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Assay Detail

CHEMBL4732999

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-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by luminescence-based assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
Kumari S,Carmona AV,Tiwari AK,Trippier PC
J Med Chem (2020) 63 : 12290 -12358
PubMed 32686940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 8.06 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8234 ENKEPHALIN 1 8.89
CHEMBL4531563 1 7.22
CHEMBL4754251 1 -
CHEMBL4749699 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8234 ENKEPHALIN EC50 = 1.3 nM 8.89
CHEMBL4531563 EC50 = 60.0 nM 7.22
CHEMBL4754251 EC50 > 10000.0 nM -
CHEMBL4749699 EC50 > 10000.0 nM -