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Assay Detail

CHEMBL1109768

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

Functional
Antagonist activity at OX2 receptor assessed as inhibition of calcium flux by FLIPR assay
8
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as potent orexin receptor antagonists.
Coleman PJ, Schreier JD, McGaughey GB, Bogusky MJ, Cox CD, Hartman GD, Ball RG, Harrell CM, Reiss DR, Prueksaritanont T, Winrow CJ, Renger JJ.
Bioorg Med Chem Lett (2010) 20 : 2311 -2315
PubMed 20207138 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.76 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL469146 1 7.57
CHEMBL1089406 1 7.57
CHEMBL1091110 3 7.36
CHEMBL1091111 1 6.96
CHEMBL1093724 1 5.43
CHEMBL1091112 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL469146 IC50 = 27.0 nM 7.57
CHEMBL1089406 IC50 = 27.0 nM 7.57
CHEMBL1091110 IC50 = 44.0 nM 7.36
CHEMBL1091110 IC50 = 65.0 nM 7.19
CHEMBL1091111 IC50 = 110.0 nM 6.96
CHEMBL1093724 IC50 = 3700.0 nM 5.43
CHEMBL1091110 IC50 = 6200.0 nM 5.21
CHEMBL1091112 IC50 > 10000.0 nM -