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Assay Detail

CHEMBL5360018

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

Functional
Antagonist activity at human OX2R expressed in CHO/dhfr- cells assessed as inhibition of orexin B-induced intracellular Ca2+ mobilization preincubated for 25 mins followed by orexin B addition by FLIPR assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO/dhfr-
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Pyrazole derivatives as selective orexin-2 receptor antagonists (2-SORA): synthesis, structure-activity-relationship, and sleep-promoting properties in rats.
Brotschi C, Bolli MH, Gatfield J, Roch C, Sifferlen T, Treiber A, Williams JT, Boss C.
RSC Med Chem (2024) 15 : 344 -354
PubMed 38283232 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.10 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2385132 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2385132 IC50 = 8.0 nM 8.10