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Assay Detail

CHEMBL3239402

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

ADMET
Agonist activity at GFP-fused mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as recruitment of beta-arrestin-2 after 10 mins by BRET assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
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

Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity.
Cai J, Song B, Cai Y, Ma Y, Lam AL, Magiera J, Sekar S, Wyse BD, Ambo A, Sasaki Y, Lazarus LH, Smith MT, Li T.
Bioorg Med Chem (2014) 22 : 2208 -2219
PubMed 24613457 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.06 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3233197 1 8.20
CHEMBL3233014 1 7.73
CHEMBL38874 DAMGO 1 6.42
CHEMBL340032 DADLE 1 5.89
CHEMBL365983 1 -
CHEMBL3233191 1 -
CHEMBL3233192 1 -
CHEMBL3233193 1 -
CHEMBL3233194 1 -
CHEMBL3233195 1 -
CHEMBL3233196 1 -
CHEMBL3233198 1 -
CHEMBL3233199 1 -
CHEMBL3233200 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3233197 EC50 = 6.3 nM 8.20
CHEMBL3233014 EC50 = 18.6 nM 7.73
CHEMBL38874 DAMGO EC50 = 378.0 nM 6.42
CHEMBL340032 DADLE EC50 = 1300.0 nM 5.89
CHEMBL365983 EC50 - -
CHEMBL3233191 EC50 - -
CHEMBL3233192 EC50 - -
CHEMBL3233193 EC50 - -
CHEMBL3233194 EC50 - -
CHEMBL3233195 EC50 - -
CHEMBL3233196 EC50 - -
CHEMBL3233198 EC50 - -
CHEMBL3233199 EC50 - -
CHEMBL3233200 EC50 - -