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Assay Detail

CHEMBL3588151

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

Binding
Displacement of (S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-((3H)-1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2 receptor expressed in CHO cell membranes after 3 hrs by scintillation counting analysis
2
Total Activities
2
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

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 2 8.45 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3338866 MK-1064 1.0 1 9.30
CHEMBL3586412 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3338866 MK-1064 Ki = 0.5 nM 9.30
CHEMBL3586412 Ki = 25.0 nM 7.60