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IP-One assay kit from US Patent US11680060: "Bicycloheptane pyrrolidine orexin receptor agonists"
Assay data:138 Active, 21 Activity ≤ 1 nM, 134 Activity ≤ 1 µM, 138 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Human Orexin 1 Receptor Radioligand Binding Studies from US Patent US11667644: "Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators"
Assay data:235 Active, 111 Activity ≤ 1 µM, 353 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Human Orexin 2 Receptor Radioligand Binding Studies from US Patent US11667644: "Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators"
Assay data:353 Active, 290 Activity ≤ 1 µM, 378 Tested
Scintillation Proximity Assay (SPA) Binding Assay from US Patent US11660293: "Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists"
Assay data:129 Active, 3 Activity ≤ 1 nM, 129 Activity ≤ 1 µM, 129 Tested
Agonist activity at human OX2R expressed in CHO cells incubated for 2 hrs by IP-one detection reagent based fluorescence assay
Assay data:6 Active, 6 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at OX2R (unknown origin) assessed as maximum efficacy at 10 uM relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at OX2R (unknown origin) assessed as maximum efficacy relative to control
Assay data:24 Tested
Agonist activity at OX2R (unknown origin)
Assay data:27 Active, 1 Activity ≤ 1 nM, 25 Activity ≤ 1 µM, 30 Tested
Agonist activity at OX1R (unknown origin) assessed as maximum efficacy at 10 uM relative to control
Assay data:3 Tested
Agonist activity at OX1R (unknown origin) assessed as maximum efficacy relative to control
Assay data:20 Tested
Agonist activity at OX1R (unknown origin)
Assay data:23 Active, 15 Activity ≤ 1 µM, 30 Tested
Antagonist activity at OX2R (unknown origin) by cell-based calcium assay
Assay data:1 Active, 6 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Antagonist activity at OX1R (unknown origin) by cell-based calcium assay
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
Antagonist activity at human OX1R expressed in CHO-K1 cells assessed as inhibition of orexin-A-induced increase in calcium mobilization preincubated for 15 mins followed orexin-A stimulation by by Fura-2-AM dye based fluorescence assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Agonist activity at human OX2R expressed in CHO-K1 cells assessed as increase in calcium mobilization by Fluo-4-AM dye based fluorescence assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Agonist activity at OX2R (unknown origin) expressed in CHO cells by cell-based calcium assay relative to orexin A
Assay data:8 Tested
Agonist activity at OX1R (unknown origin) expressed in CHO cells by cell-based calcium assay relative to orexin A
Agonist activity at OX2R (unknown origin) expressed in CHO cells by cell-based calcium assay
Assay data:7 Active, 6 Activity ≤ 1 µM, 10 Tested
Agonist activity at OX1R (unknown origin) expressed in CHO cells by cell-based calcium assay
Assay data:5 Active, 5 Activity ≤ 1 µM, 10 Tested
Agonist activity at OX2R (unknown origin) expressed in CHO cells at 10 uM by cell-based calcium assay relative to orexin A
Assay data:2 Tested
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