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Binding affinity towards human TACR2 in an in vitro assay with cellular components measured by membrane filtration
Assay data:79 Tested
SummaryRelated BioAssays by Target
Human NK-2 Binding Assay from US Patent US11731974: "N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists"
Assay data:1 Active, 44 Tested
SummaryCompounds, ActiveRelated BioAssays by DepositorRelated BioAssays by Target
Selectivity interaction (CEREP panel (GPCRS, ion channels, transporters)) EUB0000193b TACR2
Assay data:1 Active, 1 Tested
Assay data:1 Tested
Selectivity interaction (CEREP panel (ligand receptors, ion channels, transporters)) EUB0000330a TACR2
NK2 (h) CEREP ligand profiling
NK2 (h) CEREP panel
Inhibition of Neurokinin NK2 receptor (unknown origin) at 10 uM relative to control
SummaryPubMed CitationRelated BioAssays by Target
Displacement of [125I]NKA from human recombinant NK2 receptor at 10 uM after 60 mins by scintillation counting analysis relative to control
Displacement of [125I]NKA from human recombinant NK2 receptor after 60 mins by scintillation counting analysis
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
NK-1, NK-2 and NK-3 Calcium Flux FLIPR assays from US Patent US11149006: "Compounds as neurokinin-1 receptor antagonists and uses thereof"
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Binding Competition Assay from US Patent US10941151: "Chiral N-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof"
Assay data:2 Active, 7 Tested
Human NK-2 assay from US Patent US10836768: "N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists"
Binding Assay from US Patent US10683295: "Chiral N-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-A]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof"
Binding Assay from US Patent US9475814: "Chiral N-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof"
Binding Assay from US Patent US9422299: "Substituted [1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists"
Assay data:1 Active, 43 Tested
Binding Assay from US Patent US8592454: "Nitrogen-containing heterocyclic compound and use of same"
Assay data:12 Active, 11 Activity ≤ 1 nM, 12 Activity ≤ 1 µM, 12 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Human NK2 Receptor Binding Assay from US Patent US8470816: "Nitrogen-containing heterocyclic compound and use thereof"
Assay data:20 Active, 15 Activity ≤ 1 nM, 20 Activity ≤ 1 µM, 20 Tested
Inhibition Assay from US Patent US9987274: "N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists"
Radioligand Binding Assay from US Patent US9969738: "N-acyl-(3-substituted)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor-mediated disorders"
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
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