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Assay Detail

CHEMBL5043376

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

Functional
Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry
27
Total Activities
27
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

Synthesis, biological, and structural explorations of a series of μ-opioid receptor (MOR) agonists with high G protein signaling bias.
Yang Y, Wang Y, Zuo A, Li C, Wang W, Jiang W, Zhang X, Che X, Zhang Y, Wu W, Cen X, Wang H, Tian J.
Eur J Med Chem (2022) 228 : 113986 -113986
PubMed 34802839 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 26 8.27 10.15
Emax 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5074742 1 10.15
CHEMBL5082714 1 10.00
CHEMBL5084800 1 9.70
CHEMBL5083403 1 9.46
CHEMBL5075300 1 9.34
CHEMBL5082522 1 9.30
CHEMBL2443262 OLICERIDINE 4.0 1 8.74
CHEMBL5078909 1 8.74
CHEMBL38874 DAMGO 1 8.71
CHEMBL5077763 1 8.70
CHEMBL5093645 1 8.59
CHEMBL5093937 1 8.39
CHEMBL5088860 1 8.21
CHEMBL5087703 1 8.17
CHEMBL4467777 1 8.00
CHEMBL5079835 1 7.94
CHEMBL5084268 1 7.89
CHEMBL5079983 1 7.85
CHEMBL5085321 1 7.70
CHEMBL5080554 1 7.70
CHEMBL5083135 1 7.65
CHEMBL5069961 1 7.58
CHEMBL5091110 1 7.21
CHEMBL5092009 1 6.76
CHEMBL5077091 1 6.75
CHEMBL5090537 1 5.71
CHEMBL5088559 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5074742 EC50 = 0.07 nM 10.15
CHEMBL5082714 EC50 = 0.1 nM 10.00
CHEMBL5084800 EC50 = 0.2 nM 9.70
CHEMBL5083403 EC50 = 0.35 nM 9.46
CHEMBL5075300 EC50 = 0.46 nM 9.34
CHEMBL5082522 EC50 = 0.5 nM 9.30
CHEMBL2443262 OLICERIDINE EC50 = 1.8 nM 8.74
CHEMBL5078909 EC50 = 1.8 nM 8.74
CHEMBL38874 DAMGO EC50 = 1.97 nM 8.71
CHEMBL5077763 EC50 = 2.0 nM 8.70
CHEMBL5093645 EC50 = 2.6 nM 8.59
CHEMBL5093937 EC50 = 4.1 nM 8.39
CHEMBL5088860 EC50 = 6.1 nM 8.21
CHEMBL5087703 EC50 = 6.8 nM 8.17
CHEMBL4467777 EC50 = 10.0 nM 8.00
CHEMBL5079835 EC50 = 11.6 nM 7.94
CHEMBL5084268 EC50 = 12.8 nM 7.89
CHEMBL5079983 EC50 = 14.1 nM 7.85
CHEMBL5085321 EC50 = 19.9 nM 7.70
CHEMBL5080554 EC50 = 20.0 nM 7.70
CHEMBL5083135 EC50 = 22.3 nM 7.65
CHEMBL5069961 EC50 = 26.5 nM 7.58
CHEMBL5091110 EC50 = 61.6 nM 7.21
CHEMBL5092009 EC50 = 174.2 nM 6.76
CHEMBL5077091 EC50 = 178.0 nM 6.75
CHEMBL5090537 EC50 = 1930.2 nM 5.71
CHEMBL5088559 Emax = 0.19 nM -