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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
Inhibition of tachykinin NK1 receptor (unknown origin) upto 10000 nM
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
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
SummaryRelated BioAssays by DepositorRelated BioAssays by Target
Selectivity interaction (CEREP Wide Ligand screening panel (ion channels, receptors, enzymes)) EUB0000304b TACR1
Binding affinity at human NK1R assessed as inhibition constant
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of human tachykinin NK1 receptor at 10 uM by radioligand binding assay
SummaryPubMed CitationRelated BioAssays by Target
NK1/HU Eurofins SafetyScreen44 (BI)
Inhibition of tachykinin NK1 receptor (unknown origin)
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Displacement of [125I]SP from human NK1R expressed in U373 MG cells assessed as inhibitory constant incubated for 30 mins by radioligand binding assay
Displacement of [125I]SP from human NK1R expressed in U373 MG cells incubated for 30 mins by radioligand binding assay
Antagonist activity at NK1R (unknown origin) assessed as decreased IP1 levels in presence of endogenous SP ligand preincubated for 10 mins followed by 30 min incubation with antagonist and SP by HTRF-FRET assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 4 Tested
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