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Assay Detail

CHEMBL4701864

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

Binding
Agonist activity at human MOR expressed in human U2OS cells assessed as increase in beta arrestin2 recruitment incubated for 90 mins by pathhunter beta-arrestin assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies.
Gonzalez S,Dumitrascuta M,Eiselt E,Louis S,Kunze L,Blasiol A,Vivancos M,Previti S,Dewolf E,Martin C,Tourwé D,Cavelier F,Gendron L,Sarret P,Spetea M,Ballet S
J Med Chem (2020) 63 : 12929 -12941
PubMed 32902268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 6.08 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3408737 1 8.26
CHEMBL4745899 1 6.45
CHEMBL4742666 1 6.03
CHEMBL4761165 1 6.02
CHEMBL4776986 1 5.97
CHEMBL4798887 1 5.94
CHEMBL4747286 1 5.90
CHEMBL4789659 1 5.88
CHEMBL4758754 1 5.71
CHEMBL4750783 1 5.67
CHEMBL4744531 1 5.61
CHEMBL4749016 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3408737 EC50 = 5.53 nM 8.26
CHEMBL4745899 EC50 = 359.0 nM 6.45
CHEMBL4742666 EC50 = 934.0 nM 6.03
CHEMBL4761165 EC50 = 956.0 nM 6.02
CHEMBL4776986 EC50 = 1066.0 nM 5.97
CHEMBL4798887 EC50 = 1142.0 nM 5.94
CHEMBL4747286 EC50 = 1271.0 nM 5.90
CHEMBL4789659 EC50 = 1329.0 nM 5.88
CHEMBL4758754 EC50 = 1965.0 nM 5.71
CHEMBL4750783 EC50 = 2163.0 nM 5.67
CHEMBL4744531 EC50 = 2459.0 nM 5.61
CHEMBL4749016 EC50 = 3044.0 nM 5.52