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Assay Detail

CHEMBL1175135

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Binding
Binding affinity to OX2R
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat.
Coleman PJ, Schreier JD, Roecker AJ, Mercer SP, McGaughey GB, Cox CD, Hartman GD, Harrell CM, Reiss DR, Doran SM, Garson SL, Anderson WB, Tang C, Prueksaritanont T, Winrow CJ, Renger JJ.
Bioorg Med Chem Lett (2010) 20 : 4201 -4205
PubMed 20610153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.23 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1171594 2 9.40
CHEMBL469146 1 9.22
CHEMBL1172520 1 9.22
CHEMBL1170803 1 9.10
CHEMBL1170178 1 8.66
CHEMBL1172519 1 8.54
CHEMBL1170179 1 7.85
CHEMBL1171595 1 7.21
CHEMBL1171766 1 6.98
CHEMBL1171767 1 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1171594 Ki = 0.4 nM 9.40
CHEMBL469146 Ki = 0.6 nM 9.22
CHEMBL1172520 Ki = 0.6 nM 9.22
CHEMBL1170803 Ki = 0.8 nM 9.10
CHEMBL1170178 Ki = 2.2 nM 8.66
CHEMBL1172519 Ki = 2.9 nM 8.54
CHEMBL1171594 Ki = 6.7 nM 8.17
CHEMBL1170179 Ki = 14.0 nM 7.85
CHEMBL1171595 Ki = 62.0 nM 7.21
CHEMBL1171766 Ki = 105.0 nM 6.98
CHEMBL1171767 Ki = 590.0 nM 6.23