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Binding assay NK-1 from US Patent US20240199618: "NOVEL N-ACYL-[3-SUBSTITUTED]-[8-SUBSTITUTED]-5,6-DIHYDRO-[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:42 Tested
SummaryRelated BioAssays by DepositorRelated BioAssays by Target
Binding Competition Assay with Human NK-3 Receptor from US Patent US20240199618: "NOVEL N-ACYL-[3-SUBSTITUTED]-[8-SUBSTITUTED]-5,6-DIHYDRO-[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:45 Active, 45 Activity ≤ 1 µM, 45 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Cross screening panel
Assay data:1 Tested
SummaryRelated BioAssays by Target
Tachykinin NK1 Eurofins Panlabs panel
Binding affinity towards human TACR1 in an in vitro assay with cellular components measured by membrane filtration
Assay data:19 Active, 4 Activity ≤ 1 µM, 218 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of tachykinin NK1 receptor (unknown origin) upto 10000 nM
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of [3H]SP binding to human neurokinin receptor 1 expressed in CHO cells
Assay data:5 Active, 5 Activity ≤ 1 µM, 5 Tested
Binding affinity to human neurokinin receptor 1 expressed in CHO cells
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of [125I]BHSP binding to neurokinin receptor 1 in rat brain synaptosomes
Assay data:5 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 5 Tested
Displacement of [125I]-labeled SP from human NK-1 receptor expressed in CHO cells at 1 uM relative to control
Assay data:2 Tested
Displacement of [125I]-labeled SP from human NK-1 receptor expressed in CHO cells
Assay data:10 Active, 5 Activity ≤ 1 nM, 10 Activity ≤ 1 µM, 10 Tested
Antagonist activity at human neurokinin receptor 1 assessed as inhibition of 125I-substance P binding to receptor by radioligand binding assay
Assay data:2 Active, 2 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
Human NK-1 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:44 Tested
Binding Competition Assay with Human NK-3 Receptor 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:47 Active, 47 Activity ≤ 1 µM, 47 Tested
Selectivity interaction (CEREP Wide Ligand screening panel (ion channels, receptors, enzymes)) EUB0000304b TACR1
Binding affinity at human NK1R assessed as inhibition constant
Inhibition of human tachykinin NK1 receptor at 10 uM by radioligand binding assay
Tachykinin NK3 Eurofins-Panlabs radioligand binding assay
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