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LC-MS/MS-Based NSD2 Enzymatic Assay from US Patent US11420970: "Piperidinyl-methyl-purineamines as NSD2 inhibitors and anti-cancer agents"
Assay data:297 Active, 316 Activity ≤ 1 µM, 316 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
HMT Assay from Article 10.1038/nchembio.2304: "An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED."
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Binding affinity to biotinylated human NSD2 PWWP1 domain (208 to 368 residues) expressed in Escherichia coli BL2I (DE3) cells assessed as dissociation constant by surface plasmon resonance analysis
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to N-terminal GST-tagged human NSD2 PWWP1 domain (208 to 369 residues) expressed in Escherichia coli BL2I (DE3) cells assessed as dissociation constant by isothermal titration calorimetry assay
Assay data:3 Active, 2 Activity ≤ 1 µM, 3 Tested
Binding affinity to N-terminal His6/Sumo-tagged NSD2 PWWP1 domain (211 to 350 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) using ATKAARKSAPATGGV-Lys (me)2-KPHRYRPG polypeptide as substrate incubated for 3 hrs by HTRF assay
Assay data:24 Active, 8 Activity ≤ 1 µM, 38 Tested
Inhibition of NSD2 (unknown origin)
Assay data:2 Active, 1 Activity ≤ 1 µM, 4 Tested
Primary qHTS for inhibitors of nuclear receptor binding SET domain protein 2 (NSD2) in an RCH-ACV wild type WT cells (2C)
Assay data:2970 Active, 9 Activity ≤ 1 nM, 1016 Activity ≤ 1 µM, 10037 Tested
Primary qHTS for inhibitors of nuclear receptor binding SET domain protein 2 (NSD2) in an isogenic RCH-ACV NSD2 p.E1099K mutant (9B)
Assay data:2826 Active, 4 Activity ≤ 1 nM, 946 Activity ≤ 1 µM, 10037 Tested
Development of Small Molecule Probes of the Histone Methyltransferase, NSD2 Measured in Biochemical System Using Plate Reader - 7053-01_Inhibitor_Dose_CherryPick_Activity
Assay data:390 Active, 36 Activity ≤ 1 µM, 1503 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Same ProjectRelated BioAssays by Target
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