Compounds > bay 85-3934
Page last updated: 2024-11-13

bay 85-3934

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID59603622
CHEMBL ID3646118
SCHEMBL ID6114312
SCHEMBL ID2569970
MeSH IDM000613289

Synonyms (52)

Synonym
molidustat [usan:inn]
1154028-82-6
9jh486cz13 ,
unii-9jh486cz13
molidustat [usan]
2-(6-(morpholin-4-yl)pyrimidin-4-yl)-4-(1h-1,2,3-triazol-1-yl)-1,2-dihydro-3h-pyrazol-3-one
molidustat ,
molidustat [inn]
who 9655
bay 85-3934
IJMBOKOTALXLKS-UHFFFAOYSA-N ,
2-(6-morpholin-4-ylpyrimidin-4-yl)-4-(1h-1,2,3-triazol-1-yl)-1,2-dihydro-3h-pyrazol-3-one
molidustat [who-dd]
3h-pyrazol-3-one, 1,2-dihydro-2-(6-(4-morpholinyl)-4-pyrimidinyl)-4-(1h-1,2,3-triazol-1-yl)-
bay-85-3934
bdbm118339
us8653111, 72
SCHEMBL6114312
SCHEMBL2569970
AC-35448
bay85-3934
bay-853934
2-(6-morpholin-4-ylpyrimidin-4-yl)-4-(triazol-1-yl)-1h-pyrazol-3-one
gtpl8456
HY-12654
CHEMBL3646118
DTXSID80151089 ,
AKOS026750584
EX-A562
molidustat(bay85-3934)
2-[6-(4-morpholinyl)-4-pyrimidinyl]-4-(1h-1,2,3-triazol-1-yl)-1,2-dihydro-3h-pyrazol-3-one
AS-74456
2-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1h-1,2,3-triazol-1-yl)-2,3-dihydro-1h-pyrazol-3-one
2-(6-morpholinopyrimidin-4-yl)-4-(1h-1,2,3-triazol-1-yl)-1h-pyrazol-3(2h)-one
mfcd28411428
NCGC00388364-04
3h-pyrazol-3-one, 1,2-dihydro-2-[6-(4-morpholinyl)-4-pyrimidinyl]-4-(1h-1,2,3-triazol-1-yl)-
molidustat(bay 85-3934)
2-(6-morpholin-4-ylpyrimidin-4-yl)-4-(1,2,3-triazol-1-yl)-1~{h}-pyrazol-3-one
a1h ,
molidustat (bay 85-3934)
S8138
Q27087553
BCP14477
molidustat;bay 85-3934;bay-85-3934; bay 853934; bay-853934; bay853934
1-(6-morpholinopyrimidin-4-yl)-4-(1h-1,2,3-triazol-1-yl)-1h-pyrazol-5-ol
SB17156
CCG-267626
2-(6-morpholin-4-ylpyrimidin-4-yl)-4-(1,2,3-triazol-1-yl)pyrazol-3-ol
qeq ,
molidustatum
dtxcid0073580

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The primary efficacy variable for both studies was change in blood hemoglobin (Hb) level from baseline to each post-baseline visit, and safety outcomes included adverse events (AEs)."( Long-Term Efficacy and Safety of Molidustat for Anemia in Chronic Kidney Disease: DIALOGUE Extension Studies.
Akizawa, T; Bernhardt, T; Berns, JS; Iekushi, K; Krueger, T; Macdougall, IC; Staedtler, G; Taguchi, M, 2019)		0.51
" The safety outcomes included evaluation of all adverse events."( Efficacy and Safety of Molidustat for Anemia in ESA-Naive Nondialysis Patients: A Randomized, Phase 3 Trial.
Akizawa, T; Hayasaki, T; Hayashi, Y; Matsuda, Y; Nobori, K; Yamamoto, H, 2021)		0.62
" The proportion of patients who reported at least 1 treatment-emergent adverse event (TEAE) was 93."( Efficacy and Safety of Molidustat for Anemia in ESA-Naive Nondialysis Patients: A Randomized, Phase 3 Trial.
Akizawa, T; Hayasaki, T; Hayashi, Y; Matsuda, Y; Nobori, K; Yamamoto, H, 2021)		0.62

Bioavailability

ExcerptReferenceRelevance
" Herein we describe the discovery, synthesis, structure-activity relationship (SAR), and proposed binding mode of novel 2,4-diheteroaryl-1,2-dihydro-3H-pyrazol-3-ones as orally bioavailable HIF-PH inhibitors for the treatment of anemia."( Discovery of Molidustat (BAY 85-3934): A Small-Molecule Oral HIF-Prolyl Hydroxylase (HIF-PH) Inhibitor for the Treatment of Renal Anemia.
Akbaba, M; Beck, H; Ergüden, JK; Flamme, I; Hartung, IV; Jeske, M; Karig, G; Keldenich, J; Militzer, HC; Oehme, F; Stoll, F; Thede, K; Thuss, U, 2018)		0.48
" Study 2 investigated the absolute bioavailability and pharmacodynamics of molidustat (part 1, n = 12; part 2, n = 16)."( Absorption, distribution, metabolism and excretion of molidustat in healthy participants.
Gerisch, M; Kaiser, A; Kern, A; Lentini, S; Matsuno, K; Thuss, U; van der Mey, D, 2020)		0.56

Dosage Studied

ExcerptRelevanceReference
" In repeat oral dosing of BAY 85-3934, hemoglobin levels were increased compared with animals that received vehicle, while endogenous EPO remained within the normal physiological range."( Mimicking hypoxia to treat anemia: HIF-stabilizer BAY 85-3934 (Molidustat) stimulates erythropoietin production without hypertensive effects.
Ellinghaus, P; Flamme, I; Jeske, M; Keldenich, J; Oehme, F; Thuss, U, 2014)		0.96
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency2.94110.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency2.94110.00339.158239.8107AID1347411
[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)26.80005.00006.26678.5000AID1543452
Prolyl 4-hydroxylaseParamecium bursaria Chlorella virus 1Ki16.05001.07002.17503.2800AID1543452
Prolyl 3-hydroxylase OGFOD1Homo sapiens (human)IC50 (µMol)1.00001.00001.00001.0000AID1543455
Prolyl hydroxylase EGLN2Homo sapiens (human)IC50 (µMol)0.48000.48001.40442.1000AID1354514
Egl nine homolog 1Homo sapiens (human)IC50 (µMol)0.29010.00701.86148.0000AID1280627; AID1280630; AID1354515; AID1543453; AID1916161
Prolyl hydroxylase EGLN3Homo sapiens (human)IC50 (µMol)0.45000.45000.45000.4500AID1354516
Hypoxia-inducible factor 1-alpha inhibitorHomo sapiens (human)IC50 (µMol)48.50008.60008.60008.6000AID1543454; AID1916162
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (63)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon 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)
regulation of cell growthProlyl hydroxylase EGLN2Homo sapiens (human)
response to hypoxiaProlyl hydroxylase EGLN2Homo sapiens (human)
peptidyl-proline hydroxylation to 4-hydroxy-L-prolineProlyl hydroxylase EGLN2Homo sapiens (human)
intracellular estrogen receptor signaling pathwayProlyl hydroxylase EGLN2Homo sapiens (human)
regulation of neuron apoptotic processProlyl hydroxylase EGLN2Homo sapiens (human)
cell redox homeostasisProlyl hydroxylase EGLN2Homo sapiens (human)
positive regulation of protein catabolic processProlyl hydroxylase EGLN2Homo sapiens (human)
cellular response to hypoxiaProlyl hydroxylase EGLN2Homo 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)
response to hypoxiaProlyl hydroxylase EGLN3Homo sapiens (human)
apoptotic processProlyl hydroxylase EGLN3Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processProlyl hydroxylase EGLN3Homo sapiens (human)
DNA damage responseProlyl hydroxylase EGLN3Homo sapiens (human)
protein hydroxylationProlyl hydroxylase EGLN3Homo sapiens (human)
regulation of cell population proliferationProlyl hydroxylase EGLN3Homo sapiens (human)
regulation of neuron apoptotic processProlyl hydroxylase EGLN3Homo sapiens (human)
cellular response to hypoxiaProlyl hydroxylase EGLN3Homo sapiens (human)
peptidyl-proline hydroxylation to 4-hydroxy-L-prolineProlyl hydroxylase EGLN3Homo 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 (25)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon 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)
protein bindingProlyl hydroxylase EGLN2Homo sapiens (human)
ferrous iron bindingProlyl hydroxylase EGLN2Homo sapiens (human)
2-oxoglutarate-dependent dioxygenase activityProlyl hydroxylase EGLN2Homo sapiens (human)
oxygen sensor activityProlyl hydroxylase EGLN2Homo sapiens (human)
L-ascorbic acid bindingProlyl hydroxylase EGLN2Homo sapiens (human)
peptidyl-proline 4-dioxygenase activityProlyl hydroxylase EGLN2Homo sapiens (human)
hypoxia-inducible factor-proline dioxygenase activityProlyl hydroxylase EGLN2Homo 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)
protein bindingProlyl hydroxylase EGLN3Homo sapiens (human)
2-oxoglutarate-dependent dioxygenase activityProlyl hydroxylase EGLN3Homo sapiens (human)
L-ascorbic acid bindingProlyl hydroxylase EGLN3Homo sapiens (human)
peptidyl-proline 4-dioxygenase activityProlyl hydroxylase EGLN3Homo sapiens (human)
hypoxia-inducible factor-proline dioxygenase activityProlyl hydroxylase EGLN3Homo sapiens (human)
ferrous iron bindingProlyl hydroxylase EGLN3Homo 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 (11)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon 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)
nucleusProlyl hydroxylase EGLN2Homo sapiens (human)
nucleoplasmProlyl hydroxylase EGLN2Homo sapiens (human)
nucleusProlyl hydroxylase EGLN2Homo sapiens (human)
cytoplasmProlyl hydroxylase EGLN2Homo 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)
nucleusProlyl hydroxylase EGLN3Homo sapiens (human)
nucleoplasmProlyl hydroxylase EGLN3Homo sapiens (human)
cytoplasmProlyl hydroxylase EGLN3Homo sapiens (human)
cytosolProlyl hydroxylase EGLN3Homo sapiens (human)
cytoplasmProlyl hydroxylase EGLN3Homo sapiens (human)
nucleusProlyl hydroxylase EGLN3Homo 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 (19)

Assay IDTitleYearJournalArticle
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.
AID1280630Inhibition of PHD2 (unknown origin) using biotinylated HIF-1alpha (558 to 574 residues) as substrate after 1 hr by homogeneous time-resolved fluorescence assay2015ACS medicinal chemistry letters, Dec-10, Volume: 6, Issue:12
Affinity-Based Fluorescence Polarization Assay for High-Throughput Screening of Prolyl Hydroxylase 2 Inhibitors.
AID1354521In vivo inhibition of PHD in Wistar rat assessed as increase in packed cell volume at 5 mg/kg, po measured after 26 days relative to control2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
AID1354516Inhibition of recombinant human HIF-PHD3 expressed in baculovirus-infected Sf9 cells using biotin labelled DLDLEMLAPYIPMDDDFQL as substrate preincubated for 60 mins followed by substrate addition measured after 60 mins by TR-FRET assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
AID1354520In vivo inhibition of PHD in Wistar rat assessed as increase in packed cell volume at 1.25 mg/kg, po measured after 26 days relative to control2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
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.
AID1354519Oral bioavailability in monkey2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
AID1916162Inhibition of FIH (unknown origin) by solid-phase extraction coupled to MS based assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Inhibition of the Oxygen-Sensing Asparaginyl Hydroxylase Factor Inhibiting Hypoxia-Inducible Factor: A Potential Hypoxia Response Modulating Strategy.
AID1916161Inhibition of N-terminal His tagged PHD2 (181 to 426 residues) (unknown origin) measured by MALDI-TOF MS analysis2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
Inhibition of the Oxygen-Sensing Asparaginyl Hydroxylase Factor Inhibiting Hypoxia-Inducible Factor: A Potential Hypoxia Response Modulating Strategy.
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.
AID1354517Oral bioavailability in Wistar rat2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
AID1354518Oral bioavailability in dog2018Journal 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.
AID1354514Inhibition of recombinant human HIF-PHD1 expressed in baculovirus-infected Sf9 cells using biotin labelled DLDLEMLAPYIPMDDDFQL as substrate preincubated for 60 mins followed by substrate addition measured after 60 mins by TR-FRET assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
AID1354515Inhibition of recombinant human HIF-PHD2 expressed in baculovirus-infected Sf9 cells using biotin labelled DLDLEMLAPYIPMDDDFQL as substrate preincubated for 60 mins followed by substrate addition measured after 60 mins by TR-FRET assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
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.
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.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS 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.
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 (37)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's15 (40.54)24.3611
2020's22 (59.46)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.48

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index18.48 (24.57)
Research Supply Index3.89 (2.92)
Research Growth Index4.74 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.48)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials11 (29.73%)5.53%
Reviews4 (10.81%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other22 (59.46%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
adenine
[no description available]		2.25106-aminopurines;
purine nucleobase		Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
citric acid, anhydrous
Citric Acid: A key intermediate in metabolism. It is an acid compound found in citrus fruits. The salts of citric acid (citrates) can be used as anticoagulants due to their calcium chelating ability.. citric acid : A tricarboxylic acid that is propane-1,2,3-tricarboxylic acid bearing a hydroxy substituent at position 2. It is an important metabolite in the pathway of all aerobic organisms.		2.2110tricarboxylic acidantimicrobial agent;
chelator;
food acidity regulator;
fundamental metabolite
glycine
[no description available]		5.6540alpha-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
oxaloacetic acid
Oxaloacetic Acid: A dicarboxylic acid ketone that is an important metabolic intermediate of the CITRIC ACID CYCLE. It can be converted to ASPARTIC ACID by ASPARTATE TRANSAMINASE.. oxaloacetic acid : An oxodicarboxylic acid that is succinic acid bearing a single oxo group.		2.2110C4-dicarboxylic acid;
oxo dicarboxylic acid		geroprotector;
metabolite
pyruvic acid
Pyruvic Acid: An intermediate compound in the metabolism of carbohydrates, proteins, and fats. In thiamine deficiency, its oxidation is retarded and it accumulates in the tissues, especially in nervous structures. (From Stedman, 26th ed). pyruvic acid : A 2-oxo monocarboxylic acid that is the 2-keto derivative of propionic acid. It is a metabolite obtained during glycolysis.		2.21102-oxo monocarboxylic acidcofactor;
fundamental metabolite
succinic acid
Succinic Acid: A water-soluble, colorless crystal with an acid taste that is used as a chemical intermediate, in medicine, the manufacture of lacquers, and to make perfume esters. It is also used in foods as a sequestrant, buffer, and a neutralizing agent. (Hawley's Condensed Chemical Dictionary, 12th ed, p1099; McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed, p1851). succinic acid : An alpha,omega-dicarboxylic acid resulting from the formal oxidation of each of the terminal methyl groups of butane to the corresponding carboxy group. It is an intermediate metabolite in the citric acid cycle.		2.2110alpha,omega-dicarboxylic acid;
C4-dicarboxylic acid		anti-ulcer drug;
fundamental metabolite;
micronutrient;
nutraceutical;
radiation protective agent
3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole
3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole: antineoplastic; activates platelet guanylate cyclase; a radiosensitizing agent and guanylate cyclase activator; structure in first source. lificiguat : A member of the class of indazoles that is 1H-indazole which is substituted by a benzyl group at position 1 and a 5-(hydroxymethyl)-2-furyl group at position 3. It is an activator of soluble guanylate cyclase and inhibits platelet aggregation.		2.1710aromatic primary alcohol;
furans;
indazoles		antineoplastic agent;
apoptosis inducer;
platelet aggregation inhibitor;
soluble guanylate cyclase activator;
vasodilator agent
indazoles
Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.		2.1710indazole
2,4-pyridinedicarboxylic acid
lutidinic acid : A pyridinedicarboxylic acid carrying carboxy groups at positions 2 and 4.		2.2110pyridinedicarboxylic acid
malondialdehyde
Malondialdehyde: The dialdehyde of malonic acid.. malonaldehyde : A dialdehyde that is propane substituted by two oxo groups at the terminal carbon atoms respectively. A biomarker of oxidative damage to lipids caused by smoking, it exists in vivo mainly in the enol form.		2.1710dialdehydebiomarker
daminozide
daminozide: induces tumors		2.2110straight-chain fatty acid
glutamic acid
Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.		2.2110glutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		12.8133131,2,3-triazole
atazanavir sulfate
Atazanavir Sulfate: An azapeptide and HIV-PROTEASE INHIBITOR that is used in the treatment of HIV INFECTIONS and AIDS in combination with other ANTI-HIV AGENTS.		2.3110organic sulfate salt
d-2-hydroxyglutarate
(R)-2-hydroxyglutaric acid : The (R)-enantiomer of 2-hydroxyglutaric acid.		3.76202-hydroxyglutaric acidalgal metabolite
alpha-hydroxyglutarate, (l)-isomer
[no description available]		3.76202-hydroxyglutaric acid
fumaric acid
fumaric acid: see also record for ferrous fumarate; use FUMARATES for general fumaric acid esters. fumaric acid : A butenedioic acid in which the C=C double bond has E geometry. It is an intermediate metabolite in the citric acid cycle.		2.2110butenedioic acidfood acidity regulator;
fundamental metabolite;
geroprotector
5-carboxy-8-hydroxyquinoline
5-carboxy-8-hydroxyquinoline: a JmjC histone demethylase inhibitor; structure in first source		2.2110quinolines
aconitic acid
cis-aconitic acid : The cis-isomer of aconitic acid.		2.2110aconitic acidfundamental metabolite
oxalylglycine
oxalylglycine: structure given in first source. N-oxalylglycine : An amino dicarboxylic acid that is iminodiacetic acid with an oxo substituent. It is used as an inhibitor of alpha-ketoglutarate dependent (EC 1.14.11.*) enzymes.		3.7620amino 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
fg-4592
roxadustat: structure in first source. 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).		6.4370aromatic ether;
isoquinolines;
N-acylglycine		EC 1.14.11.2 (procollagen-proline dioxygenase) inhibitor;
EC 1.14.11.29 (hypoxia-inducible factor-proline dioxygenase) inhibitor
losartan potassium
Erythropoietin: Glycoprotein hormone, secreted chiefly by the KIDNEY in the adult and the LIVER in the FETUS, that acts on erythroid stem cells of the BONE MARROW to stimulate proliferation and differentiation.		8.4294
2-[[[4-hydroxy-2-oxo-1-(phenylmethyl)-3-quinolinyl]-oxomethyl]amino]acetic acid
[no description available]		2.2110quinolines
3-[[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)-4-pyrimidinyl]amino]propanoic acid
[no description available]		2.2110organonitrogen heterocyclic compound
gsk1278863
GSK1278863: a HIF prolyl hydroxylase inhibitor. daprodustat : A member of the class of barbiturates that is barbituric acid substituted by cyclohexyl groups at positions 1 and 3, and by a (carboxymethyl)aminocarbonyl group at position 5. It is an inhibitor of hypoxia-inducible factor prolyl hydroxylase developed by GlaxoSmithKline for the treatment of anaemia in patients with chronic kidney disease.		5.7430
adrenomedullin
Adrenomedullin: A 52-amino acid peptide with multi-functions. It was originally isolated from PHEOCHROMOCYTOMA and ADRENAL MEDULLA but is widely distributed throughout the body including lung and kidney tissues. Besides controlling fluid-electrolyte homeostasis, adrenomedullin is a potent vasodilator and can inhibit pituitary ACTH secretion.		2.1710
epoetin alfa
Epoetin Alfa: A recombinant glycosylated form of erythropoietin which stimulates the differentiation and proliferation of erythroid precursors. It is used for the treatment of ANEMIA associated with CHRONIC RENAL FAILURE in dialysis and predialysis patients.		3.5911
ConditionIndicatedRelationship StrengthStudiesTrials
Genetic Diseases
[description not available]		03.0910
Chronic Kidney Diseases
[description not available]		013.562721
Benign Neoplasms
[description not available]		03.0910
Bowel Diseases, Inflammatory
[description not available]		03.0910
Anemia
A reduction in the number of circulating ERYTHROCYTES or in the quantity of HEMOGLOBIN.		013.992922
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		03.0910
Inflammatory Bowel Diseases
Chronic, non-specific inflammation of the GASTROINTESTINAL TRACT. Etiology may be genetic or environmental. This term includes CROHN DISEASE and ULCERATIVE COLITIS.		03.0910
Genetic Diseases, Inborn
Diseases that are caused by genetic mutations present during embryo or fetal development, although they may be observed later in life. The mutations may be inherited from a parent's genome or they may be acquired in utero.		03.0910
Renal Insufficiency, Chronic
Conditions in which the KIDNEYS perform below the normal level for more than three months. Chronic kidney insufficiency is classified by five stages according to the decline in GLOMERULAR FILTRATION RATE and the degree of kidney damage (as measured by the level of PROTEINURIA). The most severe form is the end-stage renal disease (CHRONIC KIDNEY FAILURE). (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002)		013.562721
HbS Disease
[description not available]		02.3110
Alloxan Diabetes
[description not available]		02.3110
Diabetes Mellitus, Adult-Onset
[description not available]		02.3110
Insulin Sensitivity
[description not available]		02.3110
Anemia, Sickle Cell
A disease characterized by chronic hemolytic anemia, episodic painful crises, and pathologic involvement of many organs. It is the clinical expression of homozygosity for hemoglobin S.		02.3110
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.		02.3110
Insulin Resistance
Diminished effectiveness of INSULIN in lowering blood sugar levels: requiring the use of 200 units or more of insulin per day to prevent HYPERGLYCEMIA or KETOSIS.		02.3110
Diabetic Cardiomyopathies
Diabetes complications in which VENTRICULAR REMODELING in the absence of CORONARY ATHEROSCLEROSIS and hypertension results in cardiac dysfunctions, typically LEFT VENTRICULAR DYSFUNCTION. The changes also result in myocardial hypertrophy, myocardial necrosis and fibrosis, and collagen deposition due to impaired glucose tolerance.		02.3110
Chronic Illness
[description not available]		03.9911
Chronic Disease
Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).		03.9911
Breast Cancer
[description not available]		02.2510
Breast Neoplasms
Tumors or cancer of the human BREAST.		02.2510
Acute Kidney Failure
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		04.0440
Acute Kidney Injury
Abrupt reduction in kidney function. Acute kidney injury encompasses the entire spectrum of the syndrome including acute kidney failure; ACUTE KIDNEY TUBULAR NECROSIS; and other less severe conditions.		02.2510
Blood Pressure, High
[description not available]		02.3110
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		02.3110
Anoxemia
[description not available]		02.6620
Hypoxia
Sub-optimal OXYGEN levels in the ambient air of living organisms.		02.6620
Koch's Disease
[description not available]		02.3110
Tuberculosis
Any of the infectious diseases of man and other animals caused by species of MYCOBACTERIUM TUBERCULOSIS.		02.3110
Injury, Ischemia-Reperfusion
[description not available]		02.1710
Reperfusion Injury
Adverse functional, metabolic, or structural changes in tissues that result from the restoration of blood flow to the tissue (REPERFUSION) following ISCHEMIA.		02.1710
Kidney Diseases
Pathological processes of the KIDNEY or its component tissues.		02.1710
Innate Inflammatory Response
[description not available]		03.0610
Chronic Kidney Failure
[description not available]		03.0610
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		03.0610
Kidney Failure, Chronic
The end-stage of CHRONIC RENAL INSUFFICIENCY. It is characterized by the severe irreversible kidney damage (as measured by the level of PROTEINURIA) and the reduction in GLOMERULAR FILTRATION RATE to less than 15 ml per min (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002). These patients generally require HEMODIALYSIS or KIDNEY TRANSPLANTATION.		03.0610