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Assay Detail

CHEMBL4333170

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Functional
Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins
9
Total Activities
3
Compounds Tested
2
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

Discovery of two novel branched peptidomimetics containing endomorphin-2 and RF9 pharmacophores: Synthesis and neuropharmacological evaluation.
Zhang T, Han Z, Shi X, Zhao W, Wang Z, Zhang R, Xu B, Zhang M, Zhang Q, Xiao J, Zhu H, Zheng T, Fang Q.
Bioorg Med Chem (2019) 27 : 630 -643
PubMed 30626554 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.25 7.30
Emax 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333357 ENDOMORPHIN 2 3 7.30
CHEMBL4449491 3 5.80
CHEMBL4442534 3 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333357 ENDOMORPHIN 2 EC50 = 50.0 nM 7.30
CHEMBL333357 ENDOMORPHIN 2 EC50 = 63.1 nM 7.20
CHEMBL4449491 EC50 = 1584.89 nM 5.80
CHEMBL4449491 EC50 = 1770.0 nM 5.75
CHEMBL4442534 EC50 = 1900.0 nM 5.72
CHEMBL4442534 EC50 = 1995.26 nM 5.70
CHEMBL4449491 Emax = 54.3 % -
CHEMBL333357 ENDOMORPHIN 2 Emax = 76.8 % -
CHEMBL4442534 Emax = 62.0 % -