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Selectivity interaction (GPCR panel (PDSP screen)) EUB0000719a GABRA1
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Affinity Biochemical interaction (TR-FRET binding assay (Invitrogen)) EUB0000719a RIPK1
Affinity Phenotypic Cellular interaction (CytoTox 96 nonradioactive cytotoxicity assay (necroptosis in HT29 cells; Promega)) EUB0000719a RIPK1
TR-FRET (mouse RIPK1)
Assay data:2 Active, 1 Activity ≤ 1 µM, 3 Tested
HT29 necroptosis assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µM
TR-FRET (human RIPK1)
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 3 Tested
Induction of necroptosis in human HT-29 cells assessed as increase in TNFalpha/AT-406/zVAD-FMK-induced LDH release preincubated with cells followed by TNFalpha/AT-406/zVAD-FMK addition measured after 16 to 20 hrs by CytoTox 96 nonradioactive cytotoxicity assay
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Inhibition of fluorescent-labeled 3-(3-((3-(4-amino-5-(4-(3-(2-fluoro-5-(trifluoromethyl)phenyl)ureido)-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)propyl)amino)-3-oxopropyl)-5,5-difluoro-7,9-dimethyl-5H-dipyrrolo[1,2-c:2',1'-f]-[1,3,2]diazaborinin-4-ium-5-uide binding to human N-terminal GST/His-tagged RIPK1 (1 to 375 residues) expressed in baculovirus expression system by TR-FRET assay
Assay data:27 Active, 5 Activity ≤ 1 nM, 25 Activity ≤ 1 µM, 27 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
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