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SYK Inhibition from US Patent US20230295171: "FUSED HETEROAROMATIC PYRROLIDINONES"
Assay data:124 Active, 5 Activity ≤ 1 nM, 106 Activity ≤ 1 µM, 128 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
High Throughput Syk Biochemical Assay from US Patent US11517570: "Crystalline succinate salt of 6-(6-aminopyrazin-2-yl)-n-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine"
Assay data:11 Active, 11 Activity ≤ 1 µM, 11 Tested
Selectivity interaction (ScanMAX (DiscoverX, competition-binding assay)) EUB0000232b SYK
Assay data:1 Tested
SummaryRelated BioAssays by Target
Selectivity interaction (ScanMAX (DiscoverX)) EUB0000232b SYK
Selectivity interaction (KinomeScan (DiscoverX)) EUB0000702a SYK
Selectivity interaction (KinomeScan (DiscoverX)) EUB0000305b SYK
Selectivity interaction (Kinase panel (enzymatic assay)) EUB0000153b SYK
Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000714a SYK
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000704a SYK
Assay data:1 Active, 1 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
Affinity On-target Cellular interaction (Cellular human mast cell degranulation assay) EUB0000714a SYK
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Affinity Phenotypic Cellular interaction (Cellular human mast cell degranulation assay) EUB0000714a SYK
Affinity Phenotypic Cellular interaction (Cellular human mast cell degranulation assay) EUB0000704a SYK
Inhibition of SYK (unknown origin) at 50 nM by Z'LYTE screening method relative to control
Assay data:12 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of recombinant full-length human Syk at 1 uM assessed as residual activity at 1 uM using poly(Glu, Tyr) 4:1 as substrate measured after 40 mins in presence of [gamma33P]ATP by radiometric scintillation counting method relative to control
Inhibition of human SYK assessed as residual activity at 30 uM relative to control
Competitive inhibition of SYK (unknown origin) assessed as inhibition constant in the presence of ATP at Km concentration
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of SYK (unknown origin)
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of human full length recombinant N-terminal GST-tagged SYK expressed in baculovirus expression system at 250 nM by Z'-lyte assay
Inhibition of SYK (unknown origin) assessed as reduction of IgM-stimulated ERK phosphorylation by Cell-based assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Inhibition of SYK (unknown origin) at 1 uM
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