Assay ID | Title | Year | Journal | Article |
AID1347157 | Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347169 | Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347161 | Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347167 | Vero cells viability qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347149 | Furin counterscreen qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347152 | Confirmatory screen NINDS AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347168 | HepG2 cells viability qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347153 | Confirmatory screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1675344 | In vivo inhibition of PHD2 in po dosed C57BL/6 mouse assessed as upregulation of EPO plasma level administered 4 times for 3 days by ELISA | | | |
AID1497731 | Intrinsic aqueous solubility of the compound at pH 7.4 by potentiometric titration method | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1497726 | Inhibition of HIF-PHD2 in human Hep3B cells assessed as HIF-1alpha protein stabilization at 50 to 250 uM after 10 hrs by Western blot method | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1910214 | Inhibition of PHD2 (unknown origin) incubated for 15 mins by competitive fluorescence polarization assay | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
AID1495354 | Terminal half life in patient with hepatic impairment at 100 mg, po | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
| Discovery of novel 2-[(4-hydroxy-6-oxo-2,3-dihydro-1H-pyridine-5-carbonyl)amino]acetic acid derivatives as HIF prolyl hydroxylase inhibitors for treatment of renal anemia. |
AID1067647 | Reduction in total cholesterol level in chronic kidney disease patient administered for 16 to 24 weeks relative to control | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23
| Inhibition of hypoxia-inducible factor prolyl hydroxylase domain oxygen sensors: tricking the body into mounting orchestrated survival and repair responses. |
AID1675363 | Inhibition of FITC-HIF1alpha (556 to 574 residues) binding to PHD2 (181 to 426 residues) (unknown origin) by fluorescence polarization assay | | | |
AID1917461 | Cytotoxicity against human Hep3B cells assessed as cell viability at 100 ug/ml measured by MTT assay | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues. |
AID1901050 | Inhibition of PHD2 (unknown origin) at 1 uM measured by fluorescence polarization assay relative to control | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID1675362 | Selectivity index, ratio of IC50 for PHD1 (unknown origin) by O-phenyl enediamine(OPD) based fluorescence assay to IC50 for PHD2 (unknown origin) by O-phenyl enediamine(OPD) based fluorescence assay | | | |
AID1497717 | Selectivity ratio of IC50 for JMJD2A (unknown origin) by Alphascreen assay to IC50 for HIF-PHD2 (181 to 426 residues) (unknown origin) by fluorescence polarization assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1543455 | Inhibition of recombinant human OGFOD1 using 2OG as substrate and Fe2 as co-factor assessed as hydroxylation incubated for 15 mins in presence of L-ascorbate by MALDI-TOF MS analysis | 2019 | Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
| Inhibition of a viral prolyl hydroxylase. |
AID1901068 | Antiproliferative activity against human HK-2 cells assessed as decrease in cell viability at 50 uM measured in presence of 10 uM cisplatin after 24 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID1497723 | Inhibition of HIF-PHD2 (unknown origin) expressed in HEK293 cells harboring HRE-driven luciferase gene assessed as HIFalpha stabilization at 150 uM after 24 hrs by luciferase reporter gene assay relative to control | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1497708 | Selectivity ratio of IC50 for JMJD3 (unknown origin) by Alphascreen assay to IC50 for HIF-PHD2 (181 to 426 residues) (unknown origin) by fluorescence polarization assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1910212 | Agonist activity at human TR beta LBD (202 to 461 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as induction of N-terminal biotinylated coactivator SRC2-3 peptide recruitment by alphascreen assay | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
AID1067648 | Antianemic activity in nondialysis chronic kidney disease patient assessed as increase in hemoglobin level at 60 to 150 mg administered twice/thrice weekly for 16 to 24 weeks | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23
| Inhibition of hypoxia-inducible factor prolyl hydroxylase domain oxygen sensors: tricking the body into mounting orchestrated survival and repair responses. |
AID1901071 | Nephroprotective activity against cisplatin-induced acute kidney injury in male C57BL/6 mouse assessed as serum EPO level at 10 mg/kg/day, ip | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID1917455 | Inhibition of PHD2 in human Hep3B cells assessed as increase in EPO production measured after 24 hrs by ELISA | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues. |
AID1497718 | Cytotoxicity against human L02 cells assessed as reduction in cell viability at 10 to 100 uM after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
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. |
AID1917752 | Induction of HIF-2alpha stabilization in human Hep3B cells assessed as HIF-1alpha level at 1 to 100 uM incubated for 24 hrs by immunoblot analysis | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Improving lipophilicity of 5-(1-acetyl-5-phenylpyrazolidin-3-ylidene)-1,3-dimethylbarbituric acid increases its efficacy to activate hypoxia-inducible factors. |
AID1675357 | Selectivity index, ratio of IC50 for human ERG expressed in HEK293 cells by PatchLiner assay to IC50 for PHD2 (unknown origin) by O-phenyl enediamine(OPD) based fluorescence assay | | | |
AID1497732 | Effective permeability of the compound at pH 7.4 by PAMPA | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1497728 | Inhibition of HIF-PHD2 in human Hep3B cells assessed as upregulation of EPO mRNA level at 50 uM after 10 hrs by RT-PCR method | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1675355 | Inhibition of PHD2 in human Hep3B cells assessed as upregulation of HIF-2alpha level after 10 hrs by Western blot analysis | | | |
AID1497719 | Cytotoxicity against human Hep3B cells assessed as reduction in cell viability at 10 to 100 uM after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1497713 | Inhibition of HIF-PHD3 (unknown origin) using HIF1-alpha (556 to 574 residues) as substrate in presence of 2-OG preincubated for 30 mins followed by OPD addition measured after 10 mins by fluorescence assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1497715 | Selectivity ratio of IC50 for HIF-PHD3 (unknown origin) by OPD fluorescence assay to IC50 for HIF-PHD2 (181 to 426 residues) (unknown origin) by OPD fluorescence assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1675360 | Selectivity index, ratio of IC50 for KDM3A (unknown origin) in presence of peptide substrate incubated for 30 mins by alpha screen assay to IC50 for PHD2 (unknown origin) by O-phenyl enediamine(OPD) based fluorescence assay | | | |
AID1917457 | Inhibition of PHD2 in human Hep3B cells assessed as stabilization of HIF-2alpha at 100 uM incubated for 4 hrs | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues. |
AID1576662 | Inhibition of PHD2 (181 to 426 residues) (unknown origin) using FITC-HIF1alpha (556 to 574 residues) as substrate after 60 mins by fluorescence polarization assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
| Photoactivatable Prolyl Hydroxylase 2 Inhibitors for Stabilizing the Hypoxia-Inducible Factor with Light. |
AID1067649 | Antianemic activity in end stage renal disease patient receiving hemodialysis assessed as increase in hemoglobin level at 1.5 to 2 mg/kg, po administered thrice weekly for 6 weeks relative to control | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23
| Inhibition of hypoxia-inducible factor prolyl hydroxylase domain oxygen sensors: tricking the body into mounting orchestrated survival and repair responses. |
AID1067646 | Antianemic activity in human assessed as change in hemoglobin level administered thrice weekly for 12 weeks | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23
| Inhibition of hypoxia-inducible factor prolyl hydroxylase domain oxygen sensors: tricking the body into mounting orchestrated survival and repair responses. |
AID1497730 | Lipophilicity, log D of the compound at pH 7.4 by potentiometric titration method | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1917458 | Inhibition of PHD2 in human Hep3B cells assessed as stabilization of HIF-1alpha at 100 uM incubated for 4 hrs | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues. |
AID1654632 | Substrate activity at aldehyde oxidase in human liver cytosol at 10 uM measured after 3 hrs by UPLC/Q-TOF MS analysis | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model. |
AID1884425 | Inhibition of PHD2 (181 to 426 residue) (unknown origin) measured by fluorescence polarization assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Tetrahydropyridin-4-ylpicolinoylglycines as novel and orally active prolyl hydroxylase 2 (PHD2) inhibitors for the treatment of renal anemia. |
AID1675358 | Selectivity index, ratio of IC50 for KDM6B (unknown origin) in presence of peptide substrate incubated for 30 mins by alpha screen assay to IC50 for PHD2 (unknown origin) by O-phenyl enediamine(OPD) based fluorescence assay | | | |
AID1497729 | Dissociation constant, pKa of the compound by potentiometric titration method | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1917460 | Inhibition of PHD2 (unknown origin) at 66.7 uM relative to control | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues. |
AID1354532 | Half life in human at 1 to 2 mg/kg, po administered as two or three times weekly | 2018 | Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
| Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases. |
AID1497722 | Inhibition of HIF-PHD2 (unknown origin) expressed in HEK293 cells harboring HRE-driven luciferase gene assessed as HIFalpha stabilization at 50 uM after 24 hrs by luciferase reporter gene assay relative to control | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1497716 | Selectivity ratio of IC50 for JMJD1A (unknown origin) by Alphascreen assay to IC50 for HIF-PHD2 (181 to 426 residues) (unknown origin) by fluorescence polarization assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
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). |
AID1917751 | Induction of HIF-1alpha stabilization in human Hep3B cells assessed as HIF-1alpha level at 1 to 100 uM incubated for 24 hrs by immunoblot analysis | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Improving lipophilicity of 5-(1-acetyl-5-phenylpyrazolidin-3-ylidene)-1,3-dimethylbarbituric acid increases its efficacy to activate hypoxia-inducible factors. |
AID1354531 | Antianemic activity in human assessed as increase in hemoglobin level | 2018 | Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
| Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases. |
AID1543454 | Inhibition of recombinant human FIH 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. |
AID1901053 | Inhibition of PHD2 (unknown origin) measured by fluorescence polarization assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID1675262 | Antianemic activity in cisplatin-induced C57BL/6 mouse anemia model assessed as improvement in anemia at 10 mg/kg, po administered every other day for 1 month | | | |
AID1675350 | Inhibition of PHD2 in human MCF7 cells assessed as stabilization of HIFalpha at 5 to 50 uM incubated for 24 hrs by firefly/renilla luciferase reporter gene assay | | | |
AID1901069 | Nephroprotective activity against cisplatin-induced acute kidney injury in male C57BL/6 mouse assessed as plasma BUN concentration at 10 mg/kg/day, ip | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID1917462 | Cytotoxicity against human Hep3B cells assessed as cell viability at 12.5 ug/ml measured by MTT assay | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues. |
AID1675356 | Inhibition of PHD2 in human Hep3B cells assessed as upregulation of HIF-1alpha level after 10 hrs by Western blot analysis | | | |
AID1497721 | Cytotoxicity against HUVEC assessed as reduction in cell viability at 10 to 100 uM after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1901066 | Antiproliferative activity against human HK-2 cells assessed as decrease in cell viability at 100 uM measured after 24 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID1497714 | Selectivity ratio of IC50 for HIF-PHD1 (unknown origin) by OPD fluorescence assay to IC50 for HIF-PHD2 (181 to 426 residues) (unknown origin) by OPD fluorescence assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1675343 | In vivo inhibition of PHD2 in C57BL/6 mouse assessed as upregulation of EPO plasma level by measuring EPO level at 15 mg/kg, po measured after 4 hrs by ELISA | | | |
AID1675361 | Selectivity index, ratio of IC50 for PHD3 (unknown origin) to IC50 for PHD2 (unknown origin) by O-phenyl enediamine(OPD) based fluorescence assay | | | |
AID1901049 | Inhibition of PHD2 (unknown origin) at 0.5 uM measured by fluorescence polarization assay relative to control | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID1067650 | Antianemic activity in chronic kidney disease patient assessed as hemoglobin level administered for 4 weeks | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23
| Inhibition of hypoxia-inducible factor prolyl hydroxylase domain oxygen sensors: tricking the body into mounting orchestrated survival and repair responses. |
AID1910213 | Binding affinity to human TR beta LBD (202 to 461 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as change in melting temperature at 10 uM in presence of ZnSO4 by thermal shift assay | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
AID1497753 | Antianemic activity in C57BL/6 mouse cisplatin-induced anemia model assessed as increase in hemoglobin level at 10 mg/kg, po administered every other day for 30 days relative to control | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1497752 | Antianemic activity in C57BL/6 mouse cisplatin-induced anemia model assessed as increase in hemoglobin level administered po every other day for 30 days | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1497754 | Antianemic activity in C57BL/6 mouse cisplatin-induced anemia model assessed as increase in hemoglobin level at 25 mg/kg, po administered every other day for 30 days relative to control | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1901051 | Inhibition of PHD2 (unknown origin) at 10 uM measured by fluorescence polarization assay relative to control | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID1497709 | Inhibition of HIF-PHD2 (181 to 426 residues) (unknown origin) using FITC-HIF1-alpha (556 to 574 residues) as substrate after 60 mins by fluorescence polarization assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
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. |
AID1675261 | Antianemic activity in cisplatin-induced C57BL/6 mouse anemia model assessed as improvement in anemia at 25 mg/kg, po administered every other day for 1 month | | | |
AID1735098 | Inhibition of HIF-PHD2 (unknown origin) | 2016 | Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
| Discovery of N-[Bis(4-methoxyphenyl)methyl]-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide (MK-8617), an Orally Active Pan-Inhibitor of Hypoxia-Inducible Factor Prolyl Hydroxylase 1-3 (HIF PHD1-3) for the Treatment of Anemia. |
AID1497720 | Cytotoxicity against HEK293 cells assessed as reduction in cell viability at 10 to 100 uM after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1497751 | Upregulation of plasma EPO level in C57BL/6 mouse at 10 to 50 mg/kg, po after 4 hrs by ELISA | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1675359 | Selectivity index, ratio of IC50 for KDM4A (unknown origin) in presence of peptide substrate incubated for 30 mins by alpha screen assay to IC50 for PHD2 (unknown origin) by O-phenyl enediamine(OPD) based fluorescence assay | | | |
AID1280627 | Displacement of FITC-HIF-1alpha (556 to 574 residues) from PHD2 (181 to 426 residues) (unknown origin) after 60 mins by fluorescence polarization assay | 2015 | ACS medicinal chemistry letters, Dec-10, Volume: 6, Issue:12
| Affinity-Based Fluorescence Polarization Assay for High-Throughput Screening of Prolyl Hydroxylase 2 Inhibitors. |
AID1497712 | Inhibition of HIF-PHD2 (181 to 426 residues) (unknown origin) using HIF1-alpha (556 to 574 residues) as substrate in presence of 2-OG preincubated for 30 mins followed by OPD addition measured after 10 mins by fluorescence assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1497748 | Upregulation of plasma EPO level in C57BL/6 mouse at 10 mg/kg, iv after 4 hrs by ELISA | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1910211 | Agonist activity at wild type human TR alpha LBD expressed in Escherichia coli BL21 (DE3) assessed as induction of N-terminal biotinylated coactivator SRC2-3 peptide recruitment by alphascreen assay | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
AID1901070 | Nephroprotective activity against cisplatin-induced acute kidney injury in male C57BL/6 mouse assessed as plasma SCr concentration at 10 mg/kg/day, ip | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. |
AID1497727 | Inhibition of HIF-PHD2 in human Hep3B cells assessed as HIF-2alpha protein stabilization at 50 to 250 uM after 10 hrs by Western blot method | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia. |
AID1917456 | In vivo inhibition of PHD2 in ICR mouse assessed as increase in serum EPO production at 10 mg/kg, po and measured after 4 hrs by ELISA | 2022 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 76 | Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues. |
AID1675341 | Induction of erythropoiesis in po dosed C57BL/6 mouse assessed as increase in red blood cell count administered thrice for 3 days measured 4 hrs post last dose | | | |
AID1354533 | In vivo inhibition of PHD in human assessed as induction of EPO level in serum at 1 mg/kg, po administered as twice weekly measured at 4 to 10 hrs post dose | 2018 | Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
| Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases. |
AID1675285 | Antianemic activity in cisplatin-induced C57BL/6 mouse anemia model assessed as increase in haemoglobin level administered orally every other day for 1 month | | | |
AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |