Page last updated: 2024-10-14

fg-4592

Description

roxadustat: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

roxadustat : An N-acylglycine resulting from the formal condensation of the amino group of glycine with the carboxy group of 4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxylic acid. It is an inhibitor of hypoxia inducible factor prolyl hydroxylase (HIF-PH). [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

FloraRankFlora DefinitionFamilyFamily Definition
GlycinegenusA non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.[MeSH]FabaceaeThe large family of plants characterized by pods. Some are edible and some cause LATHYRISM or FAVISM and other forms of poisoning. Other species yield useful materials like gums from ACACIA and various LECTINS like PHYTOHEMAGGLUTININS from PHASEOLUS. Many of them harbor NITROGEN FIXATION bacteria on their roots. Many but not all species of beans belong to this family.[MeSH]

Cross-References

ID SourceID
PubMed CID11256664
CHEMBL ID2338329
CHEBI ID132774
SCHEMBL ID523705
MeSH IDM0589156

Synonyms (67)

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

Toxicity

ExcerptReference
" Roxadustat was considered safe and well tolerated when administered alone or in combination with multiple daily oral doses of 40 mg omeprazole in healthy subjects."( Effect of Multiple Doses of Omeprazole on the Pharmacokinetics, Safety, and Tolerability of Roxadustat in Healthy Subjects.
Barroso-Fernandez, B; den Adel, M; El Galta, R; Golor, G; Groenendaal-van de Meent, D; Schaddelee, M; van Dijk, J, 2018
)
" As for safety, the incidence of adverse events (AEs) in the roxadustat group was insignificantly different from that of the placebo group [risk ratio (RR) 0."( The efficacy and safety of roxadustat for anemia in patients with chronic kidney disease: a meta-analysis.
Fu, X; Huang, Y; Liu, WJ; Liu, YN; Wang, Y; Wei, R; Yang, H; Zheng, Q, 2021
)
" No difference was found between roxadustat and control group in terms of oral iron supplementation, adverse events (AEs), serious adverse events (SAEs), infection, myocardial infraction, stroke, heart failure and death."( The efficacy and safety of roxadustat treatment for anemia in patients with kidney disease: a meta-analysis and systematic review.
Duan, K; Jiao, N; Li, J; Liu, G; Liu, Y; Qie, S, 2021
)
" Pooled safety endpoints included time to major adverse cardiovascular event (MACE; myocardial infarction, stroke, and all-cause mortality [ACM]) and MACE+ (MACE plus congestive heart failure or unstable angina requiring hospitalization), ACM, and treatment-emergent adverse events (TEAEs)."( Efficacy and Cardiovascular Safety of Roxadustat in Dialysis-Dependent Chronic Kidney Disease: Pooled Analysis of Four Phase 3 Studies.
Barratt, J; Csiky, B; Esposito, C; Reusch, M; Schömig, M; Sulowicz, W; Young, J, 2021
)
" The patients were followed up every 2 weeks, and the changes in their hemoglobin index and any adverse reactions were recorded during 10 weeks of treatment."( Efficacy and safety of roxadustat in the treatment of renal allograft anemia patients: a case series.
Li, J; Lv, J; Ma, K; Peng, W; Qi, H; Rao, Y; Wang, L, 2021
)
" Only one person showed symptoms of fatigue, and there were no other obvious adverse reactions reported."( Efficacy and safety of roxadustat in the treatment of renal allograft anemia patients: a case series.
Li, J; Lv, J; Ma, K; Peng, W; Qi, H; Rao, Y; Wang, L, 2021
)
"We concluded that ROX increased Hb level and improved iron utilization parameters in NDD-CKD patients, but ROX was associated with higher serious adverse effects, especially DVT and HTN."( 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.
Abbas, KS; Abdelazeem, B; El-Shahat, NA; Eltobgy, M; Kunadi, A; Malik, B; Savarapu, P; Shehata, J, 2022
)
" The Morisky Medication Adherence Scale-8 (MMAS-8) was used to score medication compliance during rhEPO treatment and roxadustat treatment, and adverse reactions occurred during treatment were collected."( 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.
Bao, L; Bian, X; Huang, J; Luo, C; Ren, L; Zhang, A, 2022
)
" There were no serious adverse events associated with roxadustat were observed."( 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.
Bao, L; Bian, X; Huang, J; Luo, C; Ren, L; Zhang, A, 2022
)
" In terms of safety, roxadustat treatment did not increase risk of total adverse events either in dialysis-dependent or not dialysis-dependent patients."( Efficacy and Safety of Roxadustat in Patients with Chronic Kidney Disease: An Updated Meta-Analysis of Randomized Controlled Trials including 6,518 Patients.
Lei, J; Li, H; Wang, S, 2022
)
" There was no significant difference in total adverse events compared with the control group."( Efficacy and Safety of Roxadustat in Patients with Chronic Kidney Disease: An Updated Meta-Analysis of Randomized Controlled Trials including 6,518 Patients.
Lei, J; Li, H; Wang, S, 2022
)

Pharmacokinetics

ExcerptReference
" Pharmacodynamic evaluation was performed in a subset of subjects."( Randomized placebo-controlled dose-ranging and pharmacodynamics study of roxadustat (FG-4592) to treat anemia in nondialysis-dependent chronic kidney disease (NDD-CKD) patients.
Besarab, A; Hemmerich, S; Hertel, J; Klaus, SJ; Lee, T; Leong, R; Neff, TB; Provenzano, R; Yu, KH; Zabaneh, R, 2015
)
" This clinical trial was designed to evaluate the effect of roxadustat on warfarin pharmacokinetic and pharmacodynamic parameters."( The Hypoxia-inducible Factor Prolyl-Hydroxylase Inhibitor Roxadustat (FG-4592) and Warfarin in Healthy Volunteers: A Pharmacokinetic and Pharmacodynamic Drug-Drug Interaction Study.
den Adel, M; Golor, G; Groenendaal-van de Meent, D; Kerbusch, V; Krebs-Brown, A; Rijnders, S; Schaddelee, M, 2016
)
" Pharmacokinetic and pharmacodynamic parameters were estimated via noncompartmental methods."( The Hypoxia-inducible Factor Prolyl-Hydroxylase Inhibitor Roxadustat (FG-4592) and Warfarin in Healthy Volunteers: A Pharmacokinetic and Pharmacodynamic Drug-Drug Interaction Study.
den Adel, M; Golor, G; Groenendaal-van de Meent, D; Kerbusch, V; Krebs-Brown, A; Rijnders, S; Schaddelee, M, 2016
)
"The geometric mean ratios and 90% CIs for Cmax and AUC∞ of total and unbound S- and R-warfarin (with and without roxadustat) were within the standard bioequivalence interval of 80."( The Hypoxia-inducible Factor Prolyl-Hydroxylase Inhibitor Roxadustat (FG-4592) and Warfarin in Healthy Volunteers: A Pharmacokinetic and Pharmacodynamic Drug-Drug Interaction Study.
den Adel, M; Golor, G; Groenendaal-van de Meent, D; Kerbusch, V; Krebs-Brown, A; Rijnders, S; Schaddelee, M, 2016
)
"Based on the lack of clinically significant pharmacokinetic interactions and the limited influence on warfarin pharmacodynamic parameters, no dose adjustment of warfarin should be required when coadministered with roxadustat."( The Hypoxia-inducible Factor Prolyl-Hydroxylase Inhibitor Roxadustat (FG-4592) and Warfarin in Healthy Volunteers: A Pharmacokinetic and Pharmacodynamic Drug-Drug Interaction Study.
den Adel, M; Golor, G; Groenendaal-van de Meent, D; Kerbusch, V; Krebs-Brown, A; Rijnders, S; Schaddelee, M, 2016
)
" Mean terminal half-life (t ½) appeared to be longer (17."( Effect of Moderate Hepatic Impairment on the Pharmacokinetics and Pharmacodynamics of Roxadustat, an Oral Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor.
Adel, MD; Alexiev, A; Groenendaal-van de Meent, D; Krebs-Brown, A; Mateva, L; Noukens, J; Rijnders, S; Schaddelee, M, 2016
)
" Maximum plasma concentration and area under the plasma concentration-time curve for patients receiving roxadustat were slightly more than dose proportional and elimination half-life ranged from 14."( 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.
Chou, J; Hemmerich, S; Neff, TB; Provenzano, R; Tumlin, J; Yu, KP; Zabaneh, R, 2020
)
" A population pharmacokinetic analysis was undertaken to evaluate the effect of intrinsic and extrinsic factors on roxadustat pharmacokinetics."( Pharmacokinetics of Roxadustat: A Population Analysis of 2855 Dialysis- and Non-Dialysis-Dependent Patients with Chronic Kidney Disease.
Åstrand, M; Bradley, C; Chou, J; Hamrén, B; Huang, J; Kerbusch-Herben, V; Någård, M; Rekić, D; Tannenbaum, S, 2021
)
"A population pharmacokinetic model was developed for the pharmacokinetics of roxadustat in the target population."( Pharmacokinetics of Roxadustat: A Population Analysis of 2855 Dialysis- and Non-Dialysis-Dependent Patients with Chronic Kidney Disease.
Åstrand, M; Bradley, C; Chou, J; Hamrén, B; Huang, J; Kerbusch-Herben, V; Någård, M; Rekić, D; Tannenbaum, S, 2021
)
" This study in healthy individuals investigated the effect of 2 PBs, sevelamer carbonate and calcium acetate, on the pharmacokinetic properties of a single oral dose of roxadustat administered concomitantly or with a time lag."( Effect of the Phosphate Binders Sevelamer Carbonate and Calcium Acetate on the Pharmacokinetics of Roxadustat After Concomitant or Time-separated Administration in Healthy Individuals.
Barroso-Fernandez, B; den Adel, M; Golor, G; Groenendaal-van de Meent, D; Kerbusch, V; Schaddelee, M; van Dijk, J, 2021
)
"Our objective was to develop a population pharmacokinetic (PK) model to describe roxadustat plasma concentrations in Japanese dialysis-dependent chronic kidney disease (DD-CKD) patients with renal anaemia and to identify the covariate factors that affect exposure of roxadustat."( Population pharmacokinetics of roxadustat in Japanese dialysis-dependent chronic kidney disease patients with anaemia.
Groenendaal-van de Meent, D; Komatsu, K; Shibata, T; Shiga, T; Takada, A, 2022
)
" This proposed method was fully validated and applied to the pharmacokinetic (PK) and pharmacodynamic (PD) study of roxadustat among healthy subjects in China."( 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.
Chen, X; Cui, X; Hu, P; Jiang, J; Liu, T; Zhao, Q; Zheng, X, 2022
)

Bioavailability

ExcerptReference
" Roxadustat (FG-4592) is an orally bioavailable hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitor that promotes coordinated erythropoiesis through HIF-mediated transcription."( Roxadustat (FG-4592): Correction of Anemia in Incident Dialysis Patients.
Besarab, A; Chan, DT; Chernyavskaya, E; Franco, M; Gurevich, K; Hemmerich, S; Kumbar, LM; Leong, R; Motylev, I; Neff, TB; Poole, L; Saikali, KG; Shutov, E; Yu, KH; Zhong, M, 2016
)
" These are potent, selective, orally bioavailable across several species, and active in stimulating erythropoiesis."( 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.
Clements, MJ; Debenham, JS; DeMartino, JA; Hajdu, R; Hale, JJ; Kuethe, JT; Lingham, RB; Madsen-Duggan, C; Miller, RR; Milligan, JA; Pang, J; Reibarkh, M; Salowe, SP; Sherer, EC; Sonatore, LM; Stickens, D; Tong, X; Visco, DM; Walsh, TF; Wolff, M; Zhou, D, 2016
)
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
"The roxadustat PK data in Japanese DD-CKD patients with renal anaemia were well described by a 2-compartment disposition model with first-order absorption and interindividual variability on clearance, central volume of distribution and absorption rate constant."( Population pharmacokinetics of roxadustat in Japanese dialysis-dependent chronic kidney disease patients with anaemia.
Groenendaal-van de Meent, D; Komatsu, K; Shibata, T; Shiga, T; Takada, A, 2022
)
" The identified key covariates included coadministration of PBs on the roxadustat bioavailability and age on clearance of roxadustat."( Population pharmacokinetics of roxadustat in Japanese dialysis-dependent chronic kidney disease patients with anaemia.
Groenendaal-van de Meent, D; Komatsu, K; Shibata, T; Shiga, T; Takada, A, 2022
)

Dosage Studied

ExcerptReference
"Of 116 subjects receiving treatment, 104 completed 4 weeks of dosing and 96 were evaluable for efficacy."( Randomized placebo-controlled dose-ranging and pharmacodynamics study of roxadustat (FG-4592) to treat anemia in nondialysis-dependent chronic kidney disease (NDD-CKD) patients.
Besarab, A; Hemmerich, S; Hertel, J; Klaus, SJ; Lee, T; Leong, R; Neff, TB; Provenzano, R; Yu, KH; Zabaneh, R, 2015
)
"8 h) in subjects with moderate hepatic impairment, however intersubject variability on apparent total systemic clearance after single oral dosing (CL/F), apparent volume of distribution at equilibrium after oral administration (V z/F) and t ½ was approximately twofold higher."( Effect of Moderate Hepatic Impairment on the Pharmacokinetics and Pharmacodynamics of Roxadustat, an Oral Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor.
Adel, MD; Alexiev, A; Groenendaal-van de Meent, D; Krebs-Brown, A; Mateva, L; Noukens, J; Rijnders, S; Schaddelee, M, 2016
)
" Primary outcomes for both studies were area under the concentration-time curve from the time of dosing extrapolated to infinity and maximum concentration of drug in blood plasma."( Evaluation of Food and Spherical Carbon Adsorbent Effects on the Pharmacokinetics of Roxadustat in Healthy Nonelderly Adult Male Japanese Subjects.
Furihata, K; Katashima, M; Nomura, Y; Shibata, T; Takada, A; Ueno, M; Yazawa, R, 2019
)
"A Study of Intermittent Oral Dosing of ASP1517 in Hemodialysis Chronic Kidney Disease Patients with Anemia, NCT02952092 (ClinicalTrials."( Phase 3, Randomized, Double-Blind, Active-Comparator (Darbepoetin Alfa) Study of Oral Roxadustat in CKD Patients with Anemia on Hemodialysis in Japan.
Akizawa, T; Iwasaki, M; Majikawa, Y; Reusch, M; Yamaguchi, Y, 2020
)
" Roxadustat induced transient elevations of endogenous erythropoietin that peaked between 7 and 14 hours after dosing and returned to baseline by 48 hours after dosing."( 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.
Chou, J; Hemmerich, S; Neff, TB; Provenzano, R; Tumlin, J; Yu, KP; Zabaneh, R, 2020
)
" Results from this study helped inform dosing and administration guidelines aimed at reducing interactions between roxadustat and these PBs."( Effect of the Phosphate Binders Sevelamer Carbonate and Calcium Acetate on the Pharmacokinetics of Roxadustat After Concomitant or Time-separated Administration in Healthy Individuals.
Barroso-Fernandez, B; den Adel, M; Golor, G; Groenendaal-van de Meent, D; Kerbusch, V; Schaddelee, M; van Dijk, J, 2021
)
" Dosage adjustments were administrated according to the fluctuation of hemoglobin level during the treatment."( Roxadustat for dialysis patients with erythropoietin hypo-responsiveness: a single-center, prospective investigation.
Chen, XX; Lou, JZ; Yuan, HB; Zhang, YF; Zhou, Y, 2021
)
" This post hoc analysis of a Japanese, open-label, partially randomized, phase 3 study in nondialysis-dependent (NDD) CKD patients treated with traditional erythropoiesis-stimulating agents (ESAs) evaluated dosing trends of roxadustat and darbepoetin alfa (DA) required to maintain target hemoglobin concentrations in patients with risk factors associated with ESA hyporesponsiveness."( Factors Affecting Doses of Roxadustat Versus Darbepoetin Alfa for Anemia in Nondialysis Patients.
Akizawa, T; Otsuka, T; Tanaka-Amino, K; Yamaguchi, Y, 2021
)
" Oral roxadustat dosed thrice weekly was well tolerated."( 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.
Bartels, P; Bradley, C; Carraway, HE; Glaspy, J; Harrup, R; Henry, DH; Leong, R; Mittelman, M; Modelska, K; Saha, G; Yu, KP; Zhou, A, 2022
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
EC 1.14.11.2 (procollagen-proline dioxygenase) inhibitorAn 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) inhibitorAn 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).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
isoquinolinesA class of organic heteropolycyclic compound consisting of isoquinoline and its substitution derivatives.
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
N-acylglycineAn N-acyl-amino acid in which amino acid specified is glycine.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
EWS/FLI fusion proteinHomo sapiens (human)Potency5.89920.001310.157742.8575AID1259252
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Prolyl 4-hydroxylaseParamecium bursaria Chlorella virus 1IC50 (µMol)5.00005.00006.26678.5000AID1543452
Prolyl 4-hydroxylaseParamecium bursaria Chlorella virus 1Ki1.07001.07002.17503.2800AID1543452
Prolyl 3-hydroxylase OGFOD1Homo sapiens (human)IC50 (µMol)1.00001.00001.00001.0000AID1543455
Alpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)IC50 (µMol)9.80003.00006.10009.8000AID734755
Egl nine homolog 1Homo sapiens (human)IC50 (µMol)0.88360.00701.86148.0000AID1280627; AID1497709; AID1497712; AID1543453; AID1576662; AID1675363; AID1735098; AID1884425; AID1901053; AID1910214
Hypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)IC50 (µMol)100.00008.60008.60008.6000AID1543454
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Thyroid hormone receptor alphaHomo sapiens (human)EC50 (µMol)0.03270.00040.25843.7400AID1910211
Thyroid hormone receptor betaHomo sapiens (human)EC50 (µMol)0.01290.00020.03480.2400AID1910212
Egl nine homolog 1Homo sapiens (human)EC50 (µMol)6.11006.11006.11006.1100AID1917455
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (67)

Processvia Protein(s)Taxonomy
cartilage condensationThyroid hormone receptor alphaHomo sapiens (human)
ossificationThyroid hormone receptor alphaHomo sapiens (human)
regulation of thyroid hormone mediated signaling pathwayThyroid hormone receptor alphaHomo sapiens (human)
regulation of transcription by RNA polymerase IIThyroid hormone receptor alphaHomo sapiens (human)
transcription by RNA polymerase IIThyroid hormone receptor alphaHomo sapiens (human)
learning or memoryThyroid hormone receptor alphaHomo sapiens (human)
regulation of heart contractionThyroid hormone receptor alphaHomo sapiens (human)
female courtship behaviorThyroid hormone receptor alphaHomo sapiens (human)
response to coldThyroid hormone receptor alphaHomo sapiens (human)
hormone-mediated signaling pathwayThyroid hormone receptor alphaHomo sapiens (human)
negative regulation of RNA polymerase II transcription preinitiation complex assemblyThyroid hormone receptor alphaHomo sapiens (human)
erythrocyte differentiationThyroid hormone receptor alphaHomo sapiens (human)
thyroid gland developmentThyroid hormone receptor alphaHomo sapiens (human)
regulation of myeloid cell apoptotic processThyroid hormone receptor alphaHomo sapiens (human)
negative regulation of DNA-templated transcriptionThyroid hormone receptor alphaHomo sapiens (human)
positive regulation of female receptivityThyroid hormone receptor alphaHomo sapiens (human)
regulation of lipid catabolic processThyroid hormone receptor alphaHomo sapiens (human)
type I pneumocyte differentiationThyroid hormone receptor alphaHomo sapiens (human)
positive regulation of cold-induced thermogenesisThyroid hormone receptor alphaHomo sapiens (human)
negative regulation of DNA-templated transcription initiationThyroid hormone receptor alphaHomo sapiens (human)
thyroid hormone mediated signaling pathwayThyroid hormone receptor alphaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIThyroid hormone receptor alphaHomo sapiens (human)
cell differentiationThyroid hormone receptor alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIThyroid hormone receptor alphaHomo sapiens (human)
retinoic acid receptor signaling pathwayThyroid hormone receptor alphaHomo sapiens (human)
positive regulation of thyroid hormone mediated signaling pathwayThyroid hormone receptor betaHomo sapiens (human)
DNA-templated transcriptionThyroid hormone receptor betaHomo sapiens (human)
sensory perception of soundThyroid hormone receptor betaHomo sapiens (human)
negative regulation of female receptivityThyroid hormone receptor betaHomo sapiens (human)
regulation of heart contractionThyroid hormone receptor betaHomo sapiens (human)
female courtship behaviorThyroid hormone receptor betaHomo sapiens (human)
mRNA transcription by RNA polymerase IIThyroid hormone receptor betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIThyroid hormone receptor betaHomo sapiens (human)
retinal cone cell developmentThyroid hormone receptor betaHomo sapiens (human)
type I pneumocyte differentiationThyroid hormone receptor betaHomo sapiens (human)
cellular response to thyroid hormone stimulusThyroid hormone receptor betaHomo sapiens (human)
retinal cone cell apoptotic processThyroid hormone receptor betaHomo sapiens (human)
retinoic acid receptor signaling pathwayThyroid hormone receptor betaHomo sapiens (human)
cell differentiationThyroid hormone receptor betaHomo sapiens (human)
thyroid hormone mediated signaling pathwayThyroid hormone receptor betaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIThyroid hormone receptor betaHomo sapiens (human)
regulation of translational terminationProlyl 3-hydroxylase OGFOD1Homo sapiens (human)
cell population proliferationProlyl 3-hydroxylase OGFOD1Homo sapiens (human)
protein hydroxylationProlyl 3-hydroxylase OGFOD1Homo sapiens (human)
peptidyl-proline hydroxylationProlyl 3-hydroxylase OGFOD1Homo sapiens (human)
stress granule assemblyProlyl 3-hydroxylase OGFOD1Homo sapiens (human)
temperature homeostasisAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
DNA alkylation repairAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
regulation of lipid storageAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
snRNA processingAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
regulation of multicellular organism growthAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
RNA repairAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
regulation of respiratory system processAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
adipose tissue developmentAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
mRNA destabilizationAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
regulation of white fat cell proliferationAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
regulation of brown fat cell differentiationAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
response to hypoxiaEgl nine homolog 1Homo sapiens (human)
intracellular iron ion homeostasisEgl nine homolog 1Homo sapiens (human)
intracellular oxygen homeostasisEgl nine homolog 1Homo sapiens (human)
negative regulation of DNA-binding transcription factor activityEgl nine homolog 1Homo sapiens (human)
regulation of angiogenesisEgl nine homolog 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIEgl nine homolog 1Homo sapiens (human)
negative regulation of cyclic-nucleotide phosphodiesterase activityEgl nine homolog 1Homo sapiens (human)
cardiac muscle tissue morphogenesisEgl nine homolog 1Homo sapiens (human)
heart trabecula formationEgl nine homolog 1Homo sapiens (human)
ventricular septum morphogenesisEgl nine homolog 1Homo sapiens (human)
labyrinthine layer developmentEgl nine homolog 1Homo sapiens (human)
response to nitric oxideEgl nine homolog 1Homo sapiens (human)
regulation of modification of postsynaptic structureEgl nine homolog 1Homo sapiens (human)
regulation protein catabolic process at postsynapseEgl nine homolog 1Homo sapiens (human)
peptidyl-proline hydroxylation to 4-hydroxy-L-prolineEgl nine homolog 1Homo sapiens (human)
cellular response to hypoxiaEgl nine homolog 1Homo sapiens (human)
positive regulation of myoblast differentiationHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
negative regulation of Notch signaling pathwayHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
negative regulation of DNA-templated transcriptionHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
positive regulation of vasculogenesisHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (39)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingThyroid hormone receptor alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificThyroid hormone receptor alphaHomo sapiens (human)
DNA-binding transcription factor activityThyroid hormone receptor alphaHomo sapiens (human)
nuclear receptor activityThyroid hormone receptor alphaHomo sapiens (human)
protein bindingThyroid hormone receptor alphaHomo sapiens (human)
zinc ion bindingThyroid hormone receptor alphaHomo sapiens (human)
TBP-class protein bindingThyroid hormone receptor alphaHomo sapiens (human)
protein domain specific bindingThyroid hormone receptor alphaHomo sapiens (human)
chromatin DNA bindingThyroid hormone receptor alphaHomo sapiens (human)
thyroid hormone bindingThyroid hormone receptor alphaHomo sapiens (human)
general transcription initiation factor bindingThyroid hormone receptor alphaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingThyroid hormone receptor alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificThyroid hormone receptor betaHomo sapiens (human)
transcription coactivator bindingThyroid hormone receptor betaHomo sapiens (human)
DNA bindingThyroid hormone receptor betaHomo sapiens (human)
DNA-binding transcription factor activityThyroid hormone receptor betaHomo sapiens (human)
nuclear receptor activityThyroid hormone receptor betaHomo sapiens (human)
protein bindingThyroid hormone receptor betaHomo sapiens (human)
zinc ion bindingThyroid hormone receptor betaHomo sapiens (human)
enzyme bindingThyroid hormone receptor betaHomo sapiens (human)
chromatin DNA bindingThyroid hormone receptor betaHomo sapiens (human)
thyroid hormone bindingThyroid hormone receptor betaHomo sapiens (human)
sequence-specific double-stranded DNA bindingThyroid hormone receptor betaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingThyroid hormone receptor betaHomo sapiens (human)
iron ion bindingProlyl 3-hydroxylase OGFOD1Homo sapiens (human)
protein bindingProlyl 3-hydroxylase OGFOD1Homo sapiens (human)
L-ascorbic acid bindingProlyl 3-hydroxylase OGFOD1Homo sapiens (human)
peptidyl-proline dioxygenase activityProlyl 3-hydroxylase OGFOD1Homo sapiens (human)
peptidyl-proline 3-dioxygenase activityProlyl 3-hydroxylase OGFOD1Homo sapiens (human)
ferrous iron bindingAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
transferase activityAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
oxidative RNA demethylase activityAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
broad specificity oxidative DNA demethylase activityAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
mRNA N6-methyladenosine dioxygenase activityAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
tRNA demethylase activityAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
protein bindingEgl nine homolog 1Homo sapiens (human)
ferrous iron bindingEgl nine homolog 1Homo sapiens (human)
2-oxoglutarate-dependent dioxygenase activityEgl nine homolog 1Homo sapiens (human)
enzyme bindingEgl nine homolog 1Homo sapiens (human)
L-ascorbic acid bindingEgl nine homolog 1Homo sapiens (human)
peptidyl-proline dioxygenase activityEgl nine homolog 1Homo sapiens (human)
hypoxia-inducible factor-proline dioxygenase activityEgl nine homolog 1Homo sapiens (human)
peptidyl-proline 4-dioxygenase activityEgl nine homolog 1Homo sapiens (human)
transcription corepressor activityHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
Notch bindingHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
protein bindingHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
ferrous iron bindingHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
zinc ion bindingHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
oxygen sensor activityHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
carboxylic acid bindingHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
peptidyl-histidine dioxygenase activityHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
[protein]-asparagine 3-dioxygenase activityHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
protein homodimerization activityHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
NF-kappaB bindingHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
peptidyl-aspartic acid 3-dioxygenase activityHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
ankyrin repeat bindingHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (14)

Processvia Protein(s)Taxonomy
nucleusThyroid hormone receptor alphaHomo sapiens (human)
nucleoplasmThyroid hormone receptor alphaHomo sapiens (human)
cytosolThyroid hormone receptor alphaHomo sapiens (human)
chromatinThyroid hormone receptor alphaHomo sapiens (human)
nucleusThyroid hormone receptor alphaHomo sapiens (human)
RNA polymerase II transcription regulator complexThyroid hormone receptor alphaHomo sapiens (human)
nucleoplasmThyroid hormone receptor betaHomo sapiens (human)
nuclear bodyThyroid hormone receptor betaHomo sapiens (human)
RNA polymerase II transcription regulator complexThyroid hormone receptor betaHomo sapiens (human)
chromatinThyroid hormone receptor betaHomo sapiens (human)
nucleusThyroid hormone receptor betaHomo sapiens (human)
nucleoplasmProlyl 3-hydroxylase OGFOD1Homo sapiens (human)
cytosolProlyl 3-hydroxylase OGFOD1Homo sapiens (human)
cytoplasmic stress granuleProlyl 3-hydroxylase OGFOD1Homo sapiens (human)
cytoplasmProlyl 3-hydroxylase OGFOD1Homo sapiens (human)
nucleusAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
nucleoplasmAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
cytoplasmAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
cytosolAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
plasma membraneAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
nuclear speckAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-ketoglutarate-dependent dioxygenase FTOHomo sapiens (human)
cytoplasmEgl nine homolog 1Homo sapiens (human)
cytosolEgl nine homolog 1Homo sapiens (human)
postsynaptic densityEgl nine homolog 1Homo sapiens (human)
intracellular membrane-bounded organelleEgl nine homolog 1Homo sapiens (human)
glutamatergic synapseEgl nine homolog 1Homo sapiens (human)
nucleusEgl nine homolog 1Homo sapiens (human)
cytoplasmEgl nine homolog 1Homo sapiens (human)
nucleusHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
nucleoplasmHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
cytoplasmHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
cytosolHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
perinuclear region of cytoplasmHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
cytoplasmHypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (123)

Assay IDTitleYearJournalArticle
AID1347157Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347169Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347161Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347167Vero cells viability qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347149Furin counterscreen qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347152Confirmatory screen NINDS AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347168HepG2 cells viability qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347153Confirmatory screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1675344In 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
AID1497731Intrinsic aqueous solubility of the compound at pH 7.4 by potentiometric titration method2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1497726Inhibition of HIF-PHD2 in human Hep3B cells assessed as HIF-1alpha protein stabilization at 50 to 250 uM after 10 hrs by Western blot method2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1910214Inhibition of PHD2 (unknown origin) incubated for 15 mins by competitive fluorescence polarization assay2022Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist.
AID1495354Terminal half life in patient with hepatic impairment at 100 mg, po2018Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
Discovery of novel 2-[(4-hydroxy-6-oxo-2,3-dihydro-1H-pyridine-5-carbonyl)amino]acetic acid derivatives as HIF prolyl hydroxylase inhibitors for treatment of renal anemia.
AID1067647Reduction in total cholesterol level in chronic kidney disease patient administered for 16 to 24 weeks relative to control2013Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23
Inhibition of hypoxia-inducible factor prolyl hydroxylase domain oxygen sensors: tricking the body into mounting orchestrated survival and repair responses.
AID1675363Inhibition of FITC-HIF1alpha (556 to 574 residues) binding to PHD2 (181 to 426 residues) (unknown origin) by fluorescence polarization assay
AID1917461Cytotoxicity against human Hep3B cells assessed as cell viability at 100 ug/ml measured by MTT assay2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues.
AID1901050Inhibition of PHD2 (unknown origin) at 1 uM measured by fluorescence polarization assay relative to control2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID1675362Selectivity 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
AID1497717Selectivity ratio of IC50 for JMJD2A (unknown origin) by Alphascreen assay to IC50 for HIF-PHD2 (181 to 426 residues) (unknown origin) by fluorescence polarization assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1543455Inhibition 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 analysis2019Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
Inhibition of a viral prolyl hydroxylase.
AID1901068Antiproliferative 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 assay2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID1497723Inhibition 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 control2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1497708Selectivity ratio of IC50 for JMJD3 (unknown origin) by Alphascreen assay to IC50 for HIF-PHD2 (181 to 426 residues) (unknown origin) by fluorescence polarization assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1910212Agonist 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 assay2022Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist.
AID1067648Antianemic 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 weeks2013Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23
Inhibition of hypoxia-inducible factor prolyl hydroxylase domain oxygen sensors: tricking the body into mounting orchestrated survival and repair responses.
AID1901071Nephroprotective activity against cisplatin-induced acute kidney injury in male C57BL/6 mouse assessed as serum EPO level at 10 mg/kg/day, ip2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID1917455Inhibition of PHD2 in human Hep3B cells assessed as increase in EPO production measured after 24 hrs by ELISA2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues.
AID1497718Cytotoxicity against human L02 cells assessed as reduction in cell viability at 10 to 100 uM after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1543452Inhibition 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 me2019Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
Inhibition of a viral prolyl hydroxylase.
AID1917752Induction of HIF-2alpha stabilization in human Hep3B cells assessed as HIF-1alpha level at 1 to 100 uM incubated for 24 hrs by immunoblot analysis2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Improving lipophilicity of 5-(1-acetyl-5-phenylpyrazolidin-3-ylidene)-1,3-dimethylbarbituric acid increases its efficacy to activate hypoxia-inducible factors.
AID1675357Selectivity 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
AID1497732Effective permeability of the compound at pH 7.4 by PAMPA2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1497728Inhibition of HIF-PHD2 in human Hep3B cells assessed as upregulation of EPO mRNA level at 50 uM after 10 hrs by RT-PCR method2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1675355Inhibition of PHD2 in human Hep3B cells assessed as upregulation of HIF-2alpha level after 10 hrs by Western blot analysis
AID1497719Cytotoxicity against human Hep3B cells assessed as reduction in cell viability at 10 to 100 uM after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1497713Inhibition 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 assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1497715Selectivity 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 assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1675360Selectivity 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
AID1917457Inhibition of PHD2 in human Hep3B cells assessed as stabilization of HIF-2alpha at 100 uM incubated for 4 hrs2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues.
AID1576662Inhibition of PHD2 (181 to 426 residues) (unknown origin) using FITC-HIF1alpha (556 to 574 residues) as substrate after 60 mins by fluorescence polarization assay2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Photoactivatable Prolyl Hydroxylase 2 Inhibitors for Stabilizing the Hypoxia-Inducible Factor with Light.
AID1067649Antianemic 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 control2013Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23
Inhibition of hypoxia-inducible factor prolyl hydroxylase domain oxygen sensors: tricking the body into mounting orchestrated survival and repair responses.
AID1067646Antianemic activity in human assessed as change in hemoglobin level administered thrice weekly for 12 weeks2013Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23
Inhibition of hypoxia-inducible factor prolyl hydroxylase domain oxygen sensors: tricking the body into mounting orchestrated survival and repair responses.
AID1497730Lipophilicity, log D of the compound at pH 7.4 by potentiometric titration method2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1917458Inhibition of PHD2 in human Hep3B cells assessed as stabilization of HIF-1alpha at 100 uM incubated for 4 hrs2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues.
AID1654632Substrate activity at aldehyde oxidase in human liver cytosol at 10 uM measured after 3 hrs by UPLC/Q-TOF MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model.
AID1884425Inhibition of PHD2 (181 to 426 residue) (unknown origin) measured by fluorescence polarization assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Tetrahydropyridin-4-ylpicolinoylglycines as novel and orally active prolyl hydroxylase 2 (PHD2) inhibitors for the treatment of renal anemia.
AID1675358Selectivity 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
AID1497729Dissociation constant, pKa of the compound by potentiometric titration method2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1917460Inhibition of PHD2 (unknown origin) at 66.7 uM relative to control2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues.
AID1354532Half life in human at 1 to 2 mg/kg, po administered as two or three times weekly2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
AID1497722Inhibition 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 control2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1497716Selectivity ratio of IC50 for JMJD1A (unknown origin) by Alphascreen assay to IC50 for HIF-PHD2 (181 to 426 residues) (unknown origin) by fluorescence polarization assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID734755Inhibition 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 analysis2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Structural basis for inhibition of the fat mass and obesity associated protein (FTO).
AID1917751Induction of HIF-1alpha stabilization in human Hep3B cells assessed as HIF-1alpha level at 1 to 100 uM incubated for 24 hrs by immunoblot analysis2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Improving lipophilicity of 5-(1-acetyl-5-phenylpyrazolidin-3-ylidene)-1,3-dimethylbarbituric acid increases its efficacy to activate hypoxia-inducible factors.
AID1354531Antianemic activity in human assessed as increase in hemoglobin level2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
AID1543454Inhibition 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 analysis2019Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
Inhibition of a viral prolyl hydroxylase.
AID1901053Inhibition of PHD2 (unknown origin) measured by fluorescence polarization assay2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID1675262Antianemic 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
AID1675350Inhibition 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
AID1901069Nephroprotective activity against cisplatin-induced acute kidney injury in male C57BL/6 mouse assessed as plasma BUN concentration at 10 mg/kg/day, ip2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID1917462Cytotoxicity against human Hep3B cells assessed as cell viability at 12.5 ug/ml measured by MTT assay2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues.
AID1675356Inhibition of PHD2 in human Hep3B cells assessed as upregulation of HIF-1alpha level after 10 hrs by Western blot analysis
AID1497721Cytotoxicity against HUVEC assessed as reduction in cell viability at 10 to 100 uM after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1901066Antiproliferative activity against human HK-2 cells assessed as decrease in cell viability at 100 uM measured after 24 hrs by CCK-8 assay2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID1497714Selectivity 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 assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1675343In 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
AID1675361Selectivity index, ratio of IC50 for PHD3 (unknown origin) to IC50 for PHD2 (unknown origin) by O-phenyl enediamine(OPD) based fluorescence assay
AID1901049Inhibition of PHD2 (unknown origin) at 0.5 uM measured by fluorescence polarization assay relative to control2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID1067650Antianemic activity in chronic kidney disease patient assessed as hemoglobin level administered for 4 weeks2013Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23
Inhibition of hypoxia-inducible factor prolyl hydroxylase domain oxygen sensors: tricking the body into mounting orchestrated survival and repair responses.
AID1910213Binding 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 assay2022Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist.
AID1497753Antianemic 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 control2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1497752Antianemic activity in C57BL/6 mouse cisplatin-induced anemia model assessed as increase in hemoglobin level administered po every other day for 30 days2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1497754Antianemic 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 control2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1901051Inhibition of PHD2 (unknown origin) at 10 uM measured by fluorescence polarization assay relative to control2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID1497709Inhibition 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 assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1543453Inhibition 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 analysis2019Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
Inhibition of a viral prolyl hydroxylase.
AID1675261Antianemic 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
AID1735098Inhibition of HIF-PHD2 (unknown origin)2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Discovery of N-[Bis(4-methoxyphenyl)methyl]-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide (MK-8617), an Orally Active Pan-Inhibitor of Hypoxia-Inducible Factor Prolyl Hydroxylase 1-3 (HIF PHD1-3) for the Treatment of Anemia.
AID1497720Cytotoxicity against HEK293 cells assessed as reduction in cell viability at 10 to 100 uM after 72 hrs by MTT assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1497751Upregulation of plasma EPO level in C57BL/6 mouse at 10 to 50 mg/kg, po after 4 hrs by ELISA2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1675359Selectivity 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
AID1280627Displacement of FITC-HIF-1alpha (556 to 574 residues) from PHD2 (181 to 426 residues) (unknown origin) after 60 mins by fluorescence polarization assay2015ACS medicinal chemistry letters, Dec-10, Volume: 6, Issue:12
Affinity-Based Fluorescence Polarization Assay for High-Throughput Screening of Prolyl Hydroxylase 2 Inhibitors.
AID1497712Inhibition 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 assay2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1497748Upregulation of plasma EPO level in C57BL/6 mouse at 10 mg/kg, iv after 4 hrs by ELISA2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1910211Agonist 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 assay2022Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist.
AID1901070Nephroprotective activity against cisplatin-induced acute kidney injury in male C57BL/6 mouse assessed as plasma SCr concentration at 10 mg/kg/day, ip2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID1497727Inhibition of HIF-PHD2 in human Hep3B cells assessed as HIF-2alpha protein stabilization at 50 to 250 uM after 10 hrs by Western blot method2018Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
AID1917456In 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 ELISA2022Bioorganic & medicinal chemistry letters, 11-15, Volume: 76Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues.
AID1675341Induction 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
AID1354533In 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 dose2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
AID1675285Antianemic activity in cisplatin-induced C57BL/6 mouse anemia model assessed as increase in haemoglobin level administered orally every other day for 1 month
AID1347411qHTS 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) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (188)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's59 (31.38)24.3611
2020's129 (68.62)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials30 (15.79%)5.53%
Reviews24 (12.63%)6.00%
Case Studies10 (5.26%)4.05%
Observational0 (0.00%)0.25%
Other126 (66.32%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]