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Assay Detail

CHEMBL3630378

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

Functional
Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.
Liu X, Zhao L, Wang Y, Mou L, Yang J, Zhang Y, Wang D, Wang R.
Bioorg Med Chem Lett (2015) 25 : 5393 -5397
PubMed 26403932 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 9.41 10.20
Emax 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3629337 2 10.20
CHEMBL3627737 2 10.19
CHEMBL316446 ENDOMORPHIN-1 2 7.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3629337 EC50 = 0.0629 nM 10.20
CHEMBL3627737 EC50 = 0.0643 nM 10.19
CHEMBL316446 ENDOMORPHIN-1 EC50 = 14.4 nM 7.84
CHEMBL316446 ENDOMORPHIN-1 Emax = 83.13 % -
CHEMBL3629337 Emax = 98.22 % -
CHEMBL3627737 Emax = 97.01 % -