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Assay Detail

CHEMBL1833036

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

Binding
Displacement of [3H]almorexant from recombinant human OX2R expressed in CHO cells
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Orexin receptor type 2 (CHEMBL4792)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
Di Fabio R, Pellacani A, Faedo S, Roth A, Piccoli L, Gerrard P, Porter RA, Johnson CN, Thewlis K, Donati D, Stasi L, Spada S, Stemp G, Nash D, Branch C, Kindon L, Massagrande M, Poffe A, Braggio S, Chiarparin E, Marchioro C, Ratti E, Corsi M.
Bioorg Med Chem Lett (2011) 21 : 5562 -5567
PubMed 21831639 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 8.89 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1272307 SB-649868 2.0 1 8.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1272307 SB-649868 Ki = 1.288 nM 8.89