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Assay Detail

CHEMBL5629584

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

Binding
Displacement of 3H-SB-674042 from human Ox1R expressed in CHO cell membranes by liquid scintillation counting method
6
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Orexin/Hypocretin receptor type 1 (CHEMBL5113)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and first-time disclosure of CVN766, an exquisitely selective orexin 1 receptor antagonist.
Glen A, Bürli RW, Livermore D, Buffham W, Merison S, Rowland AE, Newman R, Fieldhouse C, Miller DJ, Dawson LA, Matthews K, Carlton MB, Brice NL.
Bioorg Med Chem Lett (2024) 100 : 129629 -129629
PubMed 38295907 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.93 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1083659 SUVOREXANT 4.0 1 9.17
CHEMBL3958101 CVN-766 1.0 1 8.14
CHEMBL3932722 2 7.74
CHEMBL3954899 1 7.68
CHEMBL3957941 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1083659 SUVOREXANT Ki = 0.6761 nM 9.17
CHEMBL3958101 CVN-766 Ki = 7.244 nM 8.14
CHEMBL3932722 Ki = 18.2 nM 7.74
CHEMBL3932722 Ki = 18.2 nM 7.74
CHEMBL3954899 Ki = 20.89 nM 7.68
CHEMBL3957941 Ki = 81.28 nM 7.09