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Binding affinity to N-terminal biotinylated AviTag-G4SG4S-tagged recombinant SHP2 (1 to 525 residues) (unknown origin) assessed as residence time by SPR analysis
Assay data:2 Tested
SummaryRelated BioAssays by Target
Binding affinity to N-terminal biotinylated AviTag-G4SG4S-tagged recombinant SHP2 (1 to 525 residues) (unknown origin) assessed as off-rate constant by SPR analysis
Allosteric inhibition of IRS1 peptide-activated human recombinant SHP2 (Met1 to Leu525) expressed in Escherichia coli assessed as inhibition of dephosphorylation of 6,8-difluoro-4-methylumbelliferyl phosphate using DiFMUP as substrate preincubated with enzyme for 30 mins followed by substrate addition and measured after 30 mins by DiFMUP assay
Assay data:20 Active, 18 Activity ≤ 1 µM, 23 Tested
Determination of Allosteric Inhibition Activities of the Compounds of the Present Invention on SHP2 from US Patent US20230348467: "Heteroaryl Derivative, Preparation Method Therefor, And Use Thereof"
Assay data:23 Active, 2 Activity ≤ 1 nM, 23 Activity ≤ 1 µM, 23 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
SHP2 Biochemical Assay (with IRSI_2pY) from US Patent US11702392: "Pyrimidinone derivatives as SHP2 antagonists"
Assay data:7 Active, 2 Activity ≤ 1 nM, 7 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
In-Vitro Safety Profile-Testing the Selectivity Over hErg from US Patent US11702392: "Pyrimidinone derivatives as SHP2 antagonists"
Assay data:5 Active, 2 Activity ≤ 1 µM, 7 Tested
SHP2 Biochemical Assay from US Patent US11702392: "Pyrimidinone derivatives as SHP2 antagonists"
Assay data:104 Active, 4 Activity ≤ 1 nM, 58 Activity ≤ 1 µM, 142 Tested
Inhibition of SHP2 in human KYSE-70 cells assessed as decrease in p-AKT level at 0.3 to 30 uM and measured by western blot analysis
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of SHP2 in human HeLa cells assessed as decrease in p-AKT level at 0.3 to 30 uM and measured by western blot analysis
Non-competitive inhibition of wild-type human SHP2 (1 to 535 residues) using DiFMUP as substrate assessed as Km at 0.2 uM measured by Lineweaver-Burk plot analysis
Non-competitive inhibition of wild-type human SHP2 (1 to 535 residues) using DiFMUP as substrate assessed as Km at 0.08 uM measured by Lineweaver-Burk plot analysis
Non-competitive inhibition of wild-type human SHP2 (1 to 535 residues) using DiFMUP as substrate assessed as Km at 0.032 uM measured by Lineweaver-Burk plot analysis
Non-competitive inhibition of wild-type human SHP2 (1 to 535 residues) using DiFMUP as substrate assessed as Vmax at 0.2 uM measured by Lineweaver-Burk plot analysis
Non-competitive inhibition of wild-type human SHP2 (1 to 535 residues) using DiFMUP as substrate assessed as Vmax at 0.08 uM measured by Lineweaver-Burk plot analysis
Non-competitive inhibition of wild-type human SHP2 (1 to 535 residues) using DiFMUP as substrate assessed as Vmax at 0.032 uM measured by Lineweaver-Burk plot analysis
Inhibition of wild-type PTP1B (2 to 435 residues) (unknown origin) using DiFMUP as substrate and measured by biochemical assay
Inhibition of wild-type SHP1 (2 to 595 residues) (unknown origin) using DiFMUP as substrate and measured by biochemical assay
Reversible inhibition of wild-type human SHP2 using DiFMUP as substrate and measured by jump dilution assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Allosteric inhibition of recombinant human SHP2 assessed as change in melting temperature by SYPRO orange dye based thermal shift assay
Assay data:49 Tested
Allosteric inhibition of recombinant human SHP2 PTP domain (237 to 535 residues) using DiFMUP as substrate preincubated for 30 mins and followed by substrate addition and measured by microplate reader method
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