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Assay Detail

CHEMBL1833033

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

Functional
Antagonist activity at recombinant rat OX1R expressed in CHO cells by FLIPR calcium based functional assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Orexin/Hypocretin receptor type 1 (CHEMBL1075232)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 9.93 9.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1272307 SB-649868 2.0 1 9.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1272307 SB-649868 Ki = 0.1175 nM 9.93