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Assay Detail

CHEMBL1007898

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Functional
Antagonist activity at human OX2 receptor
29
Total Activities
29
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Biomedical application of orexin/hypocretin receptor ligands in neuroscience.
Boss C, Brisbare-Roch C, Jenck F.
J Med Chem (2009) 52 : 891 -903
PubMed 19199652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.74 7.60
Ki 2 7.94 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL403259 1 9.00
CHEMBL344622 1 7.60
CHEMBL489893 1 7.55
CHEMBL140700 1 7.52
CHEMBL343786 1 7.46
CHEMBL489097 1 7.44
CHEMBL142009 1 7.40
CHEMBL139083 1 7.25
CHEMBL444602 1 7.23
CHEMBL138091 1 7.16
CHEMBL140348 1 6.89
CHEMBL255845 1 6.88
CHEMBL337367 1 6.71
CHEMBL139634 1 6.62
CHEMBL140260 1 6.40
CHEMBL140559 1 6.05
CHEMBL139915 1 6.04
CHEMBL337159 1 5.85
CHEMBL138101 1 5.70
CHEMBL139117 1 5.68
CHEMBL342583 1 5.54
CHEMBL141368 1 -
CHEMBL342363 1 -
CHEMBL435826 1 -
CHEMBL139223 1 -
CHEMBL343141 1 -
CHEMBL342039 1 -
CHEMBL138717 1 -
CHEMBL140504 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL403259 Ki = 1.0 nM 9.00
CHEMBL344622 IC50 = 25.0 nM 7.60
CHEMBL489893 IC50 = 28.0 nM 7.55
CHEMBL140700 IC50 = 30.0 nM 7.52
CHEMBL343786 IC50 = 35.0 nM 7.46
CHEMBL489097 IC50 = 36.0 nM 7.44
CHEMBL142009 IC50 = 40.0 nM 7.40
CHEMBL139083 IC50 = 56.0 nM 7.25
CHEMBL444602 IC50 = 59.0 nM 7.23
CHEMBL138091 IC50 = 70.0 nM 7.16
CHEMBL140348 IC50 = 130.0 nM 6.89
CHEMBL255845 Ki = 131.0 nM 6.88
CHEMBL337367 IC50 = 195.0 nM 6.71
CHEMBL139634 IC50 = 240.0 nM 6.62
CHEMBL140260 IC50 = 395.0 nM 6.40
CHEMBL140559 IC50 = 900.0 nM 6.05
CHEMBL139915 IC50 = 910.0 nM 6.04
CHEMBL337159 IC50 = 1400.0 nM 5.85
CHEMBL138101 IC50 = 2000.0 nM 5.70
CHEMBL139117 IC50 = 2100.0 nM 5.68
CHEMBL342583 IC50 = 2900.0 nM 5.54
CHEMBL141368 IC50 > 10000.0 nM -
CHEMBL342363 IC50 > 10000.0 nM -
CHEMBL435826 IC50 > 10000.0 nM -
CHEMBL139223 IC50 > 10000.0 nM -
CHEMBL343141 IC50 > 10000.0 nM -
CHEMBL342039 IC50 > 10000.0 nM -
CHEMBL138717 IC50 > 10000.0 nM -
CHEMBL140504 IC50 > 10000.0 nM -