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Assay Detail

CHEMBL4410977

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Functional
Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay
10
Total Activities
10
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

Synthesis and μ-Opioid Activity of the Primary Metabolites of Carfentanil.
Hsu FL, Walz AJ, Myslinski JM, Kong L, Feasel MG, Goralski TDP, Rose T, Cooper NJ, Roughley N, Timperley CM.
ACS Med Chem Lett (2019) 10 : 1568 -1572
PubMed 31749912 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 9.44 10.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4588535 1 10.85
CHEMBL4578287 1 10.55
CHEMBL4548662 1 9.70
CHEMBL4524446 1 9.55
CHEMBL596 FENTANYL 4.0 1 9.29
CHEMBL4457592 1 8.36
CHEMBL4562635 1 7.77
CHEMBL290429 CARFENTANIL 2.0 1 -
CHEMBL4463749 1 -
CHEMBL4563672 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4588535 EC50 = 0.014 nM 10.85
CHEMBL4578287 EC50 = 0.028 nM 10.55
CHEMBL4548662 EC50 = 0.2 nM 9.70
CHEMBL4524446 EC50 = 0.28 nM 9.55
CHEMBL596 FENTANYL EC50 = 0.51 nM 9.29
CHEMBL4457592 EC50 = 4.4 nM 8.36
CHEMBL4562635 EC50 = 17.0 nM 7.77
CHEMBL290429 CARFENTANIL EC50 = 0.0049 nM -
CHEMBL4463749 EC50 = 0.0051 nM -
CHEMBL4563672 EC50 = 0.0024 nM -