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Assay Detail

CHEMBL896955

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

Functional
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.
Rennison D, Neal AP, Cami-Kobeci G, Aceto MD, Martinez-Bermejo F, Lewis JW, Husbands SM.
J Med Chem (2007) 50 : 5176 -5182
PubMed 17887741 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 8.09 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113304 1 9.60
CHEMBL2113305 1 9.52
CHEMBL2113308 1 8.89
CHEMBL2113307 1 8.61
CHEMBL2113313 1 8.59
CHEMBL2113314 1 8.51
CHEMBL2113303 1 8.51
CHEMBL2113312 1 8.27
CHEMBL2113311 1 8.26
CHEMBL2113296 1 7.97
CHEMBL2113301 1 7.93
CHEMBL2113300 1 7.84
CHEMBL511142 BUPRENORPHINE 4.0 1 7.83
CHEMBL2113295 1 7.82
CHEMBL70 MORPHINE 4.0 1 7.81
CHEMBL2113299 1 7.58
CHEMBL2113294 1 7.38
CHEMBL2113302 1 7.13
CHEMBL2113309 1 6.86
CHEMBL2113310 1 6.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113304 EC50 = 0.25 nM 9.60
CHEMBL2113305 EC50 = 0.3 nM 9.52
CHEMBL2113308 EC50 = 1.3 nM 8.89
CHEMBL2113307 EC50 = 2.46 nM 8.61
CHEMBL2113313 EC50 = 2.59 nM 8.59
CHEMBL2113314 EC50 = 3.1 nM 8.51
CHEMBL2113303 EC50 = 3.12 nM 8.51
CHEMBL2113312 EC50 = 5.37 nM 8.27
CHEMBL2113311 EC50 = 5.51 nM 8.26
CHEMBL2113296 EC50 = 10.6 nM 7.97
CHEMBL2113301 EC50 = 11.7 nM 7.93
CHEMBL2113300 EC50 = 14.3 nM 7.84
CHEMBL511142 BUPRENORPHINE EC50 = 14.8 nM 7.83
CHEMBL2113295 EC50 = 15.1 nM 7.82
CHEMBL70 MORPHINE EC50 = 15.6 nM 7.81
CHEMBL2113299 EC50 = 26.0 nM 7.58
CHEMBL2113294 EC50 = 41.5 nM 7.38
CHEMBL2113302 EC50 = 74.2 nM 7.13
CHEMBL2113309 EC50 = 139.0 nM 6.86
CHEMBL2113310 EC50 = 149.0 nM 6.83