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Assay Detail

CHEMBL3240643

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Functional
Antagonist activity at human OX1 receptor assessed as Ca2+ flux by FLIPR assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
IC50 17 6.89 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3235265 1 8.20
CHEMBL3235249 1 7.80
CHEMBL3235253 1 7.51
CHEMBL3235260 1 7.23
CHEMBL3235255 1 7.08
CHEMBL3235254 1 7.00
CHEMBL3235251 1 6.85
CHEMBL3235264 1 6.53
CHEMBL3235252 1 6.15
CHEMBL3235250 1 6.07
CHEMBL3235258 1 5.41
CHEMBL3235259 1 -
CHEMBL3235261 1 -
CHEMBL3235262 1 -
CHEMBL3235263 1 -
CHEMBL3235257 1 -
CHEMBL3235256 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3235265 IC50 = 6.3 nM 8.20
CHEMBL3235249 IC50 = 16.0 nM 7.80
CHEMBL3235253 IC50 = 31.0 nM 7.51
CHEMBL3235260 IC50 = 59.0 nM 7.23
CHEMBL3235255 IC50 = 83.0 nM 7.08
CHEMBL3235254 IC50 = 100.0 nM 7.00
CHEMBL3235251 IC50 = 140.0 nM 6.85
CHEMBL3235264 IC50 = 298.0 nM 6.53
CHEMBL3235252 IC50 = 706.0 nM 6.15
CHEMBL3235250 IC50 = 861.0 nM 6.07
CHEMBL3235258 IC50 = 3878.0 nM 5.41
CHEMBL3235259 IC50 - -
CHEMBL3235261 IC50 - -
CHEMBL3235262 IC50 - -
CHEMBL3235263 IC50 - -
CHEMBL3235257 IC50 - -
CHEMBL3235256 IC50 - -