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Assay Detail

CHEMBL3395401

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

Binding
Antagonist activity at human OX1R by FLIPR assay
2
Total Activities
2
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

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

Publication

Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.
Raheem IT, Breslin MJ, Bruno J, Cabalu TD, Cooke A, Cox CD, Cui D, Garson S, Gotter AL, Fox SV, Harrell CM, Kuduk SD, Lemaire W, Prueksaritanont T, Renger JJ, Stump C, Tannenbaum PL, Williams PD, Winrow CJ, Coleman PJ.
Bioorg Med Chem Lett (2015) 25 : 444 -450
PubMed 25577040 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.61 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2107822 FILOREXANT 2.0 1 7.80
CHEMBL3394842 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2107822 FILOREXANT IC50 = 16.0 nM 7.80
CHEMBL3394842 IC50 = 3908.0 nM 5.41