Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3240641

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

Binding
Binding affinity to human OX1 receptor in cell membrane by in vitro radioligand binding assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Orexin/Hypocretin receptor type 1 (CHEMBL5113)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of carbon-linked analogs of dual orexin receptor antagonist filorexant.
Kuduk SD, Skudlarek JW, Di Marco CN, Bruno JG, Pausch MA, O'Brien JA, Cabalu TD, Stevens J, Brunner J, Tannenbaum PL, Gotter AL, Winrow CJ, Renger JJ, Coleman PJ.
Bioorg Med Chem Lett (2014) 24 : 1784 -1789
PubMed 24630562 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.42 9.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3235265 1 9.25
CHEMBL3235249 1 9.00
CHEMBL3235253 1 8.96
CHEMBL3235251 1 7.77
CHEMBL3235260 1 7.75
CHEMBL3235257 1 7.62
CHEMBL3235256 1 7.58
CHEMBL3235254 1 7.57
CHEMBL3235261 1 7.12
CHEMBL3235264 1 7.12
CHEMBL3235255 1 6.97
CHEMBL3235263 1 6.97
CHEMBL3235252 1 6.87
CHEMBL3235259 1 6.68
CHEMBL3235262 1 6.47
CHEMBL3235250 1 6.33
CHEMBL3235258 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3235265 Ki = 0.56 nM 9.25
CHEMBL3235249 Ki = 1.0 nM 9.00
CHEMBL3235253 Ki = 1.1 nM 8.96
CHEMBL3235251 Ki = 17.0 nM 7.77
CHEMBL3235260 Ki = 18.0 nM 7.75
CHEMBL3235257 Ki = 24.0 nM 7.62
CHEMBL3235256 Ki = 26.0 nM 7.58
CHEMBL3235254 Ki = 27.0 nM 7.57
CHEMBL3235261 Ki = 76.0 nM 7.12
CHEMBL3235264 Ki = 75.0 nM 7.12
CHEMBL3235255 Ki = 107.0 nM 6.97
CHEMBL3235263 Ki = 108.0 nM 6.97
CHEMBL3235252 Ki = 135.0 nM 6.87
CHEMBL3235259 Ki = 211.0 nM 6.68
CHEMBL3235262 Ki = 339.0 nM 6.47
CHEMBL3235250 Ki = 470.0 nM 6.33
CHEMBL3235258 Ki = 866.0 nM 6.06