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Assay Detail

CHEMBL3588236

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

Binding
Displacement of [125I]-orexin A from OX2 receptor (unknown origin) expressed in CHOK1 cells after 90 to 120 mins by scintillation counting analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate.
Letavic MA, Bonaventure P, Carruthers NI, Dugovic C, Koudriakova T, Lord B, Lovenberg TW, Ly KS, Mani NS, Nepomuceno D, Pippel DJ, Rizzolio M, Shelton JE, Shah CR, Shireman BT, Young LK, Yun S.
J Med Chem (2015) 58 : 5620 -5636
PubMed 26087021 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 8.30 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL359632 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL359632 Ki = 5.012 nM 8.30