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Assay Detail

CHEMBL3771652

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

Functional
Antagonist activity at human OX1R expressed in CHO cell membranes assessed as inhibition of orexin-A-induced intracellular calcium release after 120 mins
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.
Roecker AJ, Cox CD, Coleman PJ.
J Med Chem (2016) 59 : 504 -530
PubMed 26317591 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.96 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2107822 FILOREXANT 2.0 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2107822 FILOREXANT IC50 = 11.0 nM 7.96