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Antagonist activity at OX1R (unknown origin) expressed in CHO cells at 10 uM in presence of orexin A by cell based calcium assay
Assay data:6 Tested
SummaryPubMed CitationRelated BioAssays by Target
Biological Assay from US Patent US8653263: "Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators"
Assay data:353 Active, 293 Activity ≤ 1 µM, 377 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
FLIPR Ca2+ Flux Assay from US Patent US10010539: "Pyrazole, triazole and tetrazole orexin receptor antagonists"
Assay data:108 Active, 105 Activity ≤ 1 µM, 108 Tested
Displacement of [3H]-SB67404 from human orexin 1 receptor expressed in CHO cells incubated for 2 hrs by whole cell radioligand binding assay
Assay data:13 Active, 3 Activity ≤ 1 µM, 124 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Antagonist activity at human OX1 receptor expressed in CHO cell membranes assessed as inhibition of orexin A-induced Ca2+ elevation after 30 mins in presence of orexin A by FLIPR calcium 4 assay
Assay data:2 Active, 7 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Antagonist activity at human OX1R expressed in CHOK1 cells assessed as inhibition of orexin A-induced intracellular Ca2+ release preincubated for 15 mins followed by orexin A addition by Fura 2-AM dye based fluorescence assay based by Cheng-Prusoff equation analysis
Assay data:3 Active, 8 Activity ≤ 1 µM, 8 Tested
Agonist activity at human OX1 receptor expressed in CHOK1 cells assessed as increase in calcium accumulation at 10 uM incubated for 30 mins measured for 150 secs in presence of OX1R antagonist SB-334867 by calcium-4 dye based FLIPR assay
Assay data:2 Tested
Binding affinity to OX1R
Assay data:10 Active, 4 Activity ≤ 1 nM, 10 Activity ≤ 1 µM, 10 Tested
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