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Assay Detail

CHEMBL5149864

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

Functional
Agonist activity at human OX2R expressed in CHO cells incubated for 2 hrs by IP-one detection reagent based fluorescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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 3-Aminopyrrolidine and Piperidine Macrocyclic Orexin Receptor Agonists for Treating Sleep Disorders.
Sabnis RW.
ACS Med Chem Lett (2022) 13 : 1390 -1391
PubMed 36105324 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 10.15 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5196538 1 10.40
CHEMBL5194793 1 10.30
CHEMBL5177846 1 10.15
CHEMBL5195414 1 10.05
CHEMBL5190821 1 10.00
CHEMBL5206338 1 10.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5196538 IC50 = 0.04 nM 10.40
CHEMBL5194793 IC50 = 0.05 nM 10.30
CHEMBL5177846 IC50 = 0.07 nM 10.15
CHEMBL5195414 IC50 = 0.09 nM 10.05
CHEMBL5190821 IC50 = 0.1 nM 10.00
CHEMBL5206338 IC50 = 0.1 nM 10.00