| Assay ID | Title | Year | Journal | Article |
|---|
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
| Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors. |
| AID721523 | Inhibition of human PHD2 catalytic domain (181 to 426) Mn2 expressed in Escherichia coli by NMR spectroscopic analysis | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
| Reporter ligand NMR screening method for 2-oxoglutarate oxygenase inhibitors. |
| AID770449 | Growth inhibition of human KYSE-150 cells after 48 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity. |
| AID770460 | Inhibition of KDM7B (unknown origin) using H3K4me3K9me2 and 2-oxoglutarate as substrate after 1 hr by matrix-assisted laser desorption ionization time of flight mass spectrometry | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity. |
| AID1249054 | Inhibition of KDM4E (unknown origin) | 2014 | MedChemComm, Dec-01, Volume: 5, Issue:12
| Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor. |
| AID721525 | Binding affinity to human PHD2 catalytic domain (181 to 426) Mn2 expressed in Escherichia coli by NMR spectroscopic analysis | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
| Reporter ligand NMR screening method for 2-oxoglutarate oxygenase inhibitors. |
| AID323624 | Inhibition of Aeromonas hydrophila beta lactamase CphA at pH 10.0 | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila. |
| AID1181282 | Cytotoxicity against human LNCAP cells after 3 days by MTT assay | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| KDM4B as a target for prostate cancer: structural analysis and selective inhibition by a novel inhibitor. |
| AID1810106 | Inhibition of recombinant human MINA53 expressed in Escherichia coli BL21 (DE3) using RPL27A G31RGNAGGLHHHRINFDKYHP49 as substrate preincubated for 15 mins followed by substrate addition and measured after 30 to 60 mins by RapidFire Mass spectrometry assa | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
| First-in-Class Inhibitors of the Ribosomal Oxygenase MINA53. |
| AID499339 | Inhibition of human recombinant PHD2 expressed in Sf9 cells by time-resolved fluorescence assay | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
| Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors. |
| AID1543453 | Inhibition of recombinant human PHD2 using 2OG as substrate and Fe2 as co-factor assessed as hydroxylation incubated for 15 mins in presence of L-ascorbate by LC-MS analysis | 2019 | Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
| Inhibition of a viral prolyl hydroxylase. |
| AID770458 | Inhibition of KDM4A (unknown origin) using H3K9me3 peptide and 2-oxoglutarate as substrate after 1 hr by FDH-coupled assay | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity. |
| AID1282319 | Selectivity ratio of IC50 for FIH (unknown origin) expressed in Escherichia coli to IC50 for KDM4C (1 to 352 residues) (unknown origin) expressed in Escherichia coli | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID1282307 | Competitive inhibition of N-terminal His6-tagged KDM4C (1 to 352 residues) (unknown origin) expressed in Escherichia coli Rosetta 2(DE3)pLysS using 250 uM ARK(Me3)STGGK peptide/50 uM alpha-ketoglutarate as substrate/cofactor by FDH coupling-based Lineweav | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID1677973 | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with high 200 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
| Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase. |
| AID1714493 | Displacement of sodium 5-(3-(8-(3-carboxy-N-hydroxyacrylamido)octyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoate from Naegleria Tet-1 incubated for 20 mins followed by sodium 5-(3-(8-(3-carboxy-N-hydroxyacrylamido)octyl)thioureido)-2-(6-hydroxy | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2
| A Fluorescence Polarization Biophysical Assay for the Naegleria DNA Hydroxylase Tet1. |
| AID1282311 | Inhibition of KDM5A (1 to 797 residues) (unknown origin) expressed in insect sf21 cells using ARTK(Me3)QTARKSTGGKAPRK peptide/ 100 uM alpha-ketoglutarate as substrate/cofactor incubated for 45 mins by MALDI assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID678710 | Inhibition of KDM4C | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
| Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C). |
| AID323615 | Inhibition of Bacillus cereus metallo beta lactamase Bc2 assessed as residual enzyme activity at 100 uM | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila. |
| AID323622 | Inhibition of Aeromonas hydrophila beta lactamase CphA at pH 8.0 | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila. |
| AID323626 | Inhibition of Aeromonas hydrophila beta lactamase CphA by competitive inhibition assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila. |
| AID1181278 | Inhibition of purified recombinant KDM4E (1 to 347 aa) (unknown origin) expressed in Escherichia coli using H3K9me3 peptide as substrate after 30 mins by FDH-coupled assay | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| KDM4B as a target for prostate cancer: structural analysis and selective inhibition by a novel inhibitor. |
| AID1249068 | Inhibition of KDM5C (unknown origin) | 2014 | MedChemComm, Dec-01, Volume: 5, Issue:12
| Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor. |
| AID349747 | Inhibition of human recombinant PHD2 (181-426) expressed in Escherichia coli BL21 (DE3) by TR-FRET assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Application of a proteolysis/mass spectrometry method for investigating the effects of inhibitors on hydroxylase structure. |
| AID323620 | Inhibition of Legionella gormani beta lactamase metallo FEZ1 expressed in Escherichia coli assessed as residual enzyme activity at 100 uM | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila. |
| AID678707 | Inhibition of KDM4C catalytic core-mediated demethylation of ARK(Me)3STGGK after 30 mins by FDH-coupled assay | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
| Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C). |
| AID323623 | Inhibition of Aeromonas hydrophila beta lactamase CphA at pH 9.0 | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila. |
| AID323621 | Inhibition of Aeromonas hydrophila beta lactamase CphA at pH 7.0 | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila. |
| AID1249066 | Inhibition of KDM2A (unknown origin) | 2014 | MedChemComm, Dec-01, Volume: 5, Issue:12
| Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor. |
| AID1282318 | Selectivity ratio of IC50 for KDM5A (unknown origin) expressed in Escherichia coli to IC50 for KDM4C (1 to 352 residues) (unknown origin) expressed in Escherichia coli | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID1282322 | Selectivity ratio of IC50 for KDM5B (unknown origin) expressed in Escherichia coli to IC50 for KDM4C (1 to 352 residues) (unknown origin) expressed in Escherichia coli | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID499337 | Inhibition of recombinant His-tagged JMJD2A expressed in Escherichia coli Rosetta 2 (DE3) pLysS cells by formaldehyde dehydrogenase-coupled assay | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
| Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors. |
| AID1543452 | Inhibition of N-terminal His6-tagged recombinant Paramecium bursaria chlorella virus 1 CPH expressed in Escherichia coli Rosetta 2 (DE3) cells pre-incubated for 5 mins before 2OG as substrate and Fe2 as co-factor addition in presence of L-ascorbate and me | 2019 | Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
| Inhibition of a viral prolyl hydroxylase. |
| AID1530048 | Inhibition of Streptococcus pyogenes SrtA deltaN81 mutant expressed in Escherichia coli BL21(DE3) at 100 uM using Abz-LPETA-Dap(Dnp) as substrate preincubated for 10 mins followed by substrate addition measured every min for 2.5 hrs by fluorimetric assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Identification of potential antivirulence agents by substitution-oriented screening for inhibitors of Streptococcus pyogenes sortase A. |
| AID1282317 | Inhibition of KDM4D (unknown origin) expressed in Escherichia coli using H3 (1 to 21 residues) K9Me3-GGK-Biotin KDM4 Cognate Ligand/10 uM alpha-ketoglutarate as substrate/cofactor preincubated for 5 mins followed by substrate addition measured after 20 mi | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID1282309 | Inhibition of N-terminal His6-tagged KDM4C (1 to 352 residues) (unknown origin) expressed in Escherichia coli Rosetta 2(DE3)pLysS using ARTKQTARK(Me3)STGGKA peptide/100 uM alpha-ketoglutarate as substrate/cofactor incubated for 45 mins by MALDI assay | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID323627 | Inhibition of Aeromonas hydrophila beta lactamase CphA N116H-N220G mutant by competitive inhibition assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila. |
| AID323616 | Inhibition of metallo beta lactamase VIM2 assessed as residual enzyme activity at 100 uM | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila. |
| AID499336 | Inhibition of recombinant His-tagged JMJD2C expressed in Escherichia coli Rosetta 2 (DE3) pLysS cells by formaldehyde dehydrogenase-coupled assay | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
| Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors. |
| AID770450 | Growth inhibition of human HeLa cells after 48 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity. |
| AID1282312 | Inhibition of N-terminal His6-tagged KDM4C (1 to 352 residues) (unknown origin) expressed in Escherichia coli Rosetta 2(DE3)pLysS using biotinylated peptide/ 2 uM alpha-ketoglutarate as substrate/cofactor preincubated for 15 mins followed by substrate add | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID604082 | Inhibition of JMJD2E | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
| Inhibitors of histone demethylases. |
| AID1249069 | Inhibition of KDM6B (unknown origin) | 2014 | MedChemComm, Dec-01, Volume: 5, Issue:12
| Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor. |
| AID1249064 | Inhibition of KDM4C (unknown origin) | 2014 | MedChemComm, Dec-01, Volume: 5, Issue:12
| Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor. |
| AID344921 | Inhibition of human collagene prolyl-4-hydroxylase | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
| AID323619 | Inhibition of Stenotrophomonas maltophilia metallo beta lactamase L1 assessed as residual enzyme activity at 100 uM | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila. |
| AID74835 | Inhibitory activity against vesicular glutamate transport (GVT) in synaptic vesicles isolated from rat forebrain | 1999 | Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17
| Quinoline-2,4-dicarboxylic acids: synthesis and evaluation as inhibitors of the glutamate vesicular transport system. |
| AID344923 | Inhibition of human recombinant HIF PHD1 | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
| AID1876799 | Inhibition of KDM4C (unknown origin) using H3(21-44)-K36(Me3)-GK(Biotin) as substrate at 10 uM incubated for 1 hrs by alpha screen assay | | | |
| AID721519 | Displacement of 2OG from FBXL11 (1 to 517) (unknown origin) expressed in Escherichia coli at 800 uM | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
| Reporter ligand NMR screening method for 2-oxoglutarate oxygenase inhibitors. |
| AID770459 | Inhibition of KDM4C (unknown origin) using H3K9me3 peptide and 2-oxoglutarate as substrate after 1 hr by FDH-coupled assay | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity. |
| AID499340 | Selectivity ratio of IC50 for recombinant His-tagged JMJD2A to IC50 for recombinant His-tagged JMJD2C | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
| Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors. |
| AID344914 | Inhibition of human recombinant PHD2 | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
| AID1282310 | Inhibition of N-terminal His6-tagged full-length FIH (unknown origin) expressed in Escherichia coli Rosetta 2(DE3)pLysS using SMDESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRALDQVN peptide/100 uM alpha-ketoglutarate as substrate/cofactor incubated for 45 mins by MALDI | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID1677972 | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
| Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase. |
| AID770453 | Inhibition of KDM7A (unknown origin) using K27me2 peptide as substrate by MALDI assay | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity. |
| AID1785098 | Inhibition of N-terminal His6-tagged KDM4E (1 to 337 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3)-R3 assessed as Vmax at 1 uM in presence of alpha-KG by Michaelis-Menten analysis (Rvb = 42 /s) | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Enhanced Properties of a Benzimidazole Benzylpyrazole Lysine Demethylase Inhibitor: Mechanism-of-Action, Binding Site Analysis, and Activity in Cellular Models of Prostate Cancer. |
| AID349748 | Destabilizing effect on human recombinant PHD2 (181-426) expressed in Escherichia coli BL21 (DE3) assessed as half life by limited trypsinolysis/MALDI-MS analysis in presence of ferrous ion | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Application of a proteolysis/mass spectrometry method for investigating the effects of inhibitors on hydroxylase structure. |
| AID323617 | Inhibition of metallo beta lactamase VIM4 assessed as residual enzyme activity at 100 uM | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila. |
| AID517386 | Inhibition of FIH by HTRF assay | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
| Structural basis for binding of cyclic 2-oxoglutarate analogues to factor-inhibiting hypoxia-inducible factor. |
| AID1282320 | Selectivity ratio of IC50 for KDM2A (unknown origin) expressed in Escherichia coli to IC50 for KDM4C (1 to 352 residues) (unknown origin) expressed in Escherichia coli | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID344924 | Inhibition of human recombinant HIF PHD3 | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
| AID344918 | Inhibition of 2-oxoglutarate-dependent human JMJD2E preincubated for 30 mins by FDH coupled assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
| AID517384 | Inhibition of PHD1 by HTRF assay | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
| Structural basis for binding of cyclic 2-oxoglutarate analogues to factor-inhibiting hypoxia-inducible factor. |
| AID1677974 | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and high 20 uM FAS incubated for 35 mins by MS analysis | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
| Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase. |
| AID734755 | Inhibition of human hexahistidine-tagged full-length FTO expressed in Escherichia coli BL21 (DE3) using 3-methylthymidine as substrate assessed as inhibition of 3-methylthymidine conversion to thymidine after 1 hr by liquid chromatographic analysis | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
| Structural basis for inhibition of the fat mass and obesity associated protein (FTO). |
| AID344922 | Inhibition of human collagene prolyl-3-hydroxylase | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
| AID344916 | Inhibition of 2-oxoglutarate-dependent human JMJD2E in presence of excess 2-oxoglutarate and 10 uM Fe2 by FDH coupled assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
| AID344917 | Inhibition of 2-oxoglutarate-dependent human JMJD2E in presence of excess H3K9me3 peptide and 10 uM Fe2 by FDH coupled assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
| AID323614 | Inhibition of Pseudomonas aeruginosa 101/1477 metallo beta lactamase IMP1 expressed in in Escherichia coli assessed as residual enzyme activity at 100 uM in presence of zinc chloride | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila. |
| AID1785094 | Inhibition of N-terminal His6-tagged KDM4E (1 to 337 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3)-R3 assessed as Km at 1 uM in presence of alpha-KG by Michaelis-Menten analysis (Rvb = 22 uM) | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Enhanced Properties of a Benzimidazole Benzylpyrazole Lysine Demethylase Inhibitor: Mechanism-of-Action, Binding Site Analysis, and Activity in Cellular Models of Prostate Cancer. |
| AID517385 | Inhibition of PHD2 at 1 mM by HTRF assay | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
| Structural basis for binding of cyclic 2-oxoglutarate analogues to factor-inhibiting hypoxia-inducible factor. |
| AID1282321 | Selectivity ratio of IC50 for KDM6B (unknown origin) expressed in Escherichia coli to IC50 for KDM4C (1 to 352 residues) (unknown origin) expressed in Escherichia coli | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID1282314 | Inhibition of KDM6B (unknown origin) expressed in Escherichia coli using H3 (21 to 44 residues) K27Me3-GGK-Biotin JMJD3 Cognate Ligand/10 uM alpha-ketoglutarate as substrate/cofactor preincubated for 5 mins followed by substrate addition measured after 5 | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID1249065 | Inhibition of KDM3A (unknown origin) | 2014 | MedChemComm, Dec-01, Volume: 5, Issue:12
| Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor. |
| AID1282313 | Inhibition of KDM2A (unknown origin) expressed in Escherichia coli using Biotin H3 (28 to 48 residues) Me2 KDM2A Cognate Ligande/10 uM alpha-ketoglutarate as substrate/cofactor preincubated for 15 mins followed by substrate addition measured after 30 mins | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID1810105 | Inhibition of recombinant human NO66 expressed in Escherichia coli BL21 (DE3) using RPL8 N205PVEHPFGGGNHQHIGKPST224 as substrate preincubated for 15 mins followed by substrate addition and measured after 30 to 60 mins by RapidFire Mass spectrometry assay | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
| First-in-Class Inhibitors of the Ribosomal Oxygenase MINA53. |
| AID1652966 | Inhibition of recombinant KDM5B catalytic domain (1 to 769 residues) (unknown origin) | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Lysine demethylase 5B (KDM5B): A potential anti-cancer drug target. |
| AID1181277 | Inhibition of purified recombinant KDM4D (1 to 350 aa) (unknown origin) expressed in Escherichia coli using H3K9me3 peptide as substrate after 30 mins by FDH-coupled assay | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| KDM4B as a target for prostate cancer: structural analysis and selective inhibition by a novel inhibitor. |
| AID721529 | Displacement of 2OG from catalytic domain of PHD2 (181 to 426) (unknown origin) expressed in Escherichia coli at 400 uM | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
| Reporter ligand NMR screening method for 2-oxoglutarate oxygenase inhibitors. |
| AID323618 | Inhibition of Aeromonas hydrophila metallo beta lactamase CphA assessed as residual enzyme activity at 100 uM in absence of zinc | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila. |
| AID770454 | Inhibition of KDM2A (unknown origin) | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity. |
| AID1282306 | Competitive inhibition of N-terminal His6-tagged KDM4C (1 to 352 residues) (unknown origin) expressed in Escherichia coli Rosetta 2(DE3)pLysS using 50 uM ARK(Me3)STGGK peptide/50 uM alpha-ketoglutarate as substrate/cofactor by FDH coupling-based Lineweave | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID678711 | Inhibition of KDM6A | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18
| Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C). |
| AID344925 | Inhibition of human JMJD2A by FDH coupled assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
| AID499338 | Inhibition of human recombinant PHD1 expressed in Sf9 cells by time-resolved fluorescence assay | 2010 | Journal of medicinal chemistry, Aug-12, Volume: 53, Issue:15
| Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors. |
| AID1282315 | Inhibition of KDM5B (unknown origin) expressed in Escherichia coli using H3 (1 to 21 residues) K4Me3-GGK-Biotin KDM5B Cognate Ligand/10 uM alpha-ketoglutarate as substrate/cofactor preincubated for 5 mins followed by substrate addition measured after 20 m | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID1282325 | Competitive inhibition of N-terminal His6-tagged KDM4C (1 to 352 residues) (unknown origin) expressed in Escherichia coli Rosetta 2(DE3)pLysS using ARK(Me3)STGGK peptide/alpha-ketoglutarate as substrate/cofactor by FDH coupling-based Lineweaver-Burk plot | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID1677975 | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using high 10 uM hFX-CP as substrate mixture with 10 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
| Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase. |
| AID344919 | Inhibition of 2-oxoglutarate-dependent human JMJD2E in presence of 50 uM Fe by FDH coupled assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
| AID1282316 | Inhibition of KDM3A (unknown origin) expressed in Escherichia coli using H3 (1 to 21 residues) K9Me2-GGK-Biotin KDM3A Cognate Ligand/10 uM alpha-ketoglutarate as substrate/cofactor preincubated for 5 mins followed by substrate addition measured after 20 m | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID1282308 | Competitive inhibition of N-terminal His6-tagged KDM4C (1 to 352 residues) (unknown origin) expressed in Escherichia coli Rosetta 2(DE3)pLysS using 50 uM ARK(Me3)STGGK peptide/5 uM alpha-ketoglutarate as substrate/cofactor by FDH coupling-based Lineweaver | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID1677971 | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) at 20uM using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20
| Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase. |
| AID1282304 | Inhibition of N-terminal His6-tagged KDM4C (1 to 352 residues) (unknown origin) expressed in Escherichia coli Rosetta 2(DE3)pLysS using biotinylated histone H3 (1 to 21 residues) lysine 9 trimethylated peptide/2 uM alpha-ketoglutarate as substrate/cofacto | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID1282323 | Selectivity ratio of IC50 for KDM3A (unknown origin) expressed in Escherichia coli to IC50 for KDM4C (1 to 352 residues) (unknown origin) expressed in Escherichia coli | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID323613 | Inhibition of Pseudomonas aeruginosa 101/1477 metallo beta lactamase IMP1 expressed in in Escherichia coli assessed as residual enzyme activity at 100 uM in absence of zinc | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| Competitive inhibitors of the CphA metallo-beta-lactamase from Aeromonas hydrophila. |
| AID770457 | Inhibition of KDM5A (unknown origin) using H3K4me3 peptide and 2-oxoglutarate as substrate after 1 hr by FDH-coupled assay | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity. |
| AID1282324 | Selectivity ratio of IC50 for KDM4D (unknown origin) expressed in Escherichia coli to IC50 for KDM4C (1 to 352 residues) (unknown origin) expressed in Escherichia coli | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors. |
| AID1230198 | Inhibition of N-terminal hexa-histidine tagged human PHD2 (181 to 426 amino acids) at 10 uM pre-incubated for 2 mins followed by alpha-ketoglutarate addition using HIF1alpha peptide (556 to 574 amino acids) and 50 uM FeSO4 by RP-HPLC method | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Selective inhibition of prolyl 4-hydroxylases by bipyridinedicarboxylates. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | | | |
| AID1801992 | Demethylase AlphaScreen Assay from Article 10.1038/nchembio.2087: \\Structural analysis of human KDM5B guides histone demethylase inhibitor development.\\ | 2016 | Nature chemical biology, 07, Volume: 12, Issue:7
| Structural analysis of human KDM5B guides histone demethylase inhibitor development. |
| AID1798635 | FDH Coupled Inhibition Assay from Article 10.1021/jm800936s: \\Inhibitor Scaffolds for 2-Oxoglutarate-Dependent Histone Lysine Demethylases.\\ | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
| Inhibitors of histone demethylases. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
| Structural basis for inhibition of the fat mass and obesity associated protein (FTO). |
| AID1346034 | Human lysine demethylase 4E (1.14.11.- Histone demethylases) | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
| AID1346021 | Human lysine demethylase 4A (1.14.11.- Histone demethylases) | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |