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Assay Detail

CHEMBL5535127

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

Binding
Binding affinity to recombinant human alpha-1A-Adr expressed in HEK cells assessed as inhibition constant
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1A adrenergic receptor (CHEMBL229)
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 2 7.87 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2 PRAZOSIN 4.0 1 9.89
CHEMBL596 FENTANYL 4.0 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2 PRAZOSIN Ki = 0.13 nM 9.89
CHEMBL596 FENTANYL Ki = 1407.0 nM 5.85