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Assay Detail

CHEMBL758902

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

Binding
Inhibitory concentration against human orexin-1 receptor (hOX1R)
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist.
Hirose M, Egashira S, Goto Y, Hashihayata T, Ohtake N, Iwaasa H, Hata M, Fukami T, Kanatani A, Yamada K.
Bioorg Med Chem Lett (2003) 13 : 4497 -4499
PubMed 14643355 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 5.42 5.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL344622 1 5.95
CHEMBL140700 1 5.64
CHEMBL140547 1 5.44
CHEMBL343786 1 5.43
CHEMBL140348 1 5.42
CHEMBL343551 1 5.28
CHEMBL139083 1 5.26
CHEMBL138091 1 5.23
CHEMBL138101 1 5.16
CHEMBL342583 1 -
CHEMBL337367 1 -
CHEMBL140559 1 -
CHEMBL139158 1 -
CHEMBL141368 1 -
CHEMBL140260 1 -
CHEMBL342039 1 -
CHEMBL139634 1 -
CHEMBL142009 1 -
CHEMBL140504 1 -
CHEMBL337159 1 -
CHEMBL435826 1 -
CHEMBL343141 1 -
CHEMBL139915 1 -
CHEMBL444602 1 -
CHEMBL139117 1 -
CHEMBL139157 1 -
CHEMBL342363 1 -
CHEMBL138717 1 -
CHEMBL139223 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL344622 IC50 = 1130.0 nM 5.95
CHEMBL140700 IC50 = 2300.0 nM 5.64
CHEMBL140547 IC50 = 3600.0 nM 5.44
CHEMBL343786 IC50 = 3670.0 nM 5.43
CHEMBL140348 IC50 = 3850.0 nM 5.42
CHEMBL343551 IC50 = 5300.0 nM 5.28
CHEMBL139083 IC50 = 5500.0 nM 5.26
CHEMBL138091 IC50 = 5900.0 nM 5.23
CHEMBL138101 IC50 = 7000.0 nM 5.16
CHEMBL342583 IC50 > 10000.0 nM -
CHEMBL337367 IC50 > 10000.0 nM -
CHEMBL140559 IC50 > 10000.0 nM -
CHEMBL139158 IC50 > 10000.0 nM -
CHEMBL141368 IC50 > 10000.0 nM -
CHEMBL140260 IC50 > 10000.0 nM -
CHEMBL342039 IC50 > 10000.0 nM -
CHEMBL139634 IC50 > 10000.0 nM -
CHEMBL142009 IC50 > 10000.0 nM -
CHEMBL140504 IC50 > 10000.0 nM -
CHEMBL337159 IC50 > 10000.0 nM -
CHEMBL435826 IC50 > 10000.0 nM -
CHEMBL343141 IC50 > 10000.0 nM -
CHEMBL139915 IC50 > 10000.0 nM -
CHEMBL444602 IC50 > 10000.0 nM -
CHEMBL139117 IC50 > 10000.0 nM -
CHEMBL139157 IC50 > 10000.0 nM -
CHEMBL342363 IC50 > 10000.0 nM -
CHEMBL138717 IC50 > 10000.0 nM -
CHEMBL139223 IC50 > 10000.0 nM -