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Assay Detail

CHEMBL5535105

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Binding
Binding affinity to MOR (unknown origin) assessed as inhibition constant
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Molecular Pharmacology Profiling of Phenylfentanil and Its Analogues to Understand the Putative Involvement of an Adrenergic Mechanism in Fentanyl-Induced Respiratory Depression.
Li M, Pagare PP, Ma H, St Onge CM, Mendez RE, Gillespie JC, Stevens DL, Dewey WL, Selley DE, Zhang Y.
J Med Chem (2024) 67 : 603 -619
PubMed 38156970 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 9.69 10.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL596 FENTANYL 4.0 1 10.08
CHEMBL982 NALMEFENE 4.0 1 9.52
CHEMBL19019 NALTREXONE 4.0 1 9.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL596 FENTANYL Ki = 0.083 nM 10.08
CHEMBL982 NALMEFENE Ki = 0.3 nM 9.52
CHEMBL19019 NALTREXONE Ki = 0.33 nM 9.48