fg-4592 profile

ID Source	ID
PubMed CID	11256664
CHEMBL ID	2338329
SCHEMBL ID	523705
CHEBI ID	132774
MeSH ID	M0589156

Synonym
fg-4592 ,
roxadustat
CHEBI:132774
808118-40-3
fg4592
n-[(4-hydroxy-1-methyl-7-phenoxyisoquinolin-3-yl)carbonyl]glycine
roxadustatum
fg 4592
n-[(4-hydroxy-1-methyl-7-phenoxy-3-isoquinolinyl)carbonyl]glycine
bdbm50431015
glycine, n-[(4-hydroxy-1-methyl-7-phenoxy-3-isoquinolinyl)carbonyl]-
BCP9000684
HY-13426
CS-1094
BCPP000230
fg-4592,asp1517
roxadustat (fg-4592)
NCGC00346527-01
(((4-hydroxy-1-methyl-7-phenoxyisoquinolin-3-yl)carbonyl)amino)acetic acid
roxadustat [usan:inn]
x3o30d9ymx ,
asp 1517
unii-x3o30d9ymx
S1007
roxadustat [who-dd]
roxadustat [jan]
glycine, n-((4-hydroxy-1-methyl-7-phenoxy-3-isoquinolinyl)carbonyl)-
roxadustat [inn]
roxadustat [usan]
n-((4-hydroxy-1-methyl-7-phenoxy-3-isoquinolinyl)carbonyl)glycine
asp1517
asp-1517
CHEMBL2338329 ,
MLS006010023
smr004701207
SCHEMBL523705
DTXSID60230644
roxadustat (jan/usan/inn)
evrenzo (tn)
D10593
gtpl8454
evrenzo
2-[[4-hydroxy-1-methyl-7-(phenoxy)isoquinoline-3-carbonyl]amino]acetic acid
(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)glycine
AC-31003
2-[(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)amino]acetic acid
fg-4592[roxadustat]
AKOS026674331
J-522733
EX-A390
2-(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxamido)acetic acid
HMS3654M03
mfcd20040519
NCGC00346527-07
YOZBGTLTNGAVFU-UHFFFAOYSA-N
SW219900-1
roxadustat(fg-4592)
DB04847
Q27088611
AS-17052
BCP02523
AMY16514
8ho ,
2-[(1-methyl-4-oxidanyl-7-phenoxy-isoquinolin-3-yl)carbonylamino]ethanoic acid
SB16615
CCG-268052
n-[(4-hydroxy-1-methyl-7-phenoxy-3-isoquinolinyl)carbonyl]-glycine, roxadustat

Role	Description
EC 1.14.11.2 (procollagen-proline dioxygenase) inhibitor	An EC 1.14.11.* (oxidoreductase acting on paired donors, 2-oxoglutarate as one donor, incorporating 1 atom each of oxygen into both donors) inhibitor that interferes with the action of procollagen-proline dioxygenase (EC 1.14.11.2).
EC 1.14.11.29 (hypoxia-inducible factor-proline dioxygenase) inhibitor	An EC 1.14.11.* (oxidoreductase acting on paired donors, 2-oxoglutarate as one donor, incorporating 1 atom each of oxygen into both donors) inhibitor that interferes with the action of hypoxia-inducible factor-proline dioxygenase (EC 1.14.11.29).

Class	Description
isoquinolines	A class of organic heteropolycyclic compound consisting of isoquinoline and its substitution derivatives.
aromatic ether	Any ether in which the oxygen is attached to at least one aryl substituent.
N-acylglycine	An N-acyl-amino acid in which amino acid specified is glycine.

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)
EWS/FLI fusion protein	Homo sapiens (human)	Potency	5.8992	AID1259252

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)
Prolyl 4-hydroxylase	Paramecium bursaria Chlorella virus 1	IC50	5.0000	AID1543452
Prolyl 4-hydroxylase	Paramecium bursaria Chlorella virus 1	Ki	1.0700	AID1543452
Prolyl 3-hydroxylase OGFOD1	Homo sapiens (human)	IC50	1.0000	AID1543455
Alpha-ketoglutarate-dependent dioxygenase FTO	Homo sapiens (human)	IC50	9.8000	AID734755
Egl nine homolog 1	Homo sapiens (human)	IC50	0.8836	AID1280627; AID1497709; AID1497712; AID1543453; AID1576662; AID1675363; AID1735098; AID1884425; AID1901053; AID1910214
Hypoxia-inducible factor 1-alpha inhibitor	Homo sapiens (human)	IC50	100.0000	AID1543454

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)
Thyroid hormone receptor alpha	Homo sapiens (human)	EC50	0.0327	AID1910211
Thyroid hormone receptor beta	Homo sapiens (human)	EC50	0.0129	AID1910212
Egl nine homolog 1	Homo sapiens (human)	EC50	6.1100	AID1917455

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 ISSN: 1091-6490	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 ISSN: 1091-6490	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 ISSN: 2472-5560	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 ISSN: 1521-0111	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 ISSN: 1521-0111	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 ISSN: 1091-6490	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 ISSN: 1091-6490	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 ISSN: 1091-6490	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 ISSN: 1949-2553	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 ISSN: 1949-2553	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 ISSN: 1949-2553	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 ISSN: 1949-2553	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 ISSN: 1091-6490	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 ISSN: 1949-2553	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 ISSN: 1949-2553	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 ISSN: 1949-2553	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 ISSN: 1091-6490	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 ISSN: 1949-2553	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 ISSN: 1949-2553	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 ISSN: 1949-2553	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 ISSN: 1949-2553	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 ISSN: 1949-2553	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: 173ISSN: 1872-9096	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 ISSN: 1091-6490	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1745845	Primary qHTS for Inhibitors of ATXN expression	2022	The Journal of biological chemistry, 08, Volume: 298, Issue:8 ISSN: 1083-351X
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 ISSN: 1949-2553	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 ISSN: 1949-2553	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 ISSN: 1949-2553	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: 173ISSN: 1872-9096	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 ISSN: 2211-1247	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 ISSN: 1091-6490	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 ISSN: 1949-2553	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: 173ISSN: 1872-9096	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 ISSN: 1949-2553	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 ISSN: 1949-2553	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 ISSN: 1949-2553	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 ISSN: 1949-2553	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 ISSN: 1091-6490	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 ISSN: 1091-6490	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	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804
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 ISSN: 1520-4804	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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 ISSN: 1464-3405	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 ISSN: 1520-4804	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	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804
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: 76ISSN: 1464-3405	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: 230ISSN: 1768-3254	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	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804
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 ISSN: 1520-4804	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 ISSN: 1464-3391	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: 230ISSN: 1768-3254	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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: 230ISSN: 1768-3254	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: 76ISSN: 1464-3405	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 ISSN: 1520-4804	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 ISSN: 1464-3391	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: 73ISSN: 1464-3391	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	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804
AID1497732	Effective permeability of the compound at pH 7.4 by PAMPA	2018	Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12 ISSN: 1520-4804	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 ISSN: 1520-4804	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	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804
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 ISSN: 1520-4804	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804
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: 76ISSN: 1464-3405	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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: 76ISSN: 1464-3405	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 ISSN: 1520-4804	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: 238ISSN: 1768-3254	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	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804
AID1497729	Dissociation constant, pKa of the compound by potentiometric titration method	2018	Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12 ISSN: 1520-4804	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: 76ISSN: 1464-3405	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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: 73ISSN: 1464-3391	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 ISSN: 1520-4804	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 ISSN: 1464-3391	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: 230ISSN: 1768-3254	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	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804
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	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804
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: 230ISSN: 1768-3254	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: 76ISSN: 1464-3405	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	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804
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 ISSN: 1520-4804	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: 230ISSN: 1768-3254	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 ISSN: 1520-4804	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	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804
AID1675361	Selectivity index, ratio of IC50 for PHD3 (unknown origin) to IC50 for PHD2 (unknown origin) by O-phenyl enediamine(OPD) based fluorescence assay	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804
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: 230ISSN: 1768-3254	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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: 230ISSN: 1768-3254	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 ISSN: 1520-4804	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 ISSN: 1464-3391	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	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804
AID1735098	Inhibition of HIF-PHD2 (unknown origin)	2016	Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24 ISSN: 1520-4804	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804
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 ISSN: 1948-5875	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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 ISSN: 1520-4804	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: 230ISSN: 1768-3254	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 ISSN: 1520-4804	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: 76ISSN: 1464-3405	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	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804
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 ISSN: 1520-4804	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	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 ISSN: 1520-4804
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 ISSN: 1554-8937	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	59 (31.38)	24.3611
2020's	129 (68.62)	2.80

Publication Type	This drug (%)	All Drugs (%)
Trials	30 (15.79%)	5.53%
Reviews	24 (12.63%)	6.00%
Case Studies	10 (5.26%)	4.05%
Observational	0 (0.00%)	0.25%
Other	126 (66.32%)	84.16%

Substance	Classes	Roles	Relationship Strength
pk 11195	aromatic amide; isoquinolines; monocarboxylic acid amide; monochlorobenzenes	antineoplastic agent	low
5-aminoisoquinolinone	isoquinolines		low
debrisoquin	carboxamidine; isoquinolines	adrenergic agent; antihypertensive agent; human metabolite; sympatholytic agent	low
ethaverine	isoquinolines		low
n-(2-(methylamino)ethyl)-5-isoquinolinesulfonamide	isoquinolines; sulfonamide		low
N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide	bromobenzenes; isoquinolines; olefinic compound; secondary amino compound; sulfonamide	EC 2.7.11.11 (cAMP-dependent protein kinase) inhibitor	low
1-(5-isoquinolinesulfonyl)-2-methylpiperazine	isoquinolines; N-sulfonylpiperazine	EC 2.7.11.13 (protein kinase C) inhibitor	low
1-(5-isoquinolinesulfonyl)piperazine	isoquinolines		low
ha 1004	isoquinolines		low
fasudil	isoquinolines; N-sulfonyldiazepane	antihypertensive agent; calcium channel blocker; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; geroprotector; neuroprotective agent; nootropic agent; vasodilator agent	low
hydrocotarnine	isoquinolines		low
nomifensine	isoquinolines	dopamine uptake inhibitor	low
6,7-dimethoxy-3-(4-methoxy-6-methyl-7,8-dihydro-5H-[1,3]dioxolo[4,5-g]isoquinolin-5-yl)-3H-isobenzofuran-1-one	isoquinolines		low
papaverine	benzylisoquinoline alkaloid; dimethoxybenzene; isoquinolines	antispasmodic drug; vasodilator agent	low
praziquantel	isoquinolines		low
scriptaid	isoquinolines		low
tilisolol	isoquinolines		low
cotarnine	isoquinolines		low
dimethisoquin	isoquinolines		low
1,2,3,4-tetrahydroisoquinoline	isoquinolines		low
isoquinoline	azaarene; isoquinolines; mancude organic heterobicyclic parent; ortho-fused heteroarene		low
cepharanthine	bisbenzylisoquinoline alkaloid; isoquinolines		low
bicuculline	benzylisoquinoline alkaloid; isoquinoline alkaloid; isoquinolines	agrochemical; central nervous system stimulant; GABA-gated chloride channel antagonist; GABAA receptor antagonist; neurotoxin	low
isocarbostyril	isoquinolines		low
salsolidine	isoquinolines		low
laudanosine	isoquinolines		low
1-methylisoquinoline	isoquinolines		low
heliamine	aromatic ether; diether; isoquinoline alkaloid; isoquinolines	plant metabolite	low
1,2-dehydrosalsolinol	isoquinolines		low
dehydroemetine	aromatic ether; isoquinolines; pyridoisoquinoline	antileishmanial agent; antimalarial; antiprotozoal drug	low
metocurine	isoquinolines		low
thalicarpine	bisbenzylisoquinoline alkaloid; isoquinolines		low
dimoxyline	isoquinolines		low
6,7-Dimethoxy-1-methyl-3,4-dihydroisoquinoline	isoquinolines		low
coralyne	isoquinolines		low
(3R)-6,7-dimethoxy-3-[(5R)-4-methoxy-6-methyl-7,8-dihydro-5H-[1,3]dioxolo[4,5-g]isoquinolin-5-yl]-3H-isobenzofuran-1-one	isoquinolines		low
salsoline	isoquinolines		low
isosalsoline	isoquinolines		low
amonafide	isoquinolines		low
daurisoline	isoquinolines		low
magnocurarine	isoquinolines		low
quinapril	dicarboxylic acid monoester; ethyl ester; isoquinolines; tertiary carboxamide	antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug	low
tretoquinol	isoquinolines		low
moxaverine	isoquinolines		low
tritoqualine	isoquinolines		low
tubulosine	beta-carbolines; isoquinoline alkaloid; isoquinolines; phenols; secondary amino compound; tertiary amino compound		low
hernandezine	bisbenzylisoquinoline alkaloid; isoquinolines		low
tetrandrine	bisbenzylisoquinoline alkaloid; isoquinolines		low
dauricine	aromatic ether; bisbenzylisoquinoline alkaloid; isoquinolines; phenols; tertiary amino compound	plant metabolite	low
cherylline	isoquinolines		low
gliquidone	isoquinolines		low
1-methyl-1,2,3,4-tetrahydroisoquinoline	isoquinolines		low
laudanosoline	isoquinolines		low
papaveraldine	isoquinolines		low
corydaline	isoquinoline alkaloid; isoquinolines		low
4-hydroxydebrisoquin	carboxamidine; isoquinolines; secondary alcohol	metabolite	low
quinaprilat	dicarboxylic acid; isoquinolines; tertiary carboxamide	antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; vasodilator agent	low
cycleanine	bisbenzylisoquinoline alkaloid; isoquinolines		low
dihydrotetrabenazine	isoquinolines		low
7,8-dichloro-1,2,3,4-tetrahydroisoquinoline	isoquinolines; organochlorine compound		low
1,2-dimethyl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline	isoquinolines		low
cki 7	isoquinolines; organochlorine compound; primary amino compound; sulfonamide	EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor	low
pixantrone	isoquinolines		low
isodibut	isoquinolines		low
3,4-dihydro-5-methyl-1(2h)-isoquinolinone	isoquinolines		low
solifenacin	isoquinolines		low
liensinine	isoquinolines		low
trilobine	isoquinolines		low
corynoline	benzophenanthridine alkaloid; cyclic acetal; isoquinolines; organic heterohexacyclic compound; secondary alcohol	antineoplastic agent; EC 3.1.1.7 (acetylcholinesterase) inhibitor; hepatoprotective agent; metabolite	low
minalrestat	isoquinolines		low
hydrastine	isoquinolines	metabolite	low
pronuciferine	aromatic ether; cyclic ketone; isoquinoline alkaloid; isoquinolines; organic heterotetracyclic compound	plant metabolite	low
5,6-dimethyl-2-(4-fluorophenylamino)-4-(1-methyl-1,2,3,4-tetrahydroisoquinolin-2-yl)pyrimidine	isoquinolines		low
solifenacin succinate	isoquinolines		low
berbamine	bisbenzylisoquinoline alkaloid; isoquinolines		low
2-(2-oxolanylmethyl)benzo[de]isoquinoline-1,3-dione	isoquinolines		low
guatteguamerine	bisbenzylisoquinoline alkaloid; isoquinolines		low
korupensamine-b	isoquinolines; naphthalenes		low
obamegine	bisbenzylisoquinoline alkaloid; isoquinolines		low
hydrastine hydrochloride, (s-(r,s))-isomer	isoquinolines		low
narcotoline	isoquinolines		low
oxyacanthine	bisbenzylisoquinoline alkaloid; isoquinolines; macrocycle; phenols; tertiary amino compound		low
floxacillin	isoquinolines		low
dioncophylline a	biaryl; isoquinoline alkaloid; isoquinolines; methoxynaphthalene; methylnaphthalenes; naphthalenes	antifungal agent; antimalarial; metabolite; molluscicide	low
dioncophylline c	aromatic ether; biaryl; isoquinoline alkaloid; isoquinolines; methoxynaphthalene; methylnaphthalenes; naphthols	antimalarial; antiplasmodial drug; metabolite	low
h 1152	isoquinolines; N-sulfonyldiazepane	EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor	low
9,10-dimethoxy-2,4,6,7-tetrahydro-[1,3]oxazino[4,3-a]isoquinoline-1-carbonitrile	isoquinolines		low
hydrastine, (r-(r,s))-isomer	isoquinolines		low
6,7-dimethoxy-N-(4-methylphenyl)sulfonyl-3,4-dihydro-1H-isoquinoline-2-carboxamide	isoquinolines		low
5-(3,4-dihydro-1H-isoquinolin-2-yl)-2-(2-furanyl)-4-oxazolecarbonitrile	isoquinolines		low
1-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-2-phenyl-1-butanone	isoquinolines		low
methyl isoquinoline-3-carboxylate	isoquinolines		low
1-(3,4-dihydro-1H-isoquinolin-2-yl)-2-(2-fluorophenoxy)ethanone	isoquinolines		low
1-spiro[2,4-dihydroisoquinoline-3,1'-cyclohexane]thione	isoquinolines		low
N-(4-methoxyphenyl)-3,4-dihydro-1H-isoquinoline-2-carbothioamide	isoquinolines		low
N-(4-fluorophenyl)-3,4-dihydro-1H-isoquinoline-2-carboxamide	isoquinolines		low
3-amino-2-(4-methoxyphenyl)-7-nitro-1-oxo-4-isoquinolinecarbonitrile	isoquinolines		low
4-(3,4-dihydro-1H-isoquinolin-2-ylmethyl)-N-(2,6-dimethylphenyl)benzamide	isoquinolines		low
LSM-16526	isoquinolines		low
drotaverin	isoquinolines		low
5,5-diethyl-1-[oxo(1-piperidinyl)methyl]-6H-pyrrolo[2,1-a]isoquinoline-2,3-dione	isoquinolines		low
N-(4-fluorophenyl)-2-(5-methoxy-1-oxo-2-isoquinolinyl)acetamide	isoquinolines		low
2-[[1-oxo-2-[2-oxo-2-(1-piperidinyl)ethyl]-5-isoquinolinyl]oxy]acetic acid ethyl ester	isoquinolines		low
2-[[2-[2-(2,3-dihydroindol-1-yl)-2-oxoethyl]-1-oxo-5-isoquinolinyl]oxy]acetic acid ethyl ester	isoquinolines		low
5-[[2-[(3-methylphenyl)methyl]-1-oxo-3,4-dihydroisoquinolin-5-yl]oxymethyl]-2-furancarboxylic acid methyl ester	isoquinolines		low
5-[2-(3,4-dihydro-2H-quinolin-1-yl)-2-oxoethoxy]-2-[(3-methylphenyl)methyl]-3,4-dihydroisoquinolin-1-one	isoquinolines		low
4-(3,4-dihydro-1H-isoquinolin-2-ylmethyl)-N-[4-(1-pyrrolidinylsulfonyl)phenyl]benzamide	isoquinolines		low
4-(3,4-dihydro-1H-isoquinolin-2-ylmethyl)-N-[4-(1-piperidinylsulfonyl)phenyl]benzamide	isoquinolines		low
1-(5-isoquinolinyl)-3-(2-phenylethyl)thiourea	isoquinolines		low
1-(4-ethoxyphenyl)-3-(5-isoquinolinyl)thiourea	isoquinolines		low
4-[[5-(difluoromethylthio)-4-methyl-1,2,4-triazol-3-yl]methoxy]-5-methylisoquinoline	isoquinolines		low
2-[[2-(3,4-dihydro-1H-isoquinolin-2-yl)-2-oxoethyl]thio]-3-ethyl-5,6-dimethyl-4-thieno[2,3-d]pyrimidinone	isoquinolines		low
N-[6-amino-2,4-dioxo-1-(phenylmethyl)-5-pyrimidinyl]-2-(3,4-dihydro-1H-isoquinolin-2-yl)-N-(2-methoxyethyl)acetamide	isoquinolines		low
2-(Methylamino)-2,3-dihydro-1H-benzo[de]isoquinoline-1,3-dione	isoquinolines		low
3-[3-(1,3-dioxo-2-benzo[de]isoquinolinyl)propylthio]propanoic acid	isoquinolines		low
4-(1,3-dioxo-2-benzo[de]isoquinolinyl)-N-(1,1-dioxo-3-thiolanyl)butanamide	isoquinolines		low
2-[4-(3,4-dihydro-1H-isoquinolin-2-yl)-4-oxobutyl]benzo[de]isoquinoline-1,3-dione	isoquinolines		low
4-bromobenzenesulfonic acid (1,3-dioxo-2-benzo[de]isoquinolinyl) ester	isoquinolines		low
2-(3-hydroxyphenyl)-6-(1-piperidinyl)benzo[de]isoquinoline-1,3-dione	isoquinolines		low
2-[3-(1H-1,2,4-triazol-5-ylthio)propyl]benzo[de]isoquinoline-1,3-dione	isoquinolines		low
2-[2-[4-[2-hydroxy-3-(2-methylphenoxy)propyl]-1-piperazinyl]ethyl]benzo[de]isoquinoline-1,3-dione	isoquinolines		low
2-benzoyl-N-(6-methoxy-3-pyridinyl)-3,4-dihydro-1H-isoquinoline-3-carboxamide	isoquinolines		low
mcn 5652	isoquinolines		low
3-(3,4-dimethoxyphenyl)-6,7-dimethoxy-2-methyl-N-(6-methyl-2-pyridinyl)-1-oxo-3,4-dihydroisoquinoline-4-carboxamide	isoquinolines		low
4-[(4-cyclohexyl-1-piperazinyl)-oxomethyl]-2-ethyl-6,7-dimethoxy-1-isoquinolinone	isoquinolines		low
1-[[1-(2-methoxyanilino)-4-isoquinolinyl]-oxomethyl]-4-piperidinecarboxamide	isoquinolines		low
3,4-dihydro-1H-isoquinolin-2-yl-(1-ethylsulfonyl-4-piperidinyl)methanone	isoquinolines		low
1-cyclopentyl-N-[2-(3,4-dihydro-1H-isoquinolin-2-yl)ethyl]-5-oxo-3-pyrrolidinecarboxamide	isoquinolines		low
3-(3,4-dimethoxyphenyl)-2-methyl-N-[2-(4-morpholinyl)ethyl]-1-oxo-3,4-dihydroisoquinoline-4-carboxamide	isoquinolines		low
1-[2-(3,4-dihydro-1H-isoquinolin-2-yl)ethyl]-3-(4-ethylphenyl)urea	isoquinolines		low
6,7-dimethoxy-N-[(5-methyl-2-furanyl)methyl]-2-(2-methylpropyl)-1-oxo-4-isoquinolinecarboxamide	isoquinolines		low
4-[[4-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-7-methyl-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidin-2-yl]methyl]morpholine	isoquinolines		low
5-[3,4-dihydro-1H-isoquinolin-2-yl(phenyl)methyl]-6-thiazolo[3,2-b][1,2,4]triazolol	isoquinolines		low
4-chloro-N-[1-(3,4-dihydro-1H-isoquinolin-2-yl)-2-methylpropan-2-yl]benzenesulfonamide	isoquinolines		low
5-[2-[3-(4-fluorophenyl)-5-thiophen-2-yl-3,4-dihydropyrazol-2-yl]-2-oxoethoxy]-2-(phenylmethyl)-3,4-dihydroisoquinolin-1-one	isoquinolines		low
2-[[2-[2-(2,3-dihydro-1,4-benzodioxin-6-ylamino)-2-oxoethyl]-1-oxo-5-isoquinolinyl]oxy]propanoic acid ethyl ester	isoquinolines		low
N-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-(4-fluorophenyl)-2-(2-methoxyethyl)-1-oxo-3,4-dihydroisoquinoline-4-carboxamide	isoquinolines		low
2-[[2-[2-(4-methoxyanilino)-2-oxoethyl]-1-oxo-5-isoquinolinyl]oxy]propanoic acid ethyl ester	isoquinolines		low
2-(4-chlorophenyl)sulfonyl-3,4-dihydro-1H-isoquinoline-3-carboxylic acid	isoquinolines		low
4-phenyl-1,2,3,4-tetrahydroisoquinoline	isoquinolines		low
6,7-dimethoxy-N-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxamide	isoquinolines		low
8-nitro-5-[3-(trifluoromethyl)-1-piperidinyl]isoquinoline	isoquinolines		low
2-(3-methyl-1-oxo-2-isoquinolinyl)-N-(3,4,5-trimethoxyphenyl)acetamide	isoquinolines		low
8-hydroxymanzamine a	alkaloid; beta-carbolines; isoquinolines	anti-HSV-2 agent; EC 2.7.11.26 (tau-protein kinase) inhibitor; metabolite	low
isoliensinine	isoquinolines		low
mivacurium	isoquinolines		low
bw b1090u	isoquinolines		low
3,4-dihydro-1H-isoquinolin-2-yl-(4-ethyl-5-thieno[3,2-b]pyrrolyl)methanone	isoquinolines		low
papaveroline	isoquinolines		low
norbinaltorphimine	isoquinolines		low
naltrindole	isoquinolines		low
manzamine a	alkaloid; beta-carbolines; isoquinolines	animal metabolite; anti-HSV-1 agent; antimalarial; antineoplastic agent; EC 2.7.11.26 (tau-protein kinase) inhibitor; marine metabolite	low
2-(2-phenylethyl)benzo[de]isoquinoline-1,3-dione	isoquinolines		low
ripasudil	isoquinolines		low
ancistroealaine a	aromatic ether; biaryl; isoquinoline alkaloid; isoquinolines; methoxynaphthalene; methylnaphthalenes	antileishmanial agent; antiplasmodial drug; metabolite; trypanocidal drug	low
SIS3 free base	aromatic ether; enamide; isoquinolines; monocarboxylic acid amide; pyrrolopyridine; tertiary carboxamide	Smad3 inhibitor	low
sar 1118	1-benzofurans; isoquinolines; L-phenylalanine derivative; N-acyl-L-alpha-amino acid; sulfone	anti-inflammatory drug; lymphocyte function-associated antigen-1 antagonist	low
4-(4-chlorophenyl)sulfonyl-5-(3,4-dihydro-1H-isoquinolin-2-yl)-2-ethylsulfonylthiazole	isoquinolines		low
bebeerine	bisbenzylisoquinoline alkaloid; isoquinolines		low
(1S)-1-[(3-hydroxy-4-methoxyphenyl)methyl]-6-methoxy-2-methyl-2-oxido-3,4-dihydro-1H-isoquinolin-2-ium-7-ol	isoquinolines; tertiary amine oxide		low
dihydrotetrabenazine, (2alpha,3beta,11bbeta)-isomer	isoquinolines		low
jorunnamycin a	isoquinolines		low
1-[2-(3,4-dihydro-1H-isoquinolin-2-yl)ethyl]-3-(4-nitrophenyl)urea	isoquinolines		low
2-(1,3-benzodioxol-5-ylmethyl)-6,7-dimethoxy-1-methyl-3,4-dihydro-1H-isoquinoline	isoquinolines		low
N-(3-nitrophenyl)-3,4-dihydro-1H-isoquinoline-2-carboxamide	isoquinolines		low
2-(5-butoxy-1-oxo-2-isoquinolinyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)acetamide	isoquinolines		low
almorexant	isoquinolines		low
ipi-145	isoquinolines		low
nbi 31772	aromatic ketone; benzenediols; hydroxy monocarboxylic acid; isoquinolines; tetrol	insulin-like growth factor-binding protein inhibitor	low
quinacrine	acridines; aromatic ether; organochlorine compound; tertiary amino compound	antimalarial; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor	low
vanilmandelic acid	2-hydroxy monocarboxylic acid; aromatic ether; phenols	human metabolite	low
4-(2,4-dichlorophenoxy)butyric acid	aromatic ether; monocarboxylic acid; organochlorine compound	agrochemical; phenoxy herbicide; synthetic auxin	low
win 52035	aromatic ether		low
win 52084	aromatic ether		low
5-(nonyloxy)tryptamine	aromatic ether; primary amino compound; tryptamines	serotonergic agonist	low
methylbufotenin	aromatic ether; tertiary amino compound; tryptamine alkaloid	hallucinogen; plant metabolite	low
5-methoxytryptamine	aromatic ether; primary amino compound; tryptamines	5-hydroxytryptamine 2A receptor agonist; 5-hydroxytryptamine 2B receptor agonist; 5-hydroxytryptamine 2C receptor agonist; antioxidant; cardioprotective agent; human metabolite; mouse metabolite; neuroprotective agent; radiation protective agent; serotonergic agonist	low
ro 48-8071	aromatic ether; aromatic ketone; bromobenzenes; monofluorobenzenes; olefinic compound; tertiary amino compound	antineoplastic agent; EC 5.4.99.7 (lanosterol synthase) inhibitor	low
rtki cpd	aromatic ether; monochlorobenzenes; quinazolines	antineoplastic agent; antiviral agent; epidermal growth factor receptor antagonist; geroprotector	low
amsacrine	acridines; aromatic ether; sulfonamide	antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor	low
aristolochic acid i	aristolochic acids; aromatic ether; C-nitro compound; cyclic acetal; monocarboxylic acid; organic heterotetracyclic compound	carcinogenic agent; metabolite; mutagen; nephrotoxin; toxin	low
2,4-dihydroxy-7-methoxy-1,4-benzoxazin-3-one	aromatic ether; benzoxazine; cyclic hydroxamic acid; lactol	allelochemical; plant metabolite	low
bufetolol	aromatic ether		low
bufexamac	aromatic ether; hydroxamic acid	antipyretic; non-narcotic analgesic; non-steroidal anti-inflammatory drug	low
bunitrolol	aromatic ether		low
bupranolol	aromatic ether		low
verapamil	aromatic ether; nitrile; polyether; tertiary amino compound		low
cgp 12177	aromatic ether; benzimidazoles; secondary alcohol; secondary amino compound	beta-adrenergic antagonist	low
ciglitazone	aromatic ether; thiazolidinone	antineoplastic agent; insulin-sensitizing drug	low
cirazoline	aromatic ether		low
clofibrate	aromatic ether; ethyl ester; monochlorobenzenes	anticholesteremic drug; antilipemic drug; geroprotector; PPARalpha agonist	low
clofibric acid	aromatic ether; monocarboxylic acid; monochlorobenzenes	anticholesteremic drug; antilipemic drug; antineoplastic agent; herbicide; marine xenobiotic metabolite; PPARalpha agonist	low
colchicine, (+-)-isomer	acetamides; alkaloid; aromatic ether; carbotricyclic compound	microtubule-destabilising agent; plant metabolite	low
croconazole	aromatic ether; conazole antifungal drug; imidazole antifungal drug; monochlorobenzenes		low
cypermethrin	aromatic ether; cyclopropanecarboxylate ester; nitrile; organochlorine compound	agrochemical; molluscicide; pyrethroid ester acaricide; pyrethroid ester insecticide	low
racemethorphan	aromatic ether; morphinane alkaloid; morphinane-like compound; organic heterotetracyclic compound		low
dibucaine	aromatic ether; monocarboxylic acid amide; tertiary amino compound	topical anaesthetic	low
dilacor xr	acetate ester; aromatic ether; benzothiazepine; lactam; tertiary amino compound		low
domiphen	aromatic ether		low
donepezil	aromatic ether; indanones; piperidines; racemate	EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; nootropic agent	low
epirizole	aromatic ether		low
ethacrynic acid	aromatic ether; aromatic ketone; dichlorobenzene; monocarboxylic acid	EC 2.5.1.18 (glutathione transferase) inhibitor; ion transport inhibitor; loop diuretic	low
ethoxyquin	aromatic ether; quinolines	antifungal agrochemical; food antioxidant; genotoxin; geroprotector; herbicide; Hsp90 inhibitor; neuroprotective agent; UDP-glucuronosyltransferase activator	low
ethoxzolamide	aromatic ether; benzothiazoles; sulfonamide	antiglaucoma drug; diuretic; EC 4.2.1.1 (carbonic anhydrase) inhibitor	low
2-hexyloxybenzamide	aromatic ether; benzamides	antifungal agent	low
carbonyl cyanide p-trifluoromethoxyphenylhydrazone	aromatic ether; hydrazone; nitrile; organofluorine compound	ATP synthase inhibitor; geroprotector; ionophore	low
fenofibrate	aromatic ether; chlorobenzophenone; isopropyl ester; monochlorobenzenes	antilipemic drug; environmental contaminant; geroprotector; xenobiotic	low
fenvalerate	aromatic ether; carboxylic ester; monochlorobenzenes	pyrethroid ester acaricide; pyrethroid ester insecticide	low
flecainide	aromatic ether; monocarboxylic acid amide; organofluorine compound; piperidines	anti-arrhythmia drug	low
fluoxetine	(trifluoromethyl)benzenes; aromatic ether; secondary amino compound		low
gallamine triethiodide	aromatic ether		low
gemfibrozil	aromatic ether	antilipemic drug	low
haloprogin	aromatic ether		low
indomethacin	aromatic ether; indole-3-acetic acids; monochlorobenzenes; N-acylindole	analgesic; drug metabolite; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; gout suppressant; non-steroidal anti-inflammatory drug; xenobiotic metabolite; xenobiotic	low
ipriflavone	aromatic ether; isoflavones	bone density conservation agent	low
ly 171883	acetophenones; aromatic ether; phenols; tetrazoles	anti-asthmatic drug; leukotriene antagonist	low
mephenesin	aromatic ether; glycerol ether		low
methocarbamol	aromatic ether; carbamate ester; secondary alcohol		low
methoctramine	aromatic ether; tetramine	muscarinic antagonist	low
methoxsalen	aromatic ether; psoralens	antineoplastic agent; cross-linking reagent; dermatologic drug; photosensitizing agent; plant metabolite	low
metoprolol	aromatic ether; propanolamine; secondary alcohol; secondary amino compound	antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; geroprotector; xenobiotic	low
mexiletine	aromatic ether; primary amino compound	anti-arrhythmia drug	low
midodrine	amino acid amide; aromatic ether; secondary alcohol	alpha-adrenergic agonist; prodrug; sympathomimetic agent; vasoconstrictor agent	low
clorgyline	aromatic ether; dichlorobenzene; terminal acetylenic compound; tertiary amino compound	antidepressant; EC 1.4.3.4 (monoamine oxidase) inhibitor	low
nefazodone	aromatic ether; monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; triazoles	alpha-adrenergic antagonist; analgesic; antidepressant; serotonergic antagonist; serotonin uptake inhibitor	low
nimesulide	aromatic ether; C-nitro compound; sulfonamide	cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug	low
nisoxetine	aromatic ether; secondary amino compound	adrenergic uptake inhibitor; antidepressant	low
n-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide	aromatic ether; C-nitro compound; sulfonamide	antineoplastic agent; cyclooxygenase 2 inhibitor	low
omeprazole	aromatic ether; benzimidazoles; pyridines; sulfoxide		low
oxprenolol	aromatic ether		low
pantoprazole	aromatic ether; benzimidazoles; organofluorine compound; pyridines; sulfoxide	anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor; environmental contaminant; xenobiotic	low
pd 153035	aromatic amine; aromatic ether; bromobenzenes; quinazolines; secondary amino compound	EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; epidermal growth factor receptor antagonist	low
pentamidine	aromatic ether; carboxamidine; diether	anti-inflammatory agent; antifungal agent; calmodulin antagonist; chemokine receptor 5 antagonist; EC 2.3.1.48 (histone acetyltransferase) inhibitor; NMDA receptor antagonist; S100 calcium-binding protein B inhibitor; trypanocidal drug; xenobiotic	low
phenacetin	acetamides; aromatic ether	cyclooxygenase 3 inhibitor; non-narcotic analgesic; peripheral nervous system drug	low
pioglitazone	aromatic ether; pyridines; thiazolidinediones	antidepressant; cardioprotective agent; EC 2.7.1.33 (pantothenate kinase) inhibitor; EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; geroprotector; hypoglycemic agent; insulin-sensitizing drug; PPARgamma agonist; xenobiotic	low
piretanide	aromatic ether		low
pramoxine	aromatic ether; morpholines	local anaesthetic	low
prazosin	aromatic ether; furans; monocarboxylic acid amide; piperazines; quinazolines	alpha-adrenergic antagonist; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor	low
primaquine	aminoquinoline; aromatic ether; N-substituted diamine	antimalarial	low
proglumetacin	aromatic ether; benzamides; carboxylic ester; monochlorobenzenes; N-acylindole; N-alkylpiperazine	antipyretic; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; lipoxygenase inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug	low
propoxur	aromatic ether; carbamate ester	acaricide; agrochemical; carbamate insecticide; EC 3.1.1.7 (acetylcholinesterase) inhibitor	low
pyrilamine	aromatic ether; ethylenediamine derivative	H1-receptor antagonist	low
sulfadimethoxine	aromatic ether; pyrimidines; substituted aniline; sulfonamide antibiotic; sulfonamide	antiinfective agent; antimicrobial agent; drug allergen; environmental contaminant; xenobiotic	low
tetrahydropapaverine	aromatic ether; benzylisoquinoline alkaloid; benzyltetrahydroisoquinoline; polyether; secondary amino compound		low
tilorone	aromatic ether; diether; fluoren-9-ones; tertiary amino compound	anti-inflammatory agent; antineoplastic agent; antiviral agent; interferon inducer; nicotinic acetylcholine receptor agonist	low
ultram	aromatic ether; tertiary alcohol; tertiary amino compound		low
triclosan	aromatic ether; dichlorobenzene; monochlorobenzenes; phenols	antibacterial agent; antimalarial; drug allergen; EC 1.3.1.9 [enoyl-[acyl-carrier-protein] reductase (NADH)] inhibitor; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; fungicide; persistent organic pollutant; xenobiotic	low
viloxazine	aromatic ether		low
wb 4101	aromatic ether; benzodioxine; secondary amino compound	alpha-adrenergic antagonist	low
3,3',5-triiodothyropropionic acid	aromatic ether		low
methacetin	acetamides; aromatic ether		low
mestranol	17beta-hydroxy steroid; aromatic ether; terminal acetylenic compound	prodrug; xenoestrogen	low
visnagin	aromatic ether; furanochromone; polyketide	anti-inflammatory agent; antihypertensive agent; EC 1.1.1.37 (malate dehydrogenase) inhibitor; phytotoxin; plant metabolite; vasodilator agent	low
2-tert-butyl-4-hydroxyanisole	aromatic ether; phenols		low
mecoprop	aromatic ether; monocarboxylic acid; monochlorobenzenes		low
phenetidine	aromatic ether; substituted aniline		low
2-methyl-4-chlorophenoxy gamma-butyric acid	aromatic ether; monocarboxylic acid; monochlorobenzenes	environmental contaminant; phenoxy herbicide; xenobiotic	low
4-bromophenyl phenyl ether	aromatic ether; organobromine compound		low
di-(4-aminophenyl)ether	aromatic ether		low
phenyl ether	aromatic ether	plant metabolite	low
diglycidyl resorcinol ether	aromatic ether		low
phenetole	aromatic ether		low
scoparone	aromatic ether; coumarins	anti-allergic agent; anti-inflammatory agent; antihypertensive agent; antilipemic drug; immunosuppressive agent; plant metabolite	low
dimethoxyphenylethylamine	alkaloid; aromatic ether; phenylethylamine	allergen; plant metabolite	low
dichlorprop	aromatic ether; dichlorobenzene; monocarboxylic acid		low
3-tert-butyl-4-hydroxyanisole	aromatic ether; phenols	antioxidant; human xenobiotic metabolite	low
ethyl vanillin	aromatic ether; benzaldehydes; phenols	antioxidant; flavouring agent	low
benzethonium chloride	aromatic ether; chloride salt; quaternary ammonium salt	antibacterial agent; antifungal agent; antiseptic drug; antiviral agent; disinfectant	low
peucedanin	aromatic ether; furanocoumarin; lactone	plant metabolite	low
phenetidine	aromatic ether; primary amino compound; substituted aniline	drug metabolite	low
6-methoxybenzoxazolinone	aromatic ether; benzoxazole	antibacterial agent; anticonvulsant; antifungal agent; muscle relaxant; plant metabolite	low
3-anisidine	aromatic ether; substituted aniline		low
domiphen bromide	aromatic ether		low
dibrompropamidine	aromatic ether		low
4-Ethoxyphenol	aromatic ether; phenols		low
bulbocapnine	aporphine alkaloid; aromatic ether; oxacycle; phenols	EC 1.14.16.2 (tyrosine 3-monooxygenase) inhibitor; EC 1.4.3.22 (diamine oxidase) inhibitor; plant metabolite	low
benzydamine	aromatic ether; indazoles; tertiary amino compound	analgesic; central nervous system stimulant; hallucinogen; local anaesthetic; non-steroidal anti-inflammatory drug	low
xylocholine	aromatic ether		low
3-methoxycatechol	aromatic ether; catechols	G-protein-coupled receptor agonist	low
2-phenoxypropanoic acid	aromatic ether; carboxylic acid		low
6-methoxyquinoline	aromatic ether; quinolines		low
metaxalone	aromatic ether		low
2,4,6-trichlorophenyl 4-nitrophenyl ether	aromatic ether; C-nitro compound; chlorobenzenes	EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor; herbicide	low
etridiazol	aromatic ether; organochlorine compound; thiadiazole antifungal agent; thiadiazoles	antifungal agrochemical; nitrification inhibitor	low
toliprolol	aromatic ether		low
5-methoxyindoleacetic acid	aromatic ether; indole-3-acetic acids	antibacterial agent; Brassica napus metabolite; carcinogenic agent; human urinary metabolite; marine xenobiotic metabolite; rat metabolite	low
iproclozide	aromatic ether		low
phenoxyacetic acid	aromatic ether; monocarboxylic acid	allergen; Aspergillus metabolite; human xenobiotic metabolite; plant growth retardant	low
nafenopin	aromatic ether; monocarboxylic acid		low
methyl vanillate	aromatic ether; benzoate ester; phenols	antioxidant; plant metabolite	low
5-methoxyindole-2-carboxylic acid	aromatic ether; indolecarboxylic acid	EC 1.8.1.4 (dihydrolipoyl dehydrogenase) inhibitor; hypoglycemic agent; plant metabolite	low
2-isopropoxyphenol	aromatic ether; phenols		low
1,2-epoxy-3-(p-nitrophenoxy)propane	aromatic ether; C-nitro compound; epoxide		low
laurolitsine	aporphine alkaloid; aromatic ether; phenols	HIV-1 integrase inhibitor; metabolite	low
metocurine iodide	aromatic ether		low
ac 45594	aromatic ether		low
3-phenoxybenzylalcohol	aromatic ether; benzyl alcohols	marine xenobiotic metabolite	low
devrinol	aromatic ether; monocarboxylic acid amide; naphthalenes		low
fluorodifen	aromatic ether		low
acridine half-mustard	aminoacridines; aromatic ether; organochlorine compound; secondary amino compound	mutagen	low
precocene i	aromatic ether; chromenes	plant metabolite; precocenes	low
oxadiazon	aromatic ether		low
lofexidine	aromatic ether; carboxamidine; dichlorobenzene; imidazoles	alpha-adrenergic agonist; antihypertensive agent	low
alclofenac	aromatic ether; monocarboxylic acid; monochlorobenzenes	drug allergen; non-narcotic analgesic; non-steroidal anti-inflammatory drug	low
phenylglycidyl ether	aromatic ether		low
phenoxyethanol	aromatic ether; glycol ether; primary alcohol	antiinfective agent; central nervous system depressant	low
metipranolol	acetate ester; aromatic ether; propanolamine; secondary amino compound	anti-arrhythmia drug; antiglaucoma drug; antihypertensive agent; beta-adrenergic antagonist	low
silybin	aromatic ether; benzodioxine; flavonolignan; polyphenol; secondary alpha-hydroxy ketone	antineoplastic agent; antioxidant; hepatoprotective agent; plant metabolite	low
oxamethacin	aromatic ether; hydroxamic acid; N-acylindole; organochlorine compound	EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug	low
canadine	aromatic ether; berberine alkaloid; organic heteropentacyclic compound; oxacycle		low
7-ethoxycoumarin	aromatic ether; coumarins		low
medifoxamine	aromatic ether		low
chlormethoxynil	aromatic ether		low
climbazole	aromatic ether; hemiaminal ether; imidazoles; ketone; monochlorobenzenes		low
4-hexyloxyaniline	aromatic ether; substituted aniline		low
ticrynafen	aromatic ether; aromatic ketone; dichlorobenzene; monocarboxylic acid; thiophenes	antihypertensive agent; hepatotoxic agent; loop diuretic	low
2-(4-(2,4-dichlorophenoxy)phenoxy)propionic acid	aromatic ether; dichlorobenzene; diether; monocarboxylic acid		low
bezafibrate	aromatic ether; monocarboxylic acid amide; monocarboxylic acid; monochlorobenzenes	antilipemic drug; environmental contaminant; geroprotector; xenobiotic	low
oxyfluorofen	aromatic ether	EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor; herbicide	low
triadimefon	aromatic ether; hemiaminal ether; ketone; monochlorobenzenes; triazoles		low
levobunolol	aromatic ether; cyclic ketone; propanolamine	antiglaucoma drug; beta-adrenergic antagonist	low
dichlorfop-methyl	aromatic ether; dichlorobenzene; diether; methyl ester		low
decamethrin	aromatic ether; cyclopropanecarboxylate ester; nitrile; organobromine compound	agrochemical; antifeedant; calcium channel agonist; EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor; pyrethroid ester insecticide	low
triadimenol	aromatic ether; conazole fungicide; hemiaminal ether; monochlorobenzenes; secondary alcohol; triazole fungicide	antifungal agrochemical; EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor; xenobiotic metabolite	low
triclopyr	aromatic ether; chloropyridine; monocarboxylic acid	agrochemical; environmental contaminant; herbicide; xenobiotic	low
prenalterol	aromatic ether		low
st 1059	aromatic ether; primary amino compound; secondary alcohol	alpha-adrenergic agonist; sympathomimetic agent; vasoconstrictor agent	low
paroxetine	aromatic ether; benzodioxoles; organofluorine compound; piperidines	antidepressant; anxiolytic drug; hepatotoxic agent; P450 inhibitor; serotonin uptake inhibitor	low
acifluorfen	aromatic ether; benzoic acids; C-nitro compound; monocarboxylic acid; organochlorine compound; organofluorine compound	agrochemical; EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor; herbicide	low
bopindolol	aromatic ether; benzoate ester; methylindole; secondary amino compound		low
fenpropathrin, (+-)-isomer	aromatic ether; cyclopropanecarboxylate ester	agrochemical; pyrethroid ester acaricide; pyrethroid ester insecticide	low
triflumuron	aromatic ether; benzoylurea insecticide; monochlorobenzenes; organofluorine compound		low
flutolanil	(trifluoromethyl)benzenes; aromatic ether; benzamides; benzanilide fungicide	antifungal agrochemical; EC 1.3.5.1 [succinate dehydrogenase (quinone)] inhibitor	low
fenoxaprop ethyl	aromatic ether		low
triclabendazole	aromatic ether		low
4,5-amino-3,5-dichloro-6-fluoro-2-pyridinyloxyacetic acid	aminopyridine; aromatic ether; monocarboxylic acid; organochlorine compound; organofluorine compound	environmental contaminant; herbicide; xenobiotic	low
fluvalinate	(trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; nitrile; organochlorine acaricide; organochlorine insecticide; organofluorine acaricide; organofluorine insecticide	agrochemical; pyrethroid ester acaricide; pyrethroid ester insecticide	low
haloxyfop	aromatic ether; monocarboxylic acid; organochlorine compound; organofluorine compound; pyridines		low
fluazifop-butyl	aromatic ether; carboxylic ester; organofluorine compound; pyridines		low
fomesafen	aromatic ether; C-nitro compound; monochlorobenzenes; N-sulfonylcarboxamide; organofluorine compound; phenols	agrochemical; EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor; herbicide	low
fenoxycarb	aromatic ether; carbamate ester	environmental contaminant; insecticide; juvenile hormone mimic; xenobiotic	low
quizalofop-ethyl	aromatic ether; ethyl ester; organochlorine compound; quinoxaline derivative		low
cetamolol	aromatic ether		low
atomoxetine	aromatic ether; secondary amino compound; toluenes	adrenergic uptake inhibitor; antidepressant; environmental contaminant; xenobiotic	low
methyl bensulfuron	aromatic ether; methyl ester; N-sulfonylurea; pyrimidines	agrochemical; EC 2.2.1.6 (acetolactate synthase) inhibitor; herbicide	low
itraconazole	aromatic ether; conazole antifungal drug; cyclic ketal; dichlorobenzene; dioxolane; N-arylpiperazine; triazole antifungal drug; triazoles	EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor; Hedgehog signaling pathway inhibitor; P450 inhibitor	low
loxtidine	aromatic ether; piperidines; primary alcohol; triazoles	H2-receptor antagonist	low
disoxaril	aromatic ether		low
chlorimuron ethyl	aromatic ether; ethyl ester; N-sulfonylurea; organochlorine pesticide; pyrimidines; sulfamoylbenzoate	agrochemical; EC 2.2.1.6 (acetolactate synthase) inhibitor; proherbicide	low
tepoxalin	aromatic ether; hydroxamic acid; monochlorobenzenes; pyrazoles	antipyretic; apoptosis inhibitor; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; immunomodulator; lipoxygenase inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug	low
esmolol	aromatic ether; ethanolamines; methyl ester; secondary alcohol; secondary amino compound		low
pioglitazone hydrochloride	aromatic ether		low
aripiprazole	aromatic ether; delta-lactam; dichlorobenzene; N-alkylpiperazine; N-arylpiperazine; quinolone	drug metabolite; H1-receptor antagonist; second generation antipsychotic; serotonergic agonist	low
sulfametrole	aromatic ether; substituted aniline; sulfonamide antibiotic; thiadiazoles		low
propamidine	aromatic ether; guanidines; polyether	antimicrobial agent; antiseptic drug	low
hexamidine	aromatic ether; guanidines; polyether	antimicrobial agent; antiseptic drug	low
o-4-methylthymine	aromatic ether; methylthymine	human metabolite	low
fenclofenac	aromatic ether		low
tetraiodothyroacetic acid	2-halophenol; aromatic ether; iodophenol; monocarboxylic acid	apoptosis inducer; human metabolite; thyroid hormone	low
fluazuron	aromatic ether; chloropyridine; monochlorobenzenes; N-acylurea; organochlorine acaricide; organofluorine acaricide; phenylureas	acaricide; mite growth regulator	low
etiroxate	aromatic ether		low
etofamide	aromatic ether		low
d 888	aromatic ether; nitrile; tertiary amino compound	anti-arrhythmia drug; calcium channel blocker; vasodilator agent	low
esreboxetine	aromatic ether		low
guaethol	aromatic ether; phenols; volatile organic compound	flavouring agent	low
spiramide	aromatic ether; azaspiro compound; organofluorine compound; piperidines; tertiary amino compound	dopaminergic antagonist; serotonergic antagonist	low
5'-nitro-2'-propoxyacetanilide	aromatic ether; C-nitro compound		low
suberosin	aromatic ether; coumarins	anticoagulant; plant metabolite	low
4-methoxyestradiol	17beta-hydroxy steroid; 3-hydroxy steroid; aromatic ether; phenols	estrogen; human metabolite; rat metabolite	low
toltrazuril	aromatic ether		low
plafibride	aromatic ether		low
cinitapride	aromatic ether; C-nitro compound		low
isoscopoletin	aromatic ether; hydroxycoumarin	plant metabolite	low
ethofenprox	aromatic ether	pyrethroid ether insecticide	low
uk 68798	aromatic ether; sulfonamide; tertiary amino compound	anti-arrhythmia drug; potassium channel blocker	low
hp 873	1,2-benzoxazoles; aromatic ether; aromatic ketone; methyl ketone; monoamine; organofluorine compound; piperidines; tertiary amino compound	dopaminergic antagonist; second generation antipsychotic; serotonergic antagonist	low
fenoxypropazine	aromatic ether		low
fluphenacur	aromatic ether; benzoylurea insecticide; dichlorobenzene; N-acylurea; organofluorine compound		low
amezinium	aromatic ether; primary arylamine; pyridazinium ion	adrenergic uptake inhibitor; antihypotensive agent; EC 1.4.3.4 (monoamine oxidase) inhibitor; sympathomimetic agent	low
rubrofusarin	aromatic ether; benzochromenone; phenols; polyketide	biological pigment; EC 1.14.18.1 (tyrosinase) inhibitor; fungal metabolite	low
triasulfuron	1,3,5-triazines; aromatic ether; N-sulfonylurea; organochlorine compound	agrochemical; herbicide	low
uvaretin	aromatic ether; dihydrochalcones; polyketide; resorcinol	antineoplastic agent; plant metabolite	low
fangchinoline	aromatic ether; bisbenzylisoquinoline alkaloid; macrocycle	anti-HIV-1 agent; anti-inflammatory agent; antineoplastic agent; antioxidant; neuroprotective agent; plant metabolite	low
prochloraz	amide fungicide; aromatic ether; conazole fungicide; imidazole fungicide; imidazoles; trichlorobenzene; ureas	antifungal agrochemical; EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor; environmental contaminant; xenobiotic	low
stictic acid	aromatic ether		low
pramoxine hydrochloride	aromatic ether		low
4-methoxybenzylamine	aralkylamino compound; aromatic ether; primary amino compound		low
xanthurenic acid 8-methyl ether	aromatic ether; monohydroxyquinoline; quinolinemonocarboxylic acid	carcinogenic agent; metabolite; mouse metabolite	low
adriamycinol	aminoglycoside; anthracycline antibiotic; aromatic ether; deoxy hexoside; p-quinones; phenols; polyol; tetracenequinones	cardiotoxic agent; drug metabolite	low
difenoconazole	aromatic ether; conazole fungicide; cyclic ketal; dioxolane; triazole fungicide; triazoles	antifungal agrochemical; EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor; environmental contaminant; xenobiotic	low
a 8947	aromatic ether; biaryl; N-sulfonylurea; pyrazole pesticide; tetrazoles	EC 2.2.1.6 (acetolactate synthase) inhibitor; herbicide	low
thifluzamide	1,3-thiazoles; anilide fungicide; aromatic amide; aromatic ether; dibromobenzene; organofluorine compound	antifungal agrochemical; EC 1.3.5.1 [succinate dehydrogenase (quinone)] inhibitor	low
ethylhydrocupreine	aromatic ether; cinchona alkaloid	EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor	low
7,8-dihydromethysticin	2-pyranones; aromatic ether		low
4,5-dimethoxy-2-nitrobenzaldehyde	aromatic ether; C-nitro compound		low
bisphenol f diglycidyl ether	aromatic ether; diarylmethane; epoxide		low
oryzemate	1,2-benzisothiazole; aromatic ether; benzothiazole fungicide; sulfone	antifungal agrochemical; plant activator	low
bitertanol	aromatic ether; biphenyls; secondary alcohol; triazoles		low
fluazifop	aromatic ether; monocarboxylic acid; organofluorine compound; pyridines		low
diflufenican	(trifluoromethyl)benzenes; aromatic ether; pyridinecarboxamide	carotenoid biosynthesis inhibitor; environmental contaminant; herbicide; xenobiotic	low
hexafluoron	aromatic ether; benzoylurea insecticide; dichlorobenzene; N-acylurea; organochlorine insecticide; organofluorine insecticide		low
diethofencarb	aromatic ether; carbamate ester; carbanilate fungicide	antifungal agrochemical	low
pyriproxyfen	aromatic ether; pyridines	juvenile hormone mimic	low
methyl 2-(((((4-ethoxy-6-(methylamino)-1,3,5-triazin-2-yl)amino)carbonyl)amino)sulfonyl)benzoate	aromatic ether; benzoate ester; diamino-1,3,5-triazine; methyl ester; N-sulfonylurea	EC 2.2.1.6 (acetolactate synthase) inhibitor; herbicide	low
dpx e9636	aromatic ether; N-sulfonylurea; pyridines; pyrimidines; sulfone	environmental contaminant; herbicide; xenobiotic	low
aclonifen	aromatic ether; C-nitro compound; monochlorobenzenes; primary amino compound; substituted aniline	agrochemical; carotenoid biosynthesis inhibitor; EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor; herbicide	low
cinosulfuron	aromatic ether		low
clodinafop-propargyl	aromatic ether; carboxylic ester; organochlorine compound; organofluorine compound; propyzamide; pyridines	agrochemical; EC 6.4.1.2 (acetyl-CoA carboxylase) inhibitor; herbicide	low
triflusulfuron-methyl	1,3,5-triazines; aromatic ether; benzoate ester; methyl ester; N-sulfonylurea; organofluorine compound; tertiary amino compound	agrochemical; EC 2.2.1.6 (acetolactate synthase) inhibitor; proherbicide	low
vestitol	aromatic ether; hydroxyisoflavans; methoxyisoflavan	anti-inflammatory agent; phytoalexin; plant metabolite	low
laudanine	aromatic ether; benzylisoquinoline alkaloid; benzyltetrahydroisoquinoline; phenols; racemate		low
cryptopleurine	alkaloid antibiotic; alkaloid; aromatic ether; organic heteropentacyclic compound	antineoplastic agent; antiviral agent; protein synthesis inhibitor	low
6-hydroxymethylmexiletine	aromatic ether		low
4-hydroxymexiletine	aromatic ether; phenols		low
cloquintocet-mexyl	aromatic ether; carboxylic ester; organochlorine compound; quinolines		low
novaluron	aromatic ether; benzoylurea insecticide; monochlorobenzenes; organofluorine compound		low
bursehernin	aromatic ether; benzodioxoles; butan-4-olide; lignan	plant metabolite	low
2,2',4,4'-tetrabromodiphenyl ether	aromatic ether; organobromine compound		low
allocryptopine	aromatic ether; cyclic acetal; cyclic ketone; dibenzazecine alkaloid; organic heterotetracyclic compound; tertiary amino compound		low
sporidesmin	aromatic ether; cyclic ketone; diketone; organic disulfide; organic heteropentacyclic compound; organochlorine compound; secondary alcohol; tertiary alcohol; tertiary amino compound	mycotoxin; Wnt signalling activator	low
syringaresinol	aromatic ether; furofuran; lignan; polyether; polyphenol	plant metabolite	low
p-methoxy-n-methylphenethylamine	aromatic ether; secondary amino compound	metabolite	low
aflatoxin q1	aflatoxin; aromatic ether; aromatic ketone	carcinogenic agent; human xenobiotic metabolite	low
u 73122	aromatic ether; aza-steroid; maleimides	EC 3.1.4.11 (phosphoinositide phospholipase C) inhibitor	low
cyfluthrin	aromatic ether; cyclopropanecarboxylate ester; nitrile; organochlorine compound; organofluorine compound	agrochemical; pyrethroid ester insecticide	low
norverapamil	aromatic ether; nitrile; polyether; secondary amino compound		low
fumitremorgin a	aromatic ether; diol; indole alkaloid; organic heterohexacyclic compound; organic peroxide	mycotoxin	low
deguelin	aromatic ether; diether; organic heteropentacyclic compound; rotenones	angiogenesis inhibitor; anti-inflammatory agent; antineoplastic agent; antiviral agent; apoptosis inducer; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; mitochondrial NADH:ubiquinone reductase inhibitor; plant metabolite	low
aristolochic acid ii	aristolochic acids; aromatic ether; C-nitro compound; cyclic acetal; monocarboxylic acid; organic heterotetracyclic compound	carcinogenic agent; metabolite; mutagen; nephrotoxin; toxin	low
tephrosin	aromatic ether; cyclic ketone; organic heteropentacyclic compound; rotenones	antineoplastic agent; metabolite; pesticide	low
alpha-hydroxymetoprolol	aromatic ether		low
5-(tetradecyloxy)-2-furancarboxylic acid	aromatic ether; furoic acid	antineoplastic agent; apoptosis inducer; EC 6.4.1.2 (acetyl-CoA carboxylase) inhibitor; PPARalpha agonist	low
tafenoquine	(trifluoromethyl)benzenes; aminoquinoline; aromatic ether; primary amino compound; secondary amino compound		low
5-hydroxymethylomeprazole	aromatic ether; benzimidazoles; pyridines; sulfoxide	drug metabolite	low
mosapride	aromatic ether; benzamides; monochlorobenzenes; monofluorobenzenes; morpholines; secondary carboxamide; substituted aniline; tertiary amino compound		low
ym 12617	aromatic ether; secondary amino compound; sulfonamide		low
gefitinib	aromatic ether; monochlorobenzenes; monofluorobenzenes; morpholines; quinazolines; secondary amino compound; tertiary amino compound	antineoplastic agent; epidermal growth factor receptor antagonist	low
cgp 28392	aromatic ether		low
sodium-binding benzofuran isophthalate	1-benzofurans; aromatic ether; crown compound; tetracarboxylic acid	fluorochrome	low
garenoxacin	aromatic ether; cyclopropanes; isoindoles; organofluorine compound; quinolinemonocarboxylic acid; quinolone antibiotic	antibacterial drug; non-steroidal anti-inflammatory drug	low
ay 25545	acetate ester; aromatic ether; C-glycosyl compound; naphthoisochromene; olefinic compound; phenols; tertiary amine	antimicrobial agent; antineoplastic agent; bacterial metabolite	low
reboxetine	aromatic ether		low
b 823-08	aromatic ether		low
cyclazosin	aromatic amide; aromatic ether; furans; monocarboxylic acid amide; quinazolines; quinoxaline derivative	adenosine A2A receptor antagonist	low
ivabradine	aromatic ether; benzazepine; carbobicyclic compound; tertiary amino compound	cardiotonic drug	low
febuxostat	1,3-thiazolemonocarboxylic acid; aromatic ether; nitrile	EC 1.17.3.2 (xanthine oxidase) inhibitor	low
marsupsin	1-benzofurans; aromatic ether; polyphenol	antilipemic drug; hypoglycemic agent; metabolite	low
6,6'-bieckol	aromatic ether; oxacycle; phlorotannin	anti-HIV-1 agent; metabolite; radical scavenger	low
xibenolol	aromatic ether		low
cicloprolol	aromatic ether		low
chs 828	aromatic ether		low
2-(4-methoxyphenoxy)propanoic acid	aromatic ether; carboxylic acid		low
moxifloxacin	aromatic ether; cyclopropanes; fluoroquinolone antibiotic; pyrrolidinopiperidine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone	antibacterial drug	low
rp 73401	aromatic ether; benzamides; chloropyridine; monocarboxylic acid amide	anti-asthmatic drug; anti-inflammatory agent; bronchodilator agent; phosphodiesterase IV inhibitor	low
2,2',4,4',5,5'-hexabrominated diphenyl ether	aromatic ether; organobromine compound		low
varespladib	aromatic ether; benzenes; dicarboxylic acid monoamide; indoles; monocarboxylic acid; primary carboxamide	anti-inflammatory drug; antidote; EC 3.1.1.4 (phospholipase A2) inhibitor	low
birb 796	aromatic ether; morpholines; naphthalenes; pyrazoles; ureas	EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; immunomodulator	low
schizandrin b	aromatic ether; cyclic acetal; organic heterotetracyclic compound; oxacycle; tannin	anti-asthmatic agent; anti-inflammatory agent; antilipemic drug; antioxidant; apoptosis inhibitor; hepatoprotective agent; nephroprotective agent; neuroprotective agent; plant metabolite	low
s 23121	aromatic ether; dicarboximide; monochlorobenzenes; monofluorobenzenes; pyrroline; terminal acetylenic compound		low
acrovestone	acetophenones; aromatic ether; olefinic compound; polyphenol	antioxidant; EC 1.14.18.1 (tyrosinase) inhibitor; plant metabolite	low
corytuberine	aporphine alkaloid; aromatic ether; organic heterotetracyclic compound; polyphenol; tertiary amino compound	plant metabolite	low
actinodaphine	aporphine alkaloid; aromatic ether; organic heteropentacyclic compound; phenols; secondary amino compound	antibacterial agent; antifungal agent; antineoplastic agent; apoptosis inducer; plant metabolite; platelet aggregation inhibitor; topoisomerase inhibitor	low
isohomovanillic acid	aromatic ether; phenols; phenylacetic acids	metabolite	low
3,5-diiodothyropropionic acid	aromatic ether; monocarboxylic acid; organoiodine compound; phenols		low
7,8-dihydro-5,6-dehydrokawain	2-pyranones; aromatic ether		low
4-amino-2-methoxypyrimidine	aminopyrimidine; aromatic ether; methylcytosine	metabolite	low
aristolochic acid D	aristolochic acids; aromatic ether; C-nitro compound; cyclic acetal; monocarboxylic acid; organic heterotetracyclic compound	carcinogenic agent; metabolite; nephrotoxin; toxin	low
myricanone	aromatic ether; cyclic ketone; diarylheptanoid; methoxybenzenes; phenols	antineoplastic agent; plant metabolite	low
pannarin	aldehyde; aromatic ether; depsidones; organic heterotricyclic compound; organochlorine compound; phenols	antimicrobial agent; antineoplastic agent; apoptosis inducer; lichen metabolite	low
aminopotentidine	aromatic ether; benzamides; guanidines; nitrile; piperidines; substituted aniline	H2-receptor antagonist	low
aristolochic acid c	aristolochic acids; aromatic ether; C-nitro compound; cyclic acetal; monocarboxylic acid; organic heterotetracyclic compound	carcinogenic agent; metabolite; mutagen; nephrotoxin; toxin	low
pluviatolide	aromatic ether; benzodioxoles; butan-4-olide; lignan; phenols	plant metabolite	low
erysodine	aromatic ether; diether; Erythrina alkaloid; organic heterotetracyclic compound; phenols	antiparasitic agent; nicotinic antagonist; phytogenic insecticide	low
erlotinib	aromatic ether; quinazolines; secondary amino compound; terminal acetylenic compound	antineoplastic agent; epidermal growth factor receptor antagonist; protein kinase inhibitor	low
rubrofusarin B	aromatic ether; benzochromenone; naphtho-gamma-pyrone; phenols; polyketide	Aspergillus metabolite	low
ly 293111	aromatic ether		low
enrasentan	aromatic ether; benzodioxoles; indanes; monocarboxylic acid; monomethoxybenzene; primary alcohol	antihypertensive agent; endothelin receptor antagonist	low
quizalofop	aromatic ether; monocarboxylic acid; organochlorine compound; quinoxaline derivative		low
cyhalofop-butyl	aromatic ether		low
cyperin	aromatic ether		low
aflatoxin b1	aflatoxin; aromatic ether; aromatic ketone	carcinogenic agent; human metabolite	low
etravirine	aminopyrimidine; aromatic ether; dinitrile; organobromine compound	antiviral agent; HIV-1 reverse transcriptase inhibitor	low
5-o-methyllicoricidin	aromatic ether; hydroxyisoflavans; methoxyisoflavan	antibacterial agent; plant metabolite	low
dronedarone	1-benzofurans; aromatic ether; aromatic ketone; sulfonamide; tertiary amino compound	anti-arrhythmia drug; environmental contaminant; xenobiotic	low
famoxadone	aromatic ether; carbohydrazide; oxazolidinone		low
cimicoxib	aromatic ether; imidazoles; organochlorine compound; organofluorine compound; sulfonamide	cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug	low
sorafenib	(trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; phenylureas; pyridinecarboxamide	angiogenesis inhibitor; anticoronaviral agent; antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; ferroptosis inducer; tyrosine kinase inhibitor	low
dabuzalgron	aromatic ether; imidazoles; monochlorobenzenes; sulfonamide	alpha-adrenergic agonist	low
fonsecin	aromatic ether; cyclic hemiketal; heptaketide; naphtho-gamma-pyrone; phenols	Aspergillus metabolite; marine metabolite	low
lasofoxifene	aromatic ether; N-alkylpyrrolidine; naphthols; tetralins	antineoplastic agent; bone density conservation agent; cardioprotective agent; estrogen receptor agonist; estrogen receptor antagonist	low
(+-)-Dihydromethysticin	2-pyranones; aromatic ether		low
2-[2-[2-(2-aminophenoxy)ethoxy]ethoxy]aniline	aromatic ether; substituted aniline		low
chondocurine (1beta)-(+-)-isomer	aromatic ether		low
1-methyl-4-prop-2-enoxy-2-pyrimidinone	aromatic ether; pyrimidone		low
noscapine	aromatic ether; benzylisoquinoline alkaloid; cyclic acetal; isobenzofuranone; organic heterobicyclic compound; organic heterotricyclic compound; tertiary amino compound	antineoplastic agent; antitussive; apoptosis inducer; plant metabolite	low
4-[4-(3-methyl-4-nitrophenoxy)butoxy]benzonitrile	aromatic ether; C-nitro compound		low
lariciresinol	aromatic ether; lignan; oxolanes; phenols; primary alcohol	antifungal agent; plant metabolite	low
tryptoquivaline	aromatic ether; indole alkaloid; organic heteropentacyclic compound	breast cancer resistance protein inhibitor; mycotoxin	low
2-methoxyestrone	17-oxo steroid; 3-hydroxy steroid; alicyclic ketone; aromatic ether; phenolic steroid; phenols	human metabolite; mouse metabolite	low
win 54954	aromatic ether		low

Substance	Classes	Roles	Relationship Strength
protocatechuic acid	catechols; dihydroxybenzoic acid	antineoplastic agent; EC 1.1.1.25 (shikimate dehydrogenase) inhibitor; EC 1.14.11.2 (procollagen-proline dioxygenase) inhibitor; human xenobiotic metabolite; plant metabolite	low
ethyl protocatechuate	catechols; ethyl ester	antibacterial agent; antioxidant; apoptosis inducer; EC 1.14.11.2 (procollagen-proline dioxygenase) inhibitor; plant metabolite	low
dimethyloxalylglycine	glycine derivative; methyl ester; secondary carboxamide	EC 1.14.11.29 (hypoxia-inducible factor-proline dioxygenase) inhibitor; neuroprotective agent	low

Substance	Studies	Classes	Roles	First Year	Last Year	Average Age	Relationship Strength	2010's	post-2020
citric acid, anhydrous	2	tricarboxylic acid	antimicrobial agent; chelator; food acidity regulator; fundamental metabolite	2013	2019	8.0	low	2	0
malic acid	1	2-hydroxydicarboxylic acid; C4-dicarboxylic acid	food acidity regulator; fundamental metabolite	2013	2013	11.0	low	1	0
oxaloacetic acid	1	C4-dicarboxylic acid; oxo dicarboxylic acid	geroprotector; metabolite	2019	2019	5.0	low	1	0
pyruvic acid	2	2-oxo monocarboxylic acid	cofactor; fundamental metabolite	2013	2019	8.0	low	2	0
succinic acid	1	alpha,omega-dicarboxylic acid; C4-dicarboxylic acid	anti-ulcer drug; fundamental metabolite; micronutrient; nutraceutical; radiation protective agent	2019	2019	5.0	low	1	0
amodiaquine	1	aminoquinoline; organochlorine compound; phenols; secondary amino compound; tertiary amino compound	anticoronaviral agent; antimalarial; drug allergen; EC 2.1.1.8 (histamine N-methyltransferase) inhibitor; non-steroidal anti-inflammatory drug; prodrug	2020	2020	4.0	low	1	0
whi p154	1			2020	2020	4.0	low	1	0
whi p97	1	quinazolines		2020	2020	4.0	low	1	0
vorinostat	1	dicarboxylic acid diamide; hydroxamic acid	antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor	2022	2022	2.0	low	0	1
triiodothyronine	1	2-halophenol; amino acid zwitterion; iodophenol; iodothyronine	human metabolite; mouse metabolite; thyroid hormone	2022	2022	2.0	low	0	1
rhein	1	dihydroxyanthraquinone		2013	2013	11.0	low	1	0
2,4-pyridinedicarboxylic acid	2	pyridinedicarboxylic acid		2013	2019	8.0	low	2	0
daminozide	1	straight-chain fatty acid		2019	2019	5.0	low	1	0
d-glutamate	1	D-alpha-amino acid; glutamic acid	Escherichia coli metabolite; mouse metabolite	2013	2013	11.0	low	1	0
glutamic acid	2	glutamic acid; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid	Escherichia coli metabolite; ferroptosis inducer; micronutrient; mouse metabolite; neurotransmitter; nutraceutical	2013	2019	8.0	low	2	0
d-lactic acid	1	2-hydroxypropanoic acid	Escherichia coli metabolite; human metabolite	2013	2013	11.0	low	1	0
d-2-hydroxyglutarate	2	2-hydroxyglutaric acid	algal metabolite	2013	2019	8.0	high	2	0
alpha-hydroxyglutarate, (l)-isomer	2	2-hydroxyglutaric acid		2013	2019	8.0	high	2	0
trichostatin a	1	antibiotic antifungal agent; hydroxamic acid; trichostatin	bacterial metabolite; EC 3.5.1.98 (histone deacetylase) inhibitor; geroprotector	2022	2022	2.0	low	0	1
fumaric acid	2	butenedioic acid	food acidity regulator; fundamental metabolite; geroprotector	2013	2019	8.0	low	2	0
5-carboxy-8-hydroxyquinoline	2	quinolines		2013	2019	8.0	low	2	0
aconitic acid	2	aconitic acid	fundamental metabolite	2013	2019	8.0	high	2	0
oxalylglycine	2	amino dicarboxylic acid; N-acylglycine	EC 1.14.11.* (oxidoreductase acting on paired donors, 2-oxoglutarate as one donor, incorporating 1 atom each of oxygen into both donors) inhibitor	2013	2019	8.0	low	2	0
mgl-3196	1			2022	2022	2.0	low	0	1
sgx 523	1	aryl sulfide; biaryl; pyrazoles; quinolines; triazolopyridazine	c-Met tyrosine kinase inhibitor; nephrotoxic agent	2020	2020	4.0	low	1	0
sgi-1027	1			2020	2020	4.0	low	1	0
baricitinib	1	azetidines; nitrile; pyrazoles; pyrrolopyrimidine; sulfonamide	anti-inflammatory agent; antirheumatic drug; antiviral agent; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; immunosuppressive agent	2020	2020	4.0	low	1	0
jnj 42041935	1			2013	2013	11.0	high	1	0
jnj38877605	1	quinolines		2020	2020	4.0	low	1	0
(5-bromo-3-pyridinyl)-[4-(1-pyrrolidinyl)-1-piperidinyl]methanone	1	aromatic carboxylic acid; pyridinemonocarboxylic acid		2020	2020	4.0	low	1	0
2-[[[4-hydroxy-2-oxo-1-(phenylmethyl)-3-quinolinyl]-oxomethyl]amino]acetic acid	1	quinolines		2019	2019	5.0	low	1	0
3-[[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)-4-pyrimidinyl]amino]propanoic acid	1	organonitrogen heterocyclic compound		2019	2019	5.0	low	1	0
bay 85-3934	3			2015	2019	6.7	low	3	0
sgc707	1			2020	2020	4.0	low	1	0
gsk1278863	1			2018	2018	6.0	low	1	0

Inhibition of a viral prolyl hydroxylase.
Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019

Structural basis for inhibition of the fat mass and obesity associated protein (FTO).
Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013

Structural basis for inhibition of the fat mass and obesity associated protein (FTO).
Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013

Inhibition of a viral prolyl hydroxylase.
Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019

Inhibition of a viral prolyl hydroxylase.
Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019

Structural basis for inhibition of the fat mass and obesity associated protein (FTO).
Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013

Inhibition of a viral prolyl hydroxylase.
Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019

Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
Journal of medicinal chemistry, , 06-25, Volume: 63, Issue:12, 2020

Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist.
Journal of medicinal chemistry, , 05-26, Volume: 65, Issue:10, 2022

Structural basis for inhibition of the fat mass and obesity associated protein (FTO).
Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013

Inhibition of a viral prolyl hydroxylase.
Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019

Structural basis for inhibition of the fat mass and obesity associated protein (FTO).
Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013

Inhibition of a viral prolyl hydroxylase.
Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019

Structural basis for inhibition of the fat mass and obesity associated protein (FTO).
Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013

Inhibition of a viral prolyl hydroxylase.
Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019

Structural basis for inhibition of the fat mass and obesity associated protein (FTO).
Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013

Structural basis for inhibition of the fat mass and obesity associated protein (FTO).
Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013

Inhibition of a viral prolyl hydroxylase.
Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019

Structural basis for inhibition of the fat mass and obesity associated protein (FTO).
Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013

Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist.
Journal of medicinal chemistry, , 05-26, Volume: 65, Issue:10, 2022

Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
Journal of medicinal chemistry, , 06-25, Volume: 63, Issue:12, 2020

Inhibition of hypoxia-inducible factor prolyl hydroxylase domain oxygen sensors: tricking the body into mounting orchestrated survival and repair responses.
Journal of medicinal chemistry, , Dec-12, Volume: 56, Issue:23, 2013

Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
Journal of medicinal chemistry, , 06-25, Volume: 63, Issue:12, 2020

Inhibition of a viral prolyl hydroxylase.
Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019

Inhibition of a viral prolyl hydroxylase.
Bioorganic & medicinal chemistry, , 06-15, Volume: 27, Issue:12, 2019

Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
Journal of medicinal chemistry, , 08-23, Volume: 61, Issue:16, 2018

Affinity-Based Fluorescence Polarization Assay for High-Throughput Screening of Prolyl Hydroxylase 2 Inhibitors.
ACS medicinal chemistry letters, , Dec-10, Volume: 6, Issue:12, 2015

Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
Journal of medicinal chemistry, , 06-25, Volume: 63, Issue:12, 2020

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.
Bioorganic & medicinal chemistry letters, , 06-01, Volume: 28, Issue:10, 2018

Substance	Studies	Classes	Roles	First Year	Last Year	Average Age	Relationship Strength	Trials	2010's	post-2020
protocatechuic acid	1	catechols; dihydroxybenzoic acid	antineoplastic agent; EC 1.1.1.25 (shikimate dehydrogenase) inhibitor; EC 1.14.11.2 (procollagen-proline dioxygenase) inhibitor; human xenobiotic metabolite; plant metabolite	2021	2021	3.0	low	0	0	1
adenine	1	6-aminopurines; purine nucleobase	Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite	2019	2019	5.0	low	0	1	0
glycine	161	alpha-amino acid; amino acid zwitterion; proteinogenic amino acid; serine family amino acid	EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor; fundamental metabolite; hepatoprotective agent; micronutrient; neurotransmitter; NMDA receptor agonist; nutraceutical	2013	2022	4.1	high	30	82	79
deferoxamine	1	acyclic desferrioxamine	bacterial metabolite; ferroptosis inhibitor; iron chelator; siderophore	2020	2020	4.0	low	0	1	0
omeprazole	1	aromatic ether; benzimidazoles; pyridines; sulfoxide		2018	2018	6.0	low	1	1	0
temozolomide	1	imidazotetrazine; monocarboxylic acid amide; triazene derivative	alkylating agent; antineoplastic agent; prodrug	2022	2022	2.0	low	0	0	1
serine	1	L-alpha-amino acid; proteinogenic amino acid; serine family amino acid; serine zwitterion; serine	algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite	2019	2019	5.0	low	0	1	0
calcium acetate	1	calcium salt	chelator	2021	2021	3.0	low	1	0	1
acetonitrile	1	aliphatic nitrile; volatile organic compound	EC 3.5.1.4 (amidase) inhibitor; NMR chemical shift reference compound; polar aprotic solvent	2021	2021	3.0	low	0	0	1
cyclopentane	1	cycloalkane; cyclopentanes; volatile organic compound	non-polar solvent	2020	2020	4.0	low	0	1	0
limestone	1	calcium salt; carbonate salt; inorganic calcium salt; one-carbon compound	antacid; fertilizer; food colouring; food firming agent	2021	2021	3.0	low	1	0	1
d-alpha tocopherol	1	alpha-tocopherol	algal metabolite; antiatherogenic agent; anticoagulant; antioxidant; antiviral agent; EC 2.7.11.13 (protein kinase C) inhibitor; immunomodulator; micronutrient; nutraceutical; plant metabolite	2021	2021	3.0	low	0	0	1
manganese	1	elemental manganese; manganese group element atom	Escherichia coli metabolite; micronutrient	2021	2021	3.0	low	0	0	1
clodronic acid	1	1,1-bis(phosphonic acid); one-carbon compound; organochlorine compound	antineoplastic agent; bone density conservation agent	2019	2019	5.0	low	0	1	0
phenyl acetate	1	benzenes; phenyl acetates		2021	2021	3.0	low	1	0	1
transferrin	4			2020	2022	3.0	low	1	2	2
ng-nitroarginine methyl ester	1	alpha-amino acid ester; L-arginine derivative; methyl ester; N-nitro compound	EC 1.14.13.39 (nitric oxide synthase) inhibitor	2021	2021	3.0	low	0	0	1
simvastatin	1	delta-lactone; fatty acid ester; hexahydronaphthalenes; statin (semi-synthetic)	EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor; EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor; ferroptosis inducer; geroprotector; prodrug	2022	2022	2.0	low	1	0	1
atorvastatin	1	aromatic amide; dihydroxy monocarboxylic acid; monofluorobenzenes; pyrroles; statin (synthetic)	environmental contaminant; xenobiotic	2022	2022	2.0	low	1	0	1
dolomite	1			2021	2021	3.0	low	1	0	1
glucose, (beta-d)-isomer	1	D-glucopyranose	epitope; mouse metabolite	2019	2019	5.0	low	0	1	0
triazoles	4	1,2,3-triazole		2017	2021	5.0	low	0	2	2
firefly luciferin	1	1,3-thiazolemonocarboxylic acid; benzothiazoles; imidothioate	luciferin	2020	2020	4.0	low	0	1	0
methotrexate	1	dicarboxylic acid; monocarboxylic acid amide; pteridines	abortifacient; antimetabolite; antineoplastic agent; antirheumatic drug; dermatologic drug; DNA synthesis inhibitor; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; immunosuppressive agent	2019	2019	5.0	low	0	1	0
rhodioloside	1	glycoside		2019	2019	5.0	low	0	1	0
angiotensin ii	1	amino acid zwitterion; angiotensin II	human metabolite	2021	2021	3.0	low	0	0	1
fibrin	1	peptide		2019	2019	5.0	low	0	1	0
tretinoin	1	retinoic acid; vitamin A	anti-inflammatory agent; antineoplastic agent; antioxidant; AP-1 antagonist; human metabolite; keratolytic drug; retinoic acid receptor agonist; retinoid X receptor agonist; signalling molecule	2021	2021	3.0	low	0	0	1
oxalylglycine	1	amino dicarboxylic acid; N-acylglycine	EC 1.14.11.* (oxidoreductase acting on paired donors, 2-oxoglutarate as one donor, incorporating 1 atom each of oxygen into both donors) inhibitor	2014	2014	10.0	low	0	1	0
ku 55933	1			2020	2020	4.0	low	0	1	0
antimycin a	1	amidobenzoic acid		2016	2016	8.0	low	0	1	0
nutlin-3a	1	stilbenoid		2020	2020	4.0	low	0	1	0
losartan potassium	27			2015	2022	4.1	low	5	13	14
oligonucleotides	1			2020	2020	4.0	low	0	1	0
pevonedistat	1	cyclopentanols; indanes; pyrrolopyrimidine; secondary amino compound; sulfamidate	antineoplastic agent; apoptosis inducer	2020	2020	4.0	low	0	1	0
warfarin	1	benzenes; hydroxycoumarin; methyl ketone		2016	2016	8.0	low	1	1	0
antimycin	1			2016	2016	8.0	low	0	1	0
transforming growth factor beta	1			2021	2021	3.0	low	0	0	1
bay 85-3934	4			2017	2021	5.0	medium	0	2	2
imetelstat	1			2020	2020	4.0	low	0	1	0
gsk1278863	7			2017	2021	5.0	medium	0	4	3
epoetin alfa	4			2016	2022	4.5	low	3	2	2

Condition	Indicated	Studies	First Year	Last Year	Average Age	Relationship Strength	Trials	2010's	post-2020
2019 Novel Coronavirus Disease	0	2	2021	2022	2.5	low	0	0	2
Acidosis	0	1	2019	2019	5.0	low	1	1	0
Acute Ischemic Stroke	0	1	2022	2022	2.0	low	0	0	1
Acute Kidney Failure	0	4	2018	2022	3.2	low	0	1	3
Acute Kidney Injury	0	4	2018	2022	3.2	low	0	1	3
Acute Lung Injury	0	1	2020	2020	4.0	low	0	1	0
Age-Related Osteoporosis	0	1	2022	2022	2.0	low	0	0	1
Alloxan Diabetes	0	1	2019	2019	5.0	low	0	1	0
Anemia	1	89	2013	2022	4.1	medium	24	46	43
Anemia, Cooley's	0	1	2021	2021	3.0	low	0	0	1
Anemia, Iron-Deficiency	0	1	2017	2017	7.0	low	0	1	0
Anemia, Refractory	0	1	2020	2020	4.0	low	0	1	0
Anemias, Iron-Deficiency	0	1	2017	2017	7.0	low	0	1	0
Angiogenesis, Pathologic	0	1	2019	2019	5.0	low	0	1	0
Anoxemia	0	13	2013	2022	4.7	low	1	6	7
Aplasia Pure Red Cell	0	4	2020	2022	3.0	low	0	1	3
Apoplexy	0	1	2022	2022	2.0	low	0	0	1
Astrocytoma, Grade IV	0	1	2022	2022	2.0	low	0	0	1
Atherogenesis	0	1	2019	2019	5.0	low	0	1	0
Atherosclerosis	0	1	2019	2019	5.0	low	0	1	0
Benign Neoplasms	0	1	2018	2018	6.0	low	0	1	0
beta-Thalassemia	0	1	2021	2021	3.0	low	0	0	1
Blood Clot	0	1	2021	2021	3.0	low	0	0	1
Blood Poisoning	0	2	2020	2023	2.5	low	0	1	1
Blood Pressure, High	0	2	2019	2021	4.0	low	1	1	1
Body Weight	0	1	2016	2016	8.0	low	0	1	0
Bowel Diseases, Inflammatory	0	1	2018	2018	6.0	low	0	1	0
Brain Ischemia	0	1	2022	2022	2.0	low	0	0	1
Bruise	0	1	2020	2020	4.0	low	1	1	0
Cancer of Pancreas	0	1	2019	2019	5.0	low	0	1	0
Carcinoma, Lewis Lung	0	1	2020	2020	4.0	low	0	1	0
Cardiac Diseases	0	1	2023	2023	1.0	low	0	0	1
Cardiac Hypertrophy	0	1	2021	2021	3.0	low	0	0	1
Cardiomegaly	0	1	2021	2021	3.0	low	0	0	1
Cardiovascular Diseases	0	1	2018	2018	6.0	low	0	1	0
Cardiovascular Stroke	0	1	2020	2020	4.0	low	0	1	0
Cerebral Infarction, Middle Cerebral Artery	0	1	2022	2022	2.0	low	0	0	1
Cerebral Ischemia	0	1	2022	2022	2.0	low	0	0	1
Chronic Disease	0	2	2019	2022	3.5	low	1	1	1
Chronic Illness	0	2	2019	2022	3.5	low	1	1	1
Chronic Kidney Diseases	0	75	2013	2022	3.9	medium	20	37	38
Chronic Kidney Failure	0	7	2016	2021	5.0	low	4	4	3
Chronic Lung Injury	0	1	2021	2021	3.0	low	0	0	1
Cirrhosis	0	3	2020	2022	3.0	low	0	1	2
Cirrhosis, Liver	0	1	2016	2016	8.0	low	0	1	0
Congenital Zika Syndrome	0	1	2020	2020	4.0	low	0	1	0
Contusions	0	1	2020	2020	4.0	low	1	1	0
Corneal Endothelial Cell Damage	0	1	2018	2018	6.0	low	0	1	0
Depression	0	1	2020	2020	4.0	low	0	1	0
Diabetes Mellitus	0	1	2022	2022	2.0	low	1	0	1
Diabetic Glomerulosclerosis	0	1	2019	2019	5.0	low	0	1	0
Diabetic Nephropathies	0	1	2019	2019	5.0	low	0	1	0
Diarrhea	0	1	2020	2020	4.0	low	1	1	0
Disease Models, Animal	0	13	2016	2022	4.7	low	0	9	4
Dysmyelopoietic Syndromes	0	4	2020	2022	2.8	low	1	1	3
Electrolytes	0	1	2021	2021	3.0	low	0	0	1
Emesis	0	1	2020	2020	4.0	low	1	1	0
Encephalomyelitis, Subacute Necrotizing	0	1	2016	2016	8.0	low	0	1	0
Encephalopathy, Toxic	0	1	2021	2021	3.0	low	0	0	1
Endotoxin Shock	0	1	2023	2023	1.0	low	0	0	1
Experimental Lung Inflammation	0	1	2021	2021	3.0	low	0	0	1
Fatty Liver	0	1	2021	2021	3.0	low	0	0	1
Femoral Neck Fractures	0	1	2021	2021	3.0	low	0	0	1
Femur Neck Fractures	0	1	2021	2021	3.0	low	0	0	1
Fibrosis	0	3	2020	2022	3.0	low	0	1	2
Gastrointestinal Hemorrhage	0	1	2021	2021	3.0	low	0	0	1
Generalized Resistance to Thyroid Hormone	0	1	2022	2022	2.0	low	0	0	1
Genetic Diseases	0	1	2018	2018	6.0	low	0	1	0
Genetic Diseases, Inborn	0	1	2018	2018	6.0	low	0	1	0
Glioblastoma	0	1	2022	2022	2.0	low	0	0	1
Heart Diseases	0	1	2023	2023	1.0	low	0	0	1
Hematochezia	0	1	2021	2021	3.0	low	0	0	1
Hemorrhage, Retinal	0	1	2020	2020	4.0	low	1	1	0
Hyperkalemia	0	2	2019	2019	5.0	low	2	2	0
Hyperoxia	0	1	2021	2021	3.0	low	0	0	1
Hyperpotassemia	0	2	2019	2019	5.0	low	2	2	0
Hypertension	0	2	2019	2021	4.0	low	1	1	1
Hypertension, Pulmonary	0	1	2019	2019	5.0	low	0	1	0
Hypertrophy	0	1	2019	2019	5.0	low	0	1	0
Hypoxia	0	13	2013	2022	4.7	low	1	6	7
Infarction, Middle Cerebral Artery	0	1	2022	2022	2.0	low	0	0	1
Inflammation	0	2	2017	2022	4.5	low	1	1	1
Inflammatory Bowel Diseases	0	1	2018	2018	6.0	low	0	1	0
Injuries, Radiation	0	4	2019	2022	3.5	low	0	2	2
Injuries, Spinal Cord	0	1	2016	2016	8.0	low	0	1	0
Injuries, Tendon	0	1	2016	2016	8.0	low	0	1	0
Injury, Ischemia-Reperfusion	0	3	2021	2022	2.7	low	0	0	3
Injury, Myocardial Reperfusion	0	2	2020	2020	4.0	low	0	2	0
Innate Inflammatory Response	0	2	2017	2022	4.5	low	1	1	1
Interstitial Nephritis	0	1	2019	2019	5.0	low	0	1	0
Ischemia	0	2	2020	2022	3.0	low	0	1	1
Ischemic Stroke	0	1	2022	2022	2.0	low	0	0	1
Kidney Diseases	1	3	2021	2022	2.3	low	0	0	3
Kidney Failure	0	1	2021	2021	3.0	low	0	0	1
Kidney Failure, Chronic	0	7	2016	2021	5.0	low	4	4	3
Leigh Disease	0	1	2016	2016	8.0	low	0	1	0
Liver Cirrhosis	0	1	2016	2016	8.0	low	0	1	0
Liver Diseases	0	1	2016	2016	8.0	low	0	1	0
Liver Dysfunction	0	1	2016	2016	8.0	low	0	1	0
Liver Steatosis	0	1	2021	2021	3.0	low	0	0	1
Lung Injury, Acute	0	1	2020	2020	4.0	low	0	1	0
Malnourishment	0	1	2022	2022	2.0	low	1	0	1
Malnutrition	0	1	2022	2022	2.0	low	1	0	1
Metabolic Acidosis	0	1	2019	2019	5.0	low	1	1	0
Myelodysplastic Syndromes	1	4	2020	2022	2.8	low	1	1	3
Myocardial Infarction	0	1	2020	2020	4.0	low	0	1	0
Nasopharyngitis	0	1	2020	2020	4.0	low	1	1	0
Neoplasms	0	1	2018	2018	6.0	low	0	1	0
Nephritis	0	1	2018	2018	6.0	low	0	1	0
Nephritis, Interstitial	0	1	2019	2019	5.0	low	0	1	0
Osteoporosis	0	1	2022	2022	2.0	low	0	0	1
Pancreatic Neoplasms	0	1	2019	2019	5.0	low	0	1	0
Pneumonia	0	1	2021	2021	3.0	low	0	0	1
Proteinuria	0	1	2021	2021	3.0	low	0	0	1
Pulmonary Arterial Remodeling	0	1	2021	2021	3.0	low	0	0	1
Pulmonary Hypertension	0	1	2019	2019	5.0	low	0	1	0
Red-Cell Aplasia, Pure	0	4	2020	2022	3.0	low	0	1	3
Refractory Anemia	0	1	2020	2020	4.0	low	0	1	0
Renal Insufficiency	0	1	2021	2021	3.0	low	0	0	1
Renal Insufficiency, Chronic	1	75	2013	2022	3.9	medium	20	37	38
Reperfusion Injury	0	3	2021	2022	2.7	low	0	0	3
Retinal Detachment	0	1	2016	2016	8.0	low	0	1	0
Retinal Pigment Epithelial Detachment	0	1	2016	2016	8.0	low	0	1	0
Retinopathy of Prematurity	0	2	2016	2019	6.5	low	0	2	0
Retrolental Fibroplasia	0	2	2016	2019	6.5	low	0	2	0
Rhabdomyolysis	0	1	2021	2021	3.0	low	0	0	1
Sepsis	0	2	2020	2023	2.5	low	0	1	1
Shock, Septic	0	1	2023	2023	1.0	low	0	0	1
Spinal Cord Injuries	0	1	2016	2016	8.0	low	0	1	0
Stroke	0	1	2022	2022	2.0	low	0	0	1
Thrombosis	0	1	2021	2021	3.0	low	0	0	1
Ureteral Obstruction	0	1	2020	2020	4.0	low	0	1	0
Urinary Tract Infections	0	1	2021	2021	3.0	low	0	0	1
Vascular Calcification	0	1	2016	2016	8.0	low	0	1	0
Vomiting	0	1	2020	2020	4.0	low	1	1	0
Zika Virus Infection	0	1	2020	2020	4.0	low	0	1	0

Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
Proceedings of the National Academy of Sciences of the United States of America, , 12-08, Volume: 117, Issue:49, 2020

Transplantation of Roxadustat-preconditioned bone marrow stromal cells improves neurological function recovery through enhancing grafted cell survival in ischemic stroke rats.
CNS neuroscience & therapeutics, , Volume: 28, Issue:10, 2022

Roxadustat for Anemia in Patients with Kidney Disease Not Receiving Dialysis.
The New England journal of medicine, , 09-12, Volume: 381, Issue:11, 2019

Successful treatment of anti-EPO antibody associated refractory anemia with hypoxia-inducible factor prolyl hydroxylase inhibitor.
Renal failure, , Volume: 42, Issue:1, 2020

The HIFα-Stabilizing Drug Roxadustat Increases the Number of Renal Epo-Producing Sca-1
Cells, , 02-21, Volume: 11, Issue:4, 2022

Effects of Roxadustat on Erythropoietin Production in the Rat Body.
Molecules (Basel, Switzerland), , Feb-08, Volume: 27, Issue:3, 2022

Improving lipophilicity of 5-(1-acetyl-5-phenylpyrazolidin-3-ylidene)-1,3-dimethylbarbituric acid increases its efficacy to activate hypoxia-inducible factors.
Bioorganic & medicinal chemistry, , 11-01, Volume: 73, 2022

HIF-α activation by the prolyl hydroxylase inhibitor roxadustat suppresses chemoresistant glioblastoma growth by inducing ferroptosis.
Cell death & disease, , 10-08, Volume: 13, Issue:10, 2022

Physiological hypoxia restrains the senescence-associated secretory phenotype via AMPK-mediated mTOR suppression.
Molecular cell, , 05-06, Volume: 81, Issue:9, 2021

Get use to the -dustats: Roxadustat and molidustat, members of the hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor drug class promote kidney function, perfusion and oxygenation in rats through nitric oxide.
Acta physiologica (Oxford, England), , Volume: 233, Issue:1, 2021

Up-regulation of the manganese transporter SLC30A10 by hypoxia-inducible factors defines a homeostatic response to manganese toxicity.
Proceedings of the National Academy of Sciences of the United States of America, , 08-31, Volume: 118, Issue:35, 2021

Oral Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor Roxadustat (FG-4592) for Treatment of Anemia in Chronic Kidney Disease: A Placebo-Controlled Study of Pharmacokinetic and Pharmacodynamic Profiles in Hemodialysis Patients.
Journal of clinical pharmacology, , Volume: 60, Issue:11, 2020

Photoactivatable Prolyl Hydroxylase 2 Inhibitors for Stabilizing the Hypoxia-Inducible Factor with Light.
Journal of medicinal chemistry, , 08-22, Volume: 62, Issue:16, 2019

Hypoxia and the Prolyl Hydroxylase Inhibitor FG-4592 Protect Corneal Endothelial Cells From Mechanical and Perioperative Surgical Stress.
Cornea, , Volume: 37, Issue:4, 2018

Hypoxia-inducible factor-1 plays a role in phosphate-induced vascular smooth muscle cell calcification.
Kidney international, , Volume: 90, Issue:3, 2016

Targeting the hypoxia-sensing pathway in clinical hematology.
Stem cells translational medicine, , Volume: 3, Issue:2, 2014

Inhibition of hypoxia-inducible factor prolyl hydroxylase domain oxygen sensors: tricking the body into mounting orchestrated survival and repair responses.
Journal of medicinal chemistry, , Dec-12, Volume: 56, Issue:23, 2013

Treatment of Renal Anemia in Patients With Hemodialysis Using Hypoxia-inducible Factor (HIF) Stabilizer, Roxadustat: A Short-term Clinical Study.
In vivo (Athens, Greece), , Volume: 36, Issue:4

Roxadustat in the treatment of anaemia in chronic kidney disease.
Expert opinion on investigational drugs, , Volume: 27, Issue:1, 2018

Transplantation of Roxadustat-preconditioned bone marrow stromal cells improves neurological function recovery through enhancing grafted cell survival in ischemic stroke rats.
CNS neuroscience & therapeutics, , Volume: 28, Issue:10, 2022

Long-term efficacy, safety, and medication compliance of roxadustat on peritoneal dialysis patients with renal anemia affected by the COVID-19 pandemic: a retrospective study.
Annals of palliative medicine, , Volume: 11, Issue:6, 2022

Roxadustat Treatment of Chronic Kidney Disease-Associated Anemia in Japanese Patients Not on Dialysis: A Phase 2, Randomized, Double-Blind, Placebo-Controlled Trial.
Advances in therapy, , Volume: 36, Issue:6, 2019

Phase 3, Randomized, Double-Blind, Active-Comparator (Darbepoetin Alfa) Study of Oral Roxadustat in CKD Patients with Anemia on Hemodialysis in Japan.
Journal of the American Society of Nephrology : JASN, , Volume: 31, Issue:7, 2020

FG-4592 Improves Depressive-Like Behaviors through HIF-1-Mediated Neurogenesis and Synapse Plasticity in Rats.
Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics, , Volume: 17, Issue:2, 2020

Clinical parameters among patients in Japan with anemia and non-dialysis-dependent chronic kidney disease with and without diabetes mellitus who received roxadustat.
Clinical and experimental nephrology, , Volume: 26, Issue:9, 2022

Salidroside and FG-4592 ameliorate high glucose-induced glomerular endothelial cells injury via HIF upregulation.
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, , Volume: 118, 2019

Phase 3, Randomized, Double-Blind, Active-Comparator (Darbepoetin Alfa) Study of Oral Roxadustat in CKD Patients with Anemia on Hemodialysis in Japan.
Journal of the American Society of Nephrology : JASN, , Volume: 31, Issue:7, 2020

Roxadustat prevents Ang II hypertension by targeting angiotensin receptors and eNOS.
JCI insight, , 09-22, Volume: 6, Issue:18, 2021

Selective HIF stabilization alleviates hepatocellular steatosis and ballooning in a rodent model of 70% liver resection.
Clinical science (London, England : 1979), , 10-15, Volume: 135, Issue:19, 2021

HIF/Ca
Life sciences, , Jan-01, Volume: 264, 2021

Effect of Roxadustat on Factors Associated with Renal Fibrosis and Efficacy.
Computational and mathematical methods in medicine, , Volume: 2022, 2022

Anti-anemia drug FG4592 retards the AKI-to-CKD transition by improving vascular regeneration and antioxidative capability.
Clinical science (London, England : 1979), , 07-30, Volume: 135, Issue:14, 2021

Effects of orally active hypoxia inducible factor alpha prolyl hydroxylase inhibitor, FG4592 on renal fibrogenic potential in mouse unilateral ureteral obstruction model.
Journal of pharmacological sciences, , Volume: 142, Issue:3, 2020

HIF-α activation by the prolyl hydroxylase inhibitor roxadustat suppresses chemoresistant glioblastoma growth by inducing ferroptosis.
Cell death & disease, , 10-08, Volume: 13, Issue:10, 2022

Novel function of Roxadustat (FG-4592) as an anti-shock drug in sepsis by regulating mitochondrial oxidative stress and energy metabolism.
Biochimica et biophysica acta. General subjects, , Volume: 1867, Issue:1, 2023

Roxadustat prevents Ang II hypertension by targeting angiotensin receptors and eNOS.
JCI insight, , 09-22, Volume: 6, Issue:18, 2021

Does HIF-PHI increased risk of gastrointestinal hemorrhage in patients with renal anemia: a review of cases reported to the U.S. Food and drug administration adverse event reporting system.
Renal failure, , Volume: 43, Issue:1, 2021

Roxadustat Treatment for Anemia in Patients Undergoing Long-Term Dialysis.
The New England journal of medicine, , 09-12, Volume: 381, Issue:11, 2019

Roxadustat for Anemia in Patients with Kidney Disease Not Receiving Dialysis.
The New England journal of medicine, , 09-12, Volume: 381, Issue:11, 2019

Roxadustat prevents Ang II hypertension by targeting angiotensin receptors and eNOS.
JCI insight, , 09-22, Volume: 6, Issue:18, 2021

Roxadustat Treatment for Anemia in Patients Undergoing Long-Term Dialysis.
The New England journal of medicine, , 09-12, Volume: 381, Issue:11, 2019

Roxadustat: another drug that causes pulmonary hypertension? Report of first human case.
Polish archives of internal medicine, , 05-31, Volume: 129, Issue:5, 2019

Hypoxia Activates the PTHrP -MEF2C Pathway to Attenuate Hypertrophy in Mesenchymal Stem Cell Derived Cartilage.
Scientific reports, , 09-16, Volume: 9, Issue:1, 2019

A Prospective, Self-Controlled Pilot Study of the Efficacy of Roxadustat for Erythropoietin Hyporesponsiveness in Patients Requiring Chronic Ambulatory Peritoneal Dialysis.
Journal of renal nutrition : the official journal of the Council on Renal Nutrition of the National Kidney Foundation, , Volume: 32, Issue:5, 2022

Targeting Hypoxia-Inducible Factors for the Treatment of Anemia in Chronic Kidney Disease Patients.
American journal of nephrology, , Volume: 45, Issue:3, 2017

Roxadustat (FG-4592) protects against ischaemia/reperfusion-induced acute kidney injury through inhibiting the mitochondrial damage pathway in mice.
Clinical and experimental pharmacology & physiology, , Volume: 49, Issue:2, 2022

Can Pharmacological Ischemic Preconditioning Affect Myocardial Ischemic Injury?
Circulation journal : official journal of the Japanese Circulation Society, , 05-25, Volume: 84, Issue:6, 2020

Tetrahydropyridin-4-ylpicolinoylglycines as novel and orally active prolyl hydroxylase 2 (PHD2) inhibitors for the treatment of renal anemia.
European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022

Effect of Roxadustat on Factors Associated with Renal Fibrosis and Efficacy.
Computational and mathematical methods in medicine, , Volume: 2022, 2022

Retinoic acid regulates erythropoietin production cooperatively with hypoxia-inducible factors in human iPSC-derived erythropoietin-producing cells.
Scientific reports, , 02-16, Volume: 11, Issue:1, 2021

Roxadustat for anemia in patients with end-stage renal disease incident to dialysis.
Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association, , 08-27, Volume: 36, Issue:9, 2021

Roxadustat on anti-erythropoietin antibody-related pure red cell aplasia in the patient with end-stage renal disease.
Seminars in dialysis, , Volume: 34, Issue:4, 2021

Roxadustat for the Maintenance Treatment of Anemia in Patients with End-Stage Kidney Disease on Stable Dialysis: A European Phase 3, Randomized, Open-Label, Active-Controlled Study (PYRENEES).
Advances in therapy, , Volume: 38, Issue:10, 2021

Oral Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor Roxadustat (FG-4592) for Treatment of Anemia in Chronic Kidney Disease: A Placebo-Controlled Study of Pharmacokinetic and Pharmacodynamic Profiles in Hemodialysis Patients.
Journal of clinical pharmacology, , Volume: 60, Issue:11, 2020

Targeting Hypoxia-Inducible Factors for the Treatment of Anemia in Chronic Kidney Disease Patients.
American journal of nephrology, , Volume: 45, Issue:3, 2017

Emerging treatments for anemia in patients with CKD and ESRD.
Nephrology news & issues, , Volume: 31, Issue:4, 2017

Roxadustat (FG-4592) Versus Epoetin Alfa for Anemia in Patients Receiving Maintenance Hemodialysis: A Phase 2, Randomized, 6- to 19-Week, Open-Label, Active-Comparator, Dose-Ranging, Safety and Exploratory Efficacy Study.
American journal of kidney diseases : the official journal of the National Kidney Foundation, , Volume: 67, Issue:6, 2016

Hypoxia as a therapy for mitochondrial disease.
Science (New York, N.Y.), , Apr-01, Volume: 352, Issue:6281, 2016

Effect of Moderate Hepatic Impairment on the Pharmacokinetics and Pharmacodynamics of Roxadustat, an Oral Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor.
Clinical drug investigation, , Volume: 36, Issue:9, 2016

Roxadustat for the treatment of anemia in patients with lower-risk myelodysplastic syndrome: Open-label, dose-selection, lead-in stage of a phase 3 study.
American journal of hematology, , 02-01, Volume: 97, Issue:2, 2022

Targeting ineffective hematopoiesis in myelodysplastic syndromes.
American journal of hematology, , 02-01, Volume: 97, Issue:2, 2022

Clinical and Molecular Insights in Erythropoiesis Regulation of Signal Transduction Pathways in Myelodysplastic Syndromes and β-Thalassemia.
International journal of molecular sciences, , Jan-15, Volume: 22, Issue:2, 2021

New Approaches for Anemia in MDS.
Clinical lymphoma, myeloma & leukemia, , Volume: 20 Suppl 1, 2020

Roxadustat Markedly Reduces Myocardial Ischemia Reperfusion Injury in Mice.
Circulation journal : official journal of the Japanese Circulation Society, , 05-25, Volume: 84, Issue:6, 2020

Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
Journal of medicinal chemistry, , 08-23, Volume: 61, Issue:16, 2018

Mononuclear phagocytes orchestrate prolyl hydroxylase inhibition-mediated renoprotection in chronic tubulointerstitial nephritis.
Kidney international, , Volume: 96, Issue:2, 2019

Roxadustat promotes osteoblast differentiation and prevents estrogen deficiency-induced bone loss by stabilizing HIF-1α and activating the Wnt/β-catenin signaling pathway.
Journal of orthopaedic surgery and research, , May-21, Volume: 17, Issue:1, 2022

Selective EGLN Inhibition Enables Ablative Radiotherapy and Improves Survival in Unresectable Pancreatic Cancer.
Cancer research, , 05-01, Volume: 79, Issue:9, 2019

On the Increased Event Rate of Urinary Tract Infection and Pneumonia in CKD Patients Treated with Roxadustat for Anemia.
Journal of the American Society of Nephrology : JASN, , 06-01, Volume: 32, Issue:6, 2021

Roxadustat prevents Ang II hypertension by targeting angiotensin receptors and eNOS.
JCI insight, , 09-22, Volume: 6, Issue:18, 2021

Roxadustat Improves Erythropoietin Antibody-Mediated Pure Red Cell Aplasia in a Patient with Hemodialysis.
Blood purification, , Volume: 51, Issue:2, 2022

Remarkable response to roxadustat in a case of anti-erythropoietin antibody-mediated pure red cell aplasia.
Annals of hematology, , Volume: 100, Issue:2, 2021

Roxadustat on anti-erythropoietin antibody-related pure red cell aplasia in the patient with end-stage renal disease.
Seminars in dialysis, , Volume: 34, Issue:4, 2021

Resolution of epoetin-induced pure red cell aplasia, successful re-challenge with roxadustat.
International journal of laboratory hematology, , Volume: 42, Issue:6, 2020

Prolyl-4-Hydroxylases Inhibitor Stabilizes HIF-1α and Increases Mitophagy to Reduce Cell Death After Experimental Retinal Detachment.
Investigative ophthalmology & visual science, , Volume: 57, Issue:4, 2016

Serine and 1-carbon metabolism are required for HIF-mediated protection against retinopathy of prematurity.
JCI insight, , 07-25, Volume: 4, Issue:14, 2019

Comparative systems pharmacology of HIF stabilization in the prevention of retinopathy of prematurity.
Proceedings of the National Academy of Sciences of the United States of America, , May-03, Volume: 113, Issue:18, 2016

A case report of rhabdomyolysis caused by the use of roxadustat in the treatment caused by renal anaemia.
International journal of clinical practice, , Volume: 75, Issue:6, 2021

Novel function of Roxadustat (FG-4592) as an anti-shock drug in sepsis by regulating mitochondrial oxidative stress and energy metabolism.
Biochimica et biophysica acta. General subjects, , Volume: 1867, Issue:1, 2023

Stabilization of HIF-1α by FG-4592 promotes functional recovery and neural protection in experimental spinal cord injury.
Brain research, , Feb-01, Volume: 1632, 2016

Roxadustat Does Not Affect Platelet Production, Activation, and Thrombosis Formation.
Arteriosclerosis, thrombosis, and vascular biology, , Volume: 41, Issue:10, 2021

On the Increased Event Rate of Urinary Tract Infection and Pneumonia in CKD Patients Treated with Roxadustat for Anemia.
Journal of the American Society of Nephrology : JASN, , 06-01, Volume: 32, Issue:6, 2021

Phase 3, Randomized, Double-Blind, Active-Comparator (Darbepoetin Alfa) Study of Oral Roxadustat in CKD Patients with Anemia on Hemodialysis in Japan.
Journal of the American Society of Nephrology : JASN, , Volume: 31, Issue:7, 2020

Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
Journal of medicinal chemistry, , 08-23, Volume: 61, Issue:16, 2018

Roxadustat (FG-4592) protects against ischaemia/reperfusion-induced acute kidney injury through inhibiting the mitochondrial damage pathway in mice.
Clinical and experimental pharmacology & physiology, , Volume: 49, Issue:2, 2022

Reoxygenation induces reactive oxygen species production and ferroptosis in renal tubular epithelial cells by activating aryl hydrocarbon receptor.
Molecular medicine reports, , Volume: 23, Issue:1, 2021

Anti-anemia drug FG4592 retards the AKI-to-CKD transition by improving vascular regeneration and antioxidative capability.
Clinical science (London, England : 1979), , 07-30, Volume: 135, Issue:14, 2021

Clinical and Molecular Insights in Erythropoiesis Regulation of Signal Transduction Pathways in Myelodysplastic Syndromes and β-Thalassemia.
International journal of molecular sciences, , Jan-15, Volume: 22, Issue:2, 2021

Emerging treatments for anemia in patients with CKD and ESRD.
Nephrology news & issues, , Volume: 31, Issue:4, 2017

Novel function of Roxadustat (FG-4592) as an anti-shock drug in sepsis by regulating mitochondrial oxidative stress and energy metabolism.
Biochimica et biophysica acta. General subjects, , Volume: 1867, Issue:1, 2023

Hypoxia-inducible factor prolyl-hydroxylase inhibitor roxadustat (FG-4592) alleviates sepsis-induced acute lung injury.
Respiratory physiology & neurobiology, , Volume: 281, 2020

Transplantation of Roxadustat-preconditioned bone marrow stromal cells improves neurological function recovery through enhancing grafted cell survival in ischemic stroke rats.
CNS neuroscience & therapeutics, , Volume: 28, Issue:10, 2022

Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
Journal of medicinal chemistry, , 08-23, Volume: 61, Issue:16, 2018

A Prospective, Self-Controlled Pilot Study of the Efficacy of Roxadustat for Erythropoietin Hyporesponsiveness in Patients Requiring Chronic Ambulatory Peritoneal Dialysis.
Journal of renal nutrition : the official journal of the Council on Renal Nutrition of the National Kidney Foundation, , Volume: 32, Issue:5, 2022

Adipocyte Hypoxia-Inducible Factor 2α Suppresses Atherosclerosis by Promoting Adipose Ceramide Catabolism.
Cell metabolism, , 11-05, Volume: 30, Issue:5, 2019

Suppression of thyrotropin secretion during roxadustat treatment for renal anemia in a patient undergoing hemodialysis.
BMC nephrology, , 03-20, Volume: 22, Issue:1, 2021

Hypoxia-inducible factor prolyl-hydroxylase inhibitor roxadustat (FG-4592) alleviates sepsis-induced acute lung injury.
Respiratory physiology & neurobiology, , Volume: 281, 2020

Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022

Roxadustat (FG-4592) protects against ischaemia/reperfusion-induced acute kidney injury through inhibiting the mitochondrial damage pathway in mice.
Clinical and experimental pharmacology & physiology, , Volume: 49, Issue:2, 2022

Anti-anemia drug FG4592 retards the AKI-to-CKD transition by improving vascular regeneration and antioxidative capability.
Clinical science (London, England : 1979), , 07-30, Volume: 135, Issue:14, 2021

Hypoxia-inducible factor prolyl hydroxylase inhibitor roxadustat (FG-4592) protects against cisplatin-induced acute kidney injury.
Clinical science (London, England : 1979), , 04-16, Volume: 132, Issue:7, 2018

Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist.
Journal of medicinal chemistry, , 05-26, Volume: 65, Issue:10, 2022

Roxadustat attenuates hyperoxia-induced lung injury by upregulating proangiogenic factors in newborn mice.
Pediatrics and neonatology, , Volume: 62, Issue:4, 2021

Emerging treatments for anemia in patients with CKD and ESRD.
Nephrology news & issues, , Volume: 31, Issue:4, 2017

Novel function of Roxadustat (FG-4592) as an anti-shock drug in sepsis by regulating mitochondrial oxidative stress and energy metabolism.
Biochimica et biophysica acta. General subjects, , Volume: 1867, Issue:1, 2023

Hypoxia-inducible factor prolyl-hydroxylase inhibitor roxadustat (FG-4592) alleviates sepsis-induced acute lung injury.
Respiratory physiology & neurobiology, , Volume: 281, 2020

Prolyl-hydroxylase inhibitors reconstitute tumor blood vessels in mice.
Journal of pharmacological sciences, , Volume: 143, Issue:2, 2020

Transplantation of Roxadustat-preconditioned bone marrow stromal cells improves neurological function recovery through enhancing grafted cell survival in ischemic stroke rats.
CNS neuroscience & therapeutics, , Volume: 28, Issue:10, 2022

Up-regulation of the manganese transporter SLC30A10 by hypoxia-inducible factors defines a homeostatic response to manganese toxicity.
Proceedings of the National Academy of Sciences of the United States of America, , 08-31, Volume: 118, Issue:35, 2021

Transplantation of Roxadustat-preconditioned bone marrow stromal cells improves neurological function recovery through enhancing grafted cell survival in ischemic stroke rats.
CNS neuroscience & therapeutics, , Volume: 28, Issue:10, 2022

Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
Journal of medicinal chemistry, , 08-23, Volume: 61, Issue:16, 2018

A Prospective, Self-Controlled Pilot Study of the Efficacy of Roxadustat for Erythropoietin Hyporesponsiveness in Patients Requiring Chronic Ambulatory Peritoneal Dialysis.
Journal of renal nutrition : the official journal of the Council on Renal Nutrition of the National Kidney Foundation, , Volume: 32, Issue:5, 2022

Adipocyte Hypoxia-Inducible Factor 2α Suppresses Atherosclerosis by Promoting Adipose Ceramide Catabolism.
Cell metabolism, , 11-05, Volume: 30, Issue:5, 2019

Suppression of thyrotropin secretion during roxadustat treatment for renal anemia in a patient undergoing hemodialysis.
BMC nephrology, , 03-20, Volume: 22, Issue:1, 2021

Roxadustat attenuates hyperoxia-induced lung injury by upregulating proangiogenic factors in newborn mice.
Pediatrics and neonatology, , Volume: 62, Issue:4, 2021

Hypoxia-inducible factor prolyl-hydroxylase inhibitor roxadustat (FG-4592) alleviates sepsis-induced acute lung injury.
Respiratory physiology & neurobiology, , Volume: 281, 2020

Hypoxia and the Prolyl Hydroxylase Inhibitor FG-4592 Protect Corneal Endothelial Cells From Mechanical and Perioperative Surgical Stress.
Cornea, , Volume: 37, Issue:4, 2018

Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022

Roxadustat (FG-4592) protects against ischaemia/reperfusion-induced acute kidney injury through inhibiting the mitochondrial damage pathway in mice.
Clinical and experimental pharmacology & physiology, , Volume: 49, Issue:2, 2022

Anti-anemia drug FG4592 retards the AKI-to-CKD transition by improving vascular regeneration and antioxidative capability.
Clinical science (London, England : 1979), , 07-30, Volume: 135, Issue:14, 2021

Hypoxia-inducible factor prolyl hydroxylase inhibitor roxadustat (FG-4592) protects against cisplatin-induced acute kidney injury.
Clinical science (London, England : 1979), , 04-16, Volume: 132, Issue:7, 2018

Hypoxia-inducible factor-1 plays a role in phosphate-induced vascular smooth muscle cell calcification.
Kidney international, , Volume: 90, Issue:3, 2016

Roxadustat prevents Ang II hypertension by targeting angiotensin receptors and eNOS.
JCI insight, , 09-22, Volume: 6, Issue:18, 2021

Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
Proceedings of the National Academy of Sciences of the United States of America, , 12-08, Volume: 117, Issue:49, 2020

Transplantation of Roxadustat-preconditioned bone marrow stromal cells improves neurological function recovery through enhancing grafted cell survival in ischemic stroke rats.
CNS neuroscience & therapeutics, , Volume: 28, Issue:10, 2022

Long-term efficacy, safety, and medication compliance of roxadustat on peritoneal dialysis patients with renal anemia affected by the COVID-19 pandemic: a retrospective study.
Annals of palliative medicine, , Volume: 11, Issue:6, 2022

Hypoxic and pharmacological activation of HIF inhibits SARS-CoV-2 infection of lung epithelial cells.
Cell reports, , 04-20, Volume: 35, Issue:3, 2021

Roxadustat for Anemia in Patients with Kidney Disease Not Receiving Dialysis.
The New England journal of medicine, , 09-12, Volume: 381, Issue:11, 2019

Successful treatment of anti-EPO antibody associated refractory anemia with hypoxia-inducible factor prolyl hydroxylase inhibitor.
Renal failure, , Volume: 42, Issue:1, 2020

Improving lipophilicity of 5-(1-acetyl-5-phenylpyrazolidin-3-ylidene)-1,3-dimethylbarbituric acid increases its efficacy to activate hypoxia-inducible factors.
Bioorganic & medicinal chemistry, , 11-01, Volume: 73, 2022

HIF-α activation by the prolyl hydroxylase inhibitor roxadustat suppresses chemoresistant glioblastoma growth by inducing ferroptosis.
Cell death & disease, , 10-08, Volume: 13, Issue:10, 2022

The HIFα-Stabilizing Drug Roxadustat Increases the Number of Renal Epo-Producing Sca-1
Cells, , 02-21, Volume: 11, Issue:4, 2022

Effects of Roxadustat on Erythropoietin Production in the Rat Body.
Molecules (Basel, Switzerland), , Feb-08, Volume: 27, Issue:3, 2022

Physiological hypoxia restrains the senescence-associated secretory phenotype via AMPK-mediated mTOR suppression.
Molecular cell, , 05-06, Volume: 81, Issue:9, 2021

Get use to the -dustats: Roxadustat and molidustat, members of the hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor drug class promote kidney function, perfusion and oxygenation in rats through nitric oxide.
Acta physiologica (Oxford, England), , Volume: 233, Issue:1, 2021

Up-regulation of the manganese transporter SLC30A10 by hypoxia-inducible factors defines a homeostatic response to manganese toxicity.
Proceedings of the National Academy of Sciences of the United States of America, , 08-31, Volume: 118, Issue:35, 2021

Oral Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor Roxadustat (FG-4592) for Treatment of Anemia in Chronic Kidney Disease: A Placebo-Controlled Study of Pharmacokinetic and Pharmacodynamic Profiles in Hemodialysis Patients.
Journal of clinical pharmacology, , Volume: 60, Issue:11, 2020

Photoactivatable Prolyl Hydroxylase 2 Inhibitors for Stabilizing the Hypoxia-Inducible Factor with Light.
Journal of medicinal chemistry, , 08-22, Volume: 62, Issue:16, 2019

Hypoxia and the Prolyl Hydroxylase Inhibitor FG-4592 Protect Corneal Endothelial Cells From Mechanical and Perioperative Surgical Stress.
Cornea, , Volume: 37, Issue:4, 2018

Hypoxia-inducible factor-1 plays a role in phosphate-induced vascular smooth muscle cell calcification.
Kidney international, , Volume: 90, Issue:3, 2016

Targeting the hypoxia-sensing pathway in clinical hematology.
Stem cells translational medicine, , Volume: 3, Issue:2, 2014

Inhibition of hypoxia-inducible factor prolyl hydroxylase domain oxygen sensors: tricking the body into mounting orchestrated survival and repair responses.
Journal of medicinal chemistry, , Dec-12, Volume: 56, Issue:23, 2013

Treatment of Renal Anemia in Patients With Hemodialysis Using Hypoxia-inducible Factor (HIF) Stabilizer, Roxadustat: A Short-term Clinical Study.
In vivo (Athens, Greece), , Volume: 36, Issue:4

Hypoxia as a therapy for mitochondrial disease.
Science (New York, N.Y.), , Apr-01, Volume: 352, Issue:6281, 2016

Transplantation of Roxadustat-preconditioned bone marrow stromal cells improves neurological function recovery through enhancing grafted cell survival in ischemic stroke rats.
CNS neuroscience & therapeutics, , Volume: 28, Issue:10, 2022

Long-term efficacy, safety, and medication compliance of roxadustat on peritoneal dialysis patients with renal anemia affected by the COVID-19 pandemic: a retrospective study.
Annals of palliative medicine, , Volume: 11, Issue:6, 2022

Roxadustat Treatment of Chronic Kidney Disease-Associated Anemia in Japanese Patients Not on Dialysis: A Phase 2, Randomized, Double-Blind, Placebo-Controlled Trial.
Advances in therapy, , Volume: 36, Issue:6, 2019

Phase 3, Randomized, Double-Blind, Active-Comparator (Darbepoetin Alfa) Study of Oral Roxadustat in CKD Patients with Anemia on Hemodialysis in Japan.
Journal of the American Society of Nephrology : JASN, , Volume: 31, Issue:7, 2020

Roxadustat promotes angiogenesis through HIF-1α/VEGF/VEGFR2 signaling and accelerates cutaneous wound healing in diabetic rats.
Wound repair and regeneration : official publication of the Wound Healing Society [and] the European Tissue Repair Society, , Volume: 27, Issue:4, 2019

Salidroside and FG-4592 ameliorate high glucose-induced glomerular endothelial cells injury via HIF upregulation.
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, , Volume: 118, 2019

FG-4592 alleviates radiation-induced intestinal injury by facilitating recovery of intestinal stem cell and reducing damage of intestinal epithelial.
Toxicology letters, , Mar-01, Volume: 357, 2022

Anti-anemia drug FG4592 retards the AKI-to-CKD transition by improving vascular regeneration and antioxidative capability.
Clinical science (London, England : 1979), , 07-30, Volume: 135, Issue:14, 2021

Selective HIF stabilization alleviates hepatocellular steatosis and ballooning in a rodent model of 70% liver resection.
Clinical science (London, England : 1979), , 10-15, Volume: 135, Issue:19, 2021

Roxadustat Does Not Affect Platelet Production, Activation, and Thrombosis Formation.
Arteriosclerosis, thrombosis, and vascular biology, , Volume: 41, Issue:10, 2021

Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
Proceedings of the National Academy of Sciences of the United States of America, , 12-08, Volume: 117, Issue:49, 2020

Hypoxia-inducible factor prolyl-hydroxylase inhibitor roxadustat (FG-4592) alleviates sepsis-induced acute lung injury.
Respiratory physiology & neurobiology, , Volume: 281, 2020

Roxadustat Markedly Reduces Myocardial Ischemia Reperfusion Injury in Mice.
Circulation journal : official journal of the Japanese Circulation Society, , 05-25, Volume: 84, Issue:6, 2020

Mononuclear phagocytes orchestrate prolyl hydroxylase inhibition-mediated renoprotection in chronic tubulointerstitial nephritis.
Kidney international, , Volume: 96, Issue:2, 2019

Serine and 1-carbon metabolism are required for HIF-mediated protection against retinopathy of prematurity.
JCI insight, , 07-25, Volume: 4, Issue:14, 2019

Roxadustat promotes angiogenesis through HIF-1α/VEGF/VEGFR2 signaling and accelerates cutaneous wound healing in diabetic rats.
Wound repair and regeneration : official publication of the Wound Healing Society [and] the European Tissue Repair Society, , Volume: 27, Issue:4, 2019

Targeting Hypoxia-Inducible Factors for the Treatment of Anemia in Chronic Kidney Disease Patients.
American journal of nephrology, , Volume: 45, Issue:3, 2017

Hypoxia as a therapy for mitochondrial disease.
Science (New York, N.Y.), , Apr-01, Volume: 352, Issue:6281, 2016

Hypoxia-inducible factor-1 plays a role in phosphate-induced vascular smooth muscle cell calcification.
Kidney international, , Volume: 90, Issue:3, 2016

Selective HIF stabilization alleviates hepatocellular steatosis and ballooning in a rodent model of 70% liver resection.
Clinical science (London, England : 1979), , 10-15, Volume: 135, Issue:19, 2021

HIF/Ca
Life sciences, , Jan-01, Volume: 264, 2021

Effect of Roxadustat on Factors Associated with Renal Fibrosis and Efficacy.
Computational and mathematical methods in medicine, , Volume: 2022, 2022

Anti-anemia drug FG4592 retards the AKI-to-CKD transition by improving vascular regeneration and antioxidative capability.
Clinical science (London, England : 1979), , 07-30, Volume: 135, Issue:14, 2021

Effects of orally active hypoxia inducible factor alpha prolyl hydroxylase inhibitor, FG4592 on renal fibrogenic potential in mouse unilateral ureteral obstruction model.
Journal of pharmacological sciences, , Volume: 142, Issue:3, 2020

HIF-α activation by the prolyl hydroxylase inhibitor roxadustat suppresses chemoresistant glioblastoma growth by inducing ferroptosis.
Cell death & disease, , 10-08, Volume: 13, Issue:10, 2022

Novel function of Roxadustat (FG-4592) as an anti-shock drug in sepsis by regulating mitochondrial oxidative stress and energy metabolism.
Biochimica et biophysica acta. General subjects, , Volume: 1867, Issue:1, 2023

Roxadustat prevents Ang II hypertension by targeting angiotensin receptors and eNOS.
JCI insight, , 09-22, Volume: 6, Issue:18, 2021

Does HIF-PHI increased risk of gastrointestinal hemorrhage in patients with renal anemia: a review of cases reported to the U.S. Food and drug administration adverse event reporting system.
Renal failure, , Volume: 43, Issue:1, 2021

Roxadustat Treatment for Anemia in Patients Undergoing Long-Term Dialysis.
The New England journal of medicine, , 09-12, Volume: 381, Issue:11, 2019

Roxadustat for Anemia in Patients with Kidney Disease Not Receiving Dialysis.
The New England journal of medicine, , 09-12, Volume: 381, Issue:11, 2019

Roxadustat prevents Ang II hypertension by targeting angiotensin receptors and eNOS.
JCI insight, , 09-22, Volume: 6, Issue:18, 2021

Roxadustat Treatment for Anemia in Patients Undergoing Long-Term Dialysis.
The New England journal of medicine, , 09-12, Volume: 381, Issue:11, 2019

Roxadustat: another drug that causes pulmonary hypertension? Report of first human case.
Polish archives of internal medicine, , 05-31, Volume: 129, Issue:5, 2019

A Prospective, Self-Controlled Pilot Study of the Efficacy of Roxadustat for Erythropoietin Hyporesponsiveness in Patients Requiring Chronic Ambulatory Peritoneal Dialysis.
Journal of renal nutrition : the official journal of the Council on Renal Nutrition of the National Kidney Foundation, , Volume: 32, Issue:5, 2022

Targeting Hypoxia-Inducible Factors for the Treatment of Anemia in Chronic Kidney Disease Patients.
American journal of nephrology, , Volume: 45, Issue:3, 2017

Roxadustat for anemia in patients with end-stage renal disease incident to dialysis.
Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association, , 08-27, Volume: 36, Issue:9, 2021

Roxadustat on anti-erythropoietin antibody-related pure red cell aplasia in the patient with end-stage renal disease.
Seminars in dialysis, , Volume: 34, Issue:4, 2021

Roxadustat for the Maintenance Treatment of Anemia in Patients with End-Stage Kidney Disease on Stable Dialysis: A European Phase 3, Randomized, Open-Label, Active-Controlled Study (PYRENEES).
Advances in therapy, , Volume: 38, Issue:10, 2021

Oral Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor Roxadustat (FG-4592) for Treatment of Anemia in Chronic Kidney Disease: A Placebo-Controlled Study of Pharmacokinetic and Pharmacodynamic Profiles in Hemodialysis Patients.
Journal of clinical pharmacology, , Volume: 60, Issue:11, 2020

Emerging treatments for anemia in patients with CKD and ESRD.
Nephrology news & issues, , Volume: 31, Issue:4, 2017

Targeting Hypoxia-Inducible Factors for the Treatment of Anemia in Chronic Kidney Disease Patients.
American journal of nephrology, , Volume: 45, Issue:3, 2017

Roxadustat (FG-4592) Versus Epoetin Alfa for Anemia in Patients Receiving Maintenance Hemodialysis: A Phase 2, Randomized, 6- to 19-Week, Open-Label, Active-Comparator, Dose-Ranging, Safety and Exploratory Efficacy Study.
American journal of kidney diseases : the official journal of the National Kidney Foundation, , Volume: 67, Issue:6, 2016

Hypoxia as a therapy for mitochondrial disease.
Science (New York, N.Y.), , Apr-01, Volume: 352, Issue:6281, 2016

Effect of Moderate Hepatic Impairment on the Pharmacokinetics and Pharmacodynamics of Roxadustat, an Oral Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor.
Clinical drug investigation, , Volume: 36, Issue:9, 2016

Targeting ineffective hematopoiesis in myelodysplastic syndromes.
American journal of hematology, , 02-01, Volume: 97, Issue:2, 2022

Roxadustat for the treatment of anemia in patients with lower-risk myelodysplastic syndrome: Open-label, dose-selection, lead-in stage of a phase 3 study.
American journal of hematology, , 02-01, Volume: 97, Issue:2, 2022

Clinical and Molecular Insights in Erythropoiesis Regulation of Signal Transduction Pathways in Myelodysplastic Syndromes and β-Thalassemia.
International journal of molecular sciences, , Jan-15, Volume: 22, Issue:2, 2021

New Approaches for Anemia in MDS.
Clinical lymphoma, myeloma & leukemia, , Volume: 20 Suppl 1, 2020

Roxadustat Markedly Reduces Myocardial Ischemia Reperfusion Injury in Mice.
Circulation journal : official journal of the Japanese Circulation Society, , 05-25, Volume: 84, Issue:6, 2020

Phase 3, Randomized, Double-Blind, Active-Comparator (Darbepoetin Alfa) Study of Oral Roxadustat in CKD Patients with Anemia on Hemodialysis in Japan.
Journal of the American Society of Nephrology : JASN, , Volume: 31, Issue:7, 2020

Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
Journal of medicinal chemistry, , 08-23, Volume: 61, Issue:16, 2018

Roxadustat promotes angiogenesis through HIF-1α/VEGF/VEGFR2 signaling and accelerates cutaneous wound healing in diabetic rats.
Wound repair and regeneration : official publication of the Wound Healing Society [and] the European Tissue Repair Society, , Volume: 27, Issue:4, 2019

Hypoxia-inducible factor prolyl hydroxylase inhibitor roxadustat (FG-4592) protects against cisplatin-induced acute kidney injury.
Clinical science (London, England : 1979), , 04-16, Volume: 132, Issue:7, 2018

Mononuclear phagocytes orchestrate prolyl hydroxylase inhibition-mediated renoprotection in chronic tubulointerstitial nephritis.
Kidney international, , Volume: 96, Issue:2, 2019

Roxadustat promotes osteoblast differentiation and prevents estrogen deficiency-induced bone loss by stabilizing HIF-1α and activating the Wnt/β-catenin signaling pathway.
Journal of orthopaedic surgery and research, , May-21, Volume: 17, Issue:1, 2022

Selective EGLN Inhibition Enables Ablative Radiotherapy and Improves Survival in Unresectable Pancreatic Cancer.
Cancer research, , 05-01, Volume: 79, Issue:9, 2019

On the Increased Event Rate of Urinary Tract Infection and Pneumonia in CKD Patients Treated with Roxadustat for Anemia.
Journal of the American Society of Nephrology : JASN, , 06-01, Volume: 32, Issue:6, 2021

FG-4592 protects the intestine from irradiation-induced injury by targeting the TLR4 signaling pathway.
Stem cell research & therapy, , 06-21, Volume: 13, Issue:1, 2022

FG-4592 alleviates radiation-induced intestinal injury by facilitating recovery of intestinal stem cell and reducing damage of intestinal epithelial.
Toxicology letters, , Mar-01, Volume: 357, 2022

Selective EGLN Inhibition Enables Ablative Radiotherapy and Improves Survival in Unresectable Pancreatic Cancer.
Cancer research, , 05-01, Volume: 79, Issue:9, 2019

Radioprotective effects of roxadustat (FG-4592) in haematopoietic system.
Journal of cellular and molecular medicine, , Volume: 23, Issue:1, 2019

Roxadustat Improves Erythropoietin Antibody-Mediated Pure Red Cell Aplasia in a Patient with Hemodialysis.
Blood purification, , Volume: 51, Issue:2, 2022

Roxadustat on anti-erythropoietin antibody-related pure red cell aplasia in the patient with end-stage renal disease.
Seminars in dialysis, , Volume: 34, Issue:4, 2021

Remarkable response to roxadustat in a case of anti-erythropoietin antibody-mediated pure red cell aplasia.
Annals of hematology, , Volume: 100, Issue:2, 2021

Resolution of epoetin-induced pure red cell aplasia, successful re-challenge with roxadustat.
International journal of laboratory hematology, , Volume: 42, Issue:6, 2020

Prolyl-4-Hydroxylases Inhibitor Stabilizes HIF-1α and Increases Mitophagy to Reduce Cell Death After Experimental Retinal Detachment.
Investigative ophthalmology & visual science, , Volume: 57, Issue:4, 2016

Phase 3, Randomized, Double-Blind, Active-Comparator (Darbepoetin Alfa) Study of Oral Roxadustat in CKD Patients with Anemia on Hemodialysis in Japan.
Journal of the American Society of Nephrology : JASN, , Volume: 31, Issue:7, 2020

Serine and 1-carbon metabolism are required for HIF-mediated protection against retinopathy of prematurity.
JCI insight, , 07-25, Volume: 4, Issue:14, 2019

Comparative systems pharmacology of HIF stabilization in the prevention of retinopathy of prematurity.
Proceedings of the National Academy of Sciences of the United States of America, , May-03, Volume: 113, Issue:18, 2016

Novel function of Roxadustat (FG-4592) as an anti-shock drug in sepsis by regulating mitochondrial oxidative stress and energy metabolism.
Biochimica et biophysica acta. General subjects, , Volume: 1867, Issue:1, 2023

Stabilization of HIF-1α by FG-4592 promotes functional recovery and neural protection in experimental spinal cord injury.
Brain research, , Feb-01, Volume: 1632, 2016

Hypoxia enhances tenocyte differentiation of adipose-derived mesenchymal stem cells by inducing hypoxia-inducible factor-1α in a co-culture system.
Cell proliferation, , Volume: 49, Issue:2, 2016

Roxadustat Does Not Affect Platelet Production, Activation, and Thrombosis Formation.
Arteriosclerosis, thrombosis, and vascular biology, , Volume: 41, Issue:10, 2021

Effects of orally active hypoxia inducible factor alpha prolyl hydroxylase inhibitor, FG4592 on renal fibrogenic potential in mouse unilateral ureteral obstruction model.
Journal of pharmacological sciences, , Volume: 142, Issue:3, 2020

Phase 3, Randomized, Double-Blind, Active-Comparator (Darbepoetin Alfa) Study of Oral Roxadustat in CKD Patients with Anemia on Hemodialysis in Japan.
Journal of the American Society of Nephrology : JASN, , Volume: 31, Issue:7, 2020

Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
Journal of medicinal chemistry, , 08-23, Volume: 61, Issue:16, 2018

Roxadustat (FG-4592) protects against ischaemia/reperfusion-induced acute kidney injury through inhibiting the mitochondrial damage pathway in mice.
Clinical and experimental pharmacology & physiology, , Volume: 49, Issue:2, 2022

Anti-anemia drug FG4592 retards the AKI-to-CKD transition by improving vascular regeneration and antioxidative capability.
Clinical science (London, England : 1979), , 07-30, Volume: 135, Issue:14, 2021

Reoxygenation induces reactive oxygen species production and ferroptosis in renal tubular epithelial cells by activating aryl hydrocarbon receptor.
Molecular medicine reports, , Volume: 23, Issue:1, 2021

Roxadustat Markedly Reduces Myocardial Ischemia Reperfusion Injury in Mice.
Circulation journal : official journal of the Japanese Circulation Society, , 05-25, Volume: 84, Issue:6, 2020

Can Pharmacological Ischemic Preconditioning Affect Myocardial Ischemic Injury?
Circulation journal : official journal of the Japanese Circulation Society, , 05-25, Volume: 84, Issue:6, 2020

Clinical and Molecular Insights in Erythropoiesis Regulation of Signal Transduction Pathways in Myelodysplastic Syndromes and β-Thalassemia.
International journal of molecular sciences, , Jan-15, Volume: 22, Issue:2, 2021

fg-4592

Description

Cross-References

Synonyms (67)

Roles (2)

Drug Classes (3)

Protein Targets (8)

Potency Measurements

Inhibition Measurements

Activation Measurements

Bioassays (123)

Research

Studies (188)

Study Types

Safety/Toxicity (10)

Long-term Use (2)

Pharmacokinetics (13)

Bioavailability (4)

Dosage (15)

Interactions (1)

Article	Year
Efficacy and Safety of Roxadustat in Patients with Chronic Kidney Disease: An Updated Meta-Analysis of Randomized Controlled Trials including 6,518 Patients. BioMed research international, , Volume: 2022	2022
Long-term efficacy, safety, and medication compliance of roxadustat on peritoneal dialysis patients with renal anemia affected by the COVID-19 pandemic: a retrospective study. Annals of palliative medicine, , Volume: 11, Issue:6	2022
The efficacy and safety of roxadustat for the treatment of anemia in non-dialysis dependent chronic kidney disease patients: An updated systematic review and meta-analysis of randomized clinical trials. PloS one, , Volume: 17, Issue:4	2022
Efficacy and safety of roxadustat in the treatment of renal allograft anemia patients: a case series. Annals of palliative medicine, , Volume: 10, Issue:11	2021
Efficacy and Cardiovascular Safety of Roxadustat in Dialysis-Dependent Chronic Kidney Disease: Pooled Analysis of Four Phase 3 Studies. Advances in therapy, , Volume: 38, Issue:10	2021
Efficacy and safety of roxadustat for anaemia in dialysis-dependent and non-dialysis-dependent chronic kidney disease patients: A systematic review and meta-analysis. British journal of clinical pharmacology, , Volume: 88, Issue:3	2022
The efficacy and safety of roxadustat treatment for anemia in patients with kidney disease: a meta-analysis and systematic review. International urology and nephrology, , Volume: 53, Issue:5	2021
The efficacy and safety of roxadustat for anemia in patients with chronic kidney disease: a meta-analysis. Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association, , 08-27, Volume: 36, Issue:9	2021
Effect of Multiple Doses of Omeprazole on the Pharmacokinetics, Safety, and Tolerability of Roxadustat in Healthy Subjects. European journal of drug metabolism and pharmacokinetics, , Volume: 43, Issue:6	2018
Roxadustat (FG-4592) Versus Epoetin Alfa for Anemia in Patients Receiving Maintenance Hemodialysis: A Phase 2, Randomized, 6- to 19-Week, Open-Label, Active-Comparator, Dose-Ranging, Safety and Exploratory Efficacy Study. American journal of kidney diseases : the official journal of the National Kidney Foundation, , Volume: 67, Issue:6	2016

Article	Year
Hypoxia-Inducible Factor Activators in Renal Anemia: Current Clinical Experience. Advances in chronic kidney disease, , Volume: 26, Issue:4	2019
Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors: A Potential New Treatment for Anemia in Patients With CKD. American journal of kidney diseases : the official journal of the National Kidney Foundation, , Volume: 69, Issue:6	2017

Article	Year
Pharmacokinetic/pharmacodynamic modeling of roxadustat's effect on LDL cholesterol in patients in Japan with dialysis-dependent chronic kidney disease and anemia. Drug metabolism and pharmacokinetics, , Volume: 46	2022
Liquid chromatography-tandem mass spectrometry methods for quantification of roxadustat (FG-4592) in human plasma and urine and the applications in two clinical pharmacokinetic studies. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, , Jul-01, Volume: 1203	2022
Effect of Roxadustat on the Pharmacokinetics of Simvastatin, Rosuvastatin, and Atorvastatin in Healthy Subjects: Results From 3 Phase 1, Open-Label, 1-Sequence, Crossover Studies. Clinical pharmacology in drug development, , Volume: 11, Issue:4	2022
Clinical Pharmacokinetics and Pharmacodynamics of Roxadustat. Clinical pharmacokinetics, , Volume: 61, Issue:3	2022
Population pharmacokinetics of roxadustat in Japanese dialysis-dependent chronic kidney disease patients with anaemia. British journal of clinical pharmacology, , Volume: 88, Issue:2	2022
Effect of the Phosphate Binders Sevelamer Carbonate and Calcium Acetate on the Pharmacokinetics of Roxadustat After Concomitant or Time-separated Administration in Healthy Individuals. Clinical therapeutics, , Volume: 43, Issue:6	2021
Pharmacokinetics of Roxadustat: A Population Analysis of 2855 Dialysis- and Non-Dialysis-Dependent Patients with Chronic Kidney Disease. Clinical pharmacokinetics, , Volume: 60, Issue:6	2021
Oral Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor Roxadustat (FG-4592) for Treatment of Anemia in Chronic Kidney Disease: A Placebo-Controlled Study of Pharmacokinetic and Pharmacodynamic Profiles in Hemodialysis Patients. Journal of clinical pharmacology, , Volume: 60, Issue:11	2020
Evaluation of Food and Spherical Carbon Adsorbent Effects on the Pharmacokinetics of Roxadustat in Healthy Nonelderly Adult Male Japanese Subjects. Clinical pharmacology in drug development, , Volume: 8, Issue:3	2019
Effect of Multiple Doses of Omeprazole on the Pharmacokinetics, Safety, and Tolerability of Roxadustat in Healthy Subjects. European journal of drug metabolism and pharmacokinetics, , Volume: 43, Issue:6	2018
Effect of Moderate Hepatic Impairment on the Pharmacokinetics and Pharmacodynamics of Roxadustat, an Oral Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor. Clinical drug investigation, , Volume: 36, Issue:9	2016
The Hypoxia-inducible Factor Prolyl-Hydroxylase Inhibitor Roxadustat (FG-4592) and Warfarin in Healthy Volunteers: A Pharmacokinetic and Pharmacodynamic Drug-Drug Interaction Study. Clinical therapeutics, , Volume: 38, Issue:4	2016
Randomized placebo-controlled dose-ranging and pharmacodynamics study of roxadustat (FG-4592) to treat anemia in nondialysis-dependent chronic kidney disease (NDD-CKD) patients. Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association, , Volume: 30, Issue:10	2015

fg-4592

Description

Cross-References

Synonyms (67)

Roles (2)

Drug Classes (3)

Protein Targets (8)

Potency Measurements

Inhibition Measurements

Activation Measurements

Bioassays (123)

Research

Studies (188)

Study Types

Related Drugs (1,046)

Drugs in this Class (972)

Drugs with this Function (3)

Drugs Involved in Assays Together (35)

Drugs Researched Together (42)

Related Conditions (136)

Safety/Toxicity (10)

Long-term Use (2)

Pharmacokinetics (13)

Bioavailability (4)

Dosage (15)

Interactions (1)