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Assay Detail

CHEMBL3588597

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

Binding
Binding affinity to human OX2R expressed in HEK-293 cells assessed as inhibition of orexin A-induced calcium accumulation by FLIPR assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of (1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist.
Yoshida Y, Naoe Y, Terauchi T, Ozaki F, Doko T, Takemura A, Tanaka T, Sorimachi K, Beuckmann CT, Suzuki M, Ueno T, Ozaki S, Yonaga M.
J Med Chem (2015) 58 : 4648 -4664
PubMed 25953512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 9.36 9.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545367 LEMBOREXANT 4.0 1 9.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545367 LEMBOREXANT Ki = 0.44 nM 9.36