| Assay ID | Title | Year | Journal | Article |
|---|
| AID1422905 | Inhibition of PAD3 (unknown origin) assessed as ratio of Kinact to Ki | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
| Synthesis and Biological Evaluation of an Indazole-Based Selective Protein Arginine Deiminase 4 (PAD4) Inhibitor. |
| AID712877 | Selectivity ratio of Kinact to Ki for PAD1 to Kinact to Ki for PAD2 | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID1422904 | Inhibition of PAD4 (unknown origin) assessed as ratio of Kinact to Ki | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
| Synthesis and Biological Evaluation of an Indazole-Based Selective Protein Arginine Deiminase 4 (PAD4) Inhibitor. |
| AID1422899 | Inhibition of PAD3 (unknown origin) assessed as ratio of Kinact to Ki preincubated for 2.5 to 30 mins followed by BAEE addition measured after 15 mins by spectrophotometric method | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
| Synthesis and Biological Evaluation of an Indazole-Based Selective Protein Arginine Deiminase 4 (PAD4) Inhibitor. |
| AID712871 | Toxicity in C57BL/6J mouse assessed as anxiety at 150 mg/kg, po after 1 to 4 hrs | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID1632999 | Inhibition of AcGFP1-1-tagged PAD3 (unknown origin) expressed in HEK293T cells assessed as protection against thapsigargin-induced cell death measured as cell viability at 10 uM measured after 48 hrs by CellTiter-Glo assay | 2016 | ACS medicinal chemistry letters, Sep-08, Volume: 7, Issue:9
| Cellular Activity of New Small Molecule Protein Arginine Deiminase 3 (PAD3) Inhibitors. |
| AID712872 | Toxicity in C57BL/6J mouse assessed as occurrence of diarrhea at 150 mg/kg, po after 2 to 3 days | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID712870 | Toxicity in C57BL/6J mouse assessed as loss in body weight at 100 to 150 mg/kg, po after 96 hrs | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID1364667 | Ratio of Kinact to Ki for recombinant His6-tagged PAD3 (unknown origin) preincubated for 10 mins followed by BAA substrate addition measured after 15 mins by COLDER assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Development of a Selective Inhibitor of Protein Arginine Deiminase 2. |
| AID1422898 | Inhibition of PAD4 (unknown origin) assessed as ratio of Kinact to Ki preincubated for 2.5 to 30 mins followed by BAEE addition measured after 15 mins by spectrophotometric method | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
| Synthesis and Biological Evaluation of an Indazole-Based Selective Protein Arginine Deiminase 4 (PAD4) Inhibitor. |
| AID725673 | Inhibition of PAD4 (unknown origin) | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
| Interrogation of the Active Sites of Protein Arginine Deiminases (PAD1, -2, and -4) Using Designer Probes. |
| AID712852 | Toxicity in C57BL/6J mouse assessed as hunching at 150 mg/kg, po after 1 to 4 hrs | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID1422901 | Inhibition of PAD1 (unknown origin) assessed as ratio of Kinact to Ki preincubated for 2.5 to 30 mins followed by BAEE addition measured after 15 mins by spectrophotometric method | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
| Synthesis and Biological Evaluation of an Indazole-Based Selective Protein Arginine Deiminase 4 (PAD4) Inhibitor. |
| AID712868 | Toxicity in po dosed C57BL/6J mouse | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID712860 | Drug metabolism in C57Bl/6 mouse at 10 mg/kg, iv measured within 2 hrs by LC-MS/MS analysis | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID712858 | Drug metabolism in C57Bl/6 mouse at 10 mg/kg, ip measured within 4 hrs by LC-MS/MS analysis | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID1422907 | Inhibition of PAD1 (unknown origin) assessed as ratio of Kinact to Ki | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
| Synthesis and Biological Evaluation of an Indazole-Based Selective Protein Arginine Deiminase 4 (PAD4) Inhibitor. |
| AID1196532 | Inhibition of PAD4 in C57BL/6 mouse bone marrow neutrophils assessed as inhibition of PMA-stimulated neutrophil extracellular trap formation at 2 to 200 uM preincubated for 30 mins followed by PMA stimulation measured after 3 to 4 hrs by DNA/neutrophil el | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Design, synthesis, and biological evaluation of tetrazole analogs of Cl-amidine as protein arginine deiminase inhibitors. |
| AID1422900 | Inhibition of PAD2 (unknown origin) assessed as ratio of Kinact to Ki preincubated for 2.5 to 30 mins followed by BAEE addition measured after 15 mins by spectrophotometric method | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
| Synthesis and Biological Evaluation of an Indazole-Based Selective Protein Arginine Deiminase 4 (PAD4) Inhibitor. |
| AID712873 | Toxicity in C57BL/6J mouse assessed as body shaking at 150 mg/kg, po after 1 to 4 hrs | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID712864 | Antiproliferative activity against human MDA-MB-231 cells assessed as Ki-67 level at 100 to 400 uM | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID712874 | Selectivity ratio of Kinact to Ki for PAD1 to Kinact to Ki for PAD4 | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID1422917 | Inhibition of PAD4 in human HL60 cells assessed as reduction in A23187-induced citrullinated H4 level at 5 to 10 uM preincubated for 15 mins followed by A23187 addition measured after 15 mins by Western blot analysis | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
| Synthesis and Biological Evaluation of an Indazole-Based Selective Protein Arginine Deiminase 4 (PAD4) Inhibitor. |
| AID712866 | Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell number at 400 uM after 96 hrs by trypan blue assay | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID1813074 | Inhibition of PDE4 (unknown origin) by colorimetric assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Peptidylarginine deiminases 4 as a promising target in drug discovery. |
| AID712876 | Ratio of Kinact to Ki for PAD4 | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID1422906 | Inhibition of PAD2 (unknown origin) assessed as ratio of Kinact to Ki | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
| Synthesis and Biological Evaluation of an Indazole-Based Selective Protein Arginine Deiminase 4 (PAD4) Inhibitor. |
| AID712875 | Selectivity ratio of Kinact to Ki for PAD1 to Kinact to Ki for PAD3 | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID1196529 | Antiproliferative activity against human U2OS cells expressing PAD4 assessed as cell viability after 72 hrs by XTT assay | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Design, synthesis, and biological evaluation of tetrazole analogs of Cl-amidine as protein arginine deiminase inhibitors. |
| AID1196527 | Ratio of Kinact to Ki for PAD2 (unknown origin) using N-alpha-benzoyl-L-arginine ethyl ester as substrate assessed as citrulline production after 15 mins by COLDER assay | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Design, synthesis, and biological evaluation of tetrazole analogs of Cl-amidine as protein arginine deiminase inhibitors. |
| AID712867 | Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability at 200 to 400 uM after 96 hrs by trypan blue assay | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID712879 | Ratio of Kinact to Ki for PAD1 | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID712862 | Induction of apoptosis in human MDA-MB-231 cells assessed as increase in caspase-3 activity | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID1364668 | Ratio of Kinact to Ki for recombinant full length N-terminal GST-tagged human PAD4 expressed in Escherichia coli Rosetta cells preincubated for 10 mins followed by BAEE substrate addition measured after 15 mins by COLDER assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Development of a Selective Inhibitor of Protein Arginine Deiminase 2. |
| AID712880 | Ratio of Kinact to Ki for PAD2 | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID1364665 | Ratio of Kinact to Ki for recombinant His6-tagged PAD1 (unknown origin) preincubated for 10 mins followed by BAEE substrate addition measured after 15 mins by COLDER assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Development of a Selective Inhibitor of Protein Arginine Deiminase 2. |
| AID1364666 | Ratio of Kinact to Ki for recombinant human PAD2 expressed in Escherichia coli BL21(DE3)pLysS cells preincubated for 10 mins followed by BAEE substrate addition measured after 15 mins by COLDER assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Development of a Selective Inhibitor of Protein Arginine Deiminase 2. |
| AID712850 | Toxicity in C57BL/6J mouse assessed as bloody stools at 150 mg/kg, po | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID1664695 | Cytotoxicity against human U2OS cells assessed as reduction in cell viability by CellTiter 96 non-radioactive cell proliferation assay | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
| Tetrazoles as anticancer agents: A review on synthetic strategies, mechanism of action and SAR studies. |
| AID712878 | Ratio of Kinact to Ki for PAD3 | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID712859 | Half life in mouse liver microsomes | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID712851 | Toxicity in C57BL/6J mouse assessed as heavy breathing at 150 mg/kg, po after 1 to 4 hrs | 2012 | ACS medicinal chemistry letters, Oct-26, Volume: 3, Issue:12
| D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. |
| AID1346233 | Human peptidyl arginine deiminase 3 (3.5.3.15 Peptidyl arginine deiminases (PADI)) | 2015 | Journal of the American Chemical Society, Mar-18, Volume: 137, Issue:10
| Identification of multiple structurally distinct, nonpeptidic small molecule inhibitors of protein arginine deiminase 3 using a substrate-based fragment method. |
| AID1346144 | Human peptidyl arginine deiminase 4 (3.5.3.15 Peptidyl arginine deiminases (PADI)) | 2015 | Journal of the American Chemical Society, Mar-18, Volume: 137, Issue:10
| Identification of multiple structurally distinct, nonpeptidic small molecule inhibitors of protein arginine deiminase 3 using a substrate-based fragment method. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |