Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4308248

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

Functional
Agonist activity at Gi-coupled mu opioid receptor (unknown origin) expressed in HEK293T cells assessed as inhibition of cAMP production at pH 6.5 measured after 15 mins by Glo-Sensor assay
11
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

β-Fluorofentanyls Are pH-Sensitive Mu Opioid Receptor Agonists.
Rosas R, Huang XP, Roth BL, Dockendorff C.
ACS Med Chem Lett (2019) 10 : 1353 -1356
PubMed 31531209 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.25 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4471584 2 9.15
CHEMBL4468844 2 9.15
CHEMBL38874 DAMGO 1 8.71
CHEMBL596 FENTANYL 4.0 1 8.26
CHEMBL4441320 1 8.26
CHEMBL4458454 1 8.19
CHEMBL4550454 1 7.93
CHEMBL4516683 1 7.60
CHEMBL4537210 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4471584 IC50 = 0.7079 nM 9.15
CHEMBL4468844 IC50 = 0.7079 nM 9.15
CHEMBL4468844 IC50 = 0.71 nM 9.15
CHEMBL4471584 IC50 = 0.71 nM 9.15
CHEMBL38874 DAMGO IC50 = 1.95 nM 8.71
CHEMBL596 FENTANYL IC50 = 5.495 nM 8.26
CHEMBL4441320 IC50 = 5.495 nM 8.26
CHEMBL4458454 IC50 = 6.457 nM 8.19
CHEMBL4550454 IC50 = 11.75 nM 7.93
CHEMBL4516683 IC50 = 25.12 nM 7.60
CHEMBL4537210 IC50 = 5754.4 nM 5.24