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Assay Detail

CHEMBL5043397

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

Binding
Displacement of [3H]-Diprenorphine from human mu opiod receptor expressed in CHO cells incubated for 1 hr by competition binding assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis, biological, and structural explorations of a series of μ-opioid receptor (MOR) agonists with high G protein signaling bias.
Yang Y, Wang Y, Zuo A, Li C, Wang W, Jiang W, Zhang X, Che X, Zhang Y, Wu W, Cen X, Wang H, Tian J.
Eur J Med Chem (2022) 228 : 113986 -113986
PubMed 34802839 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 9.11 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5083403 1 9.29
CHEMBL38874 DAMGO 1 9.19
CHEMBL2443262 OLICERIDINE 4.0 1 8.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5083403 Ki = 0.514 nM 9.29
CHEMBL38874 DAMGO Ki = 0.64 nM 9.19
CHEMBL2443262 OLICERIDINE Ki = 1.456 nM 8.84