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Assay Detail

CHEMBL3370199

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

Binding
Agonist activity at myc-tagged mu opioid receptor (unknown origin) expressed in AtT-20 cells assessed as induction of membrane potential hyperpolarization
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type AtT20
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery, structure-activity relationship studies, and anti-nociceptive effects of 1-phenyl-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one as novel opioid receptor agonists.
Cheng MF, Ou LC, Chen SC, Chang WT, Law PY, Loh HH, Chao YS, Shih C, Yeh SH, Ueng SH.
Bioorg Med Chem (2014) 22 : 4694 -4703
PubMed 25087049 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.32 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3325715 1 7.00
CHEMBL3325716 1 6.70
CHEMBL3325714 1 5.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3325715 EC50 = 100.0 nM 7.00
CHEMBL3325716 EC50 = 200.0 nM 6.70
CHEMBL3325714 EC50 = 5490.0 nM 5.26