL3401555 EC50 = 42.7 nM 7.37
CHEMBL3401557 EC50 = 85.2 nM 7.07
CHEMBL70 MORPHINE EC50 = 120.0 nM 6.92