Compounds > GS-441524
Page last updated: 2024-11-13

GS-441524

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 CID44468216
CHEMBL ID2016757
CHEBI ID147281
SCHEMBL ID10120689

Synonyms (48)

Synonym
c12h13n5o4
gs-441524 ,
evo 984
(2r,3r,4s,5r)-2-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile
gs 441524
evo-984
evo984
1191237-69-0
gs441524
CHEBI:147281
CHEMBL2016757
S6814
SCHEMBL10120689
AC-31365
D78523
BRDWIEOJOWJCLU-LTGWCKQJSA-N
HY-103586
BS-14744
gs 441524 [who-dd]
BCP29949-1
EX-A3056
(2r,3r,4s,5r)-2-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)oxolane-2-carbonitrile
1bqk176dt6 ,
d-altrononitrile, 2-c-(4-aminopyrrolo(2,1-f)(1,2,4)triazin-7-yl)-2,5-anhydro-
(2r,3r,4s,5r)-2-(4-aminopyrrolo(2,1-f)(1,2,4)triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydro-2-furancarbonitrile
unii-1bqk176dt6
2-c-(4-aminopyrrolo(2,1-f)(1,2,4)triazin-7-yl)-2,5-anhydro-d-altrononitrile
(2~{r},3~{r},4~{s},5~{r})-2-(4-azanylpyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-(hydroxymethyl)-3,4-bis(oxidanyl)oxolane-2-carbonitrile
u08 ,
C22275
reacted form
(2r,3r,4s,5r)-2-{4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl}-3,4-dihydroxy-5-(hydroxymethyl)oxolane-2-carbonitrile
CS-0028160
A933921
mfcd32666994
remdesivir metabolite(gs-441524)
2-c-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-d-altrononitrile
remdesivir related compound 6 (gs-441524)
ZB1788
AKOS037648588
gtpl11445
DTXSID201028047
(2r,3r,4s,5r)-2-(4-aminopyrrolo[2,1-f][1,2,4]triazine-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)oxolane-2-carbonitrile
(2r,3r,4s,5r)-2-(4-aminopyrrolo[1,2-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile
remdesivir intermediate(gs-441524)
EN300-26870141
bdbm50571531
Z3952165305

Research Excerpts

Pharmacokinetics

To study the pharmacokinetic inter-individual variability of remdesivir and its main metabolite GS-441524 in a real-world setting of COVID-19 inpatients. To identify possible associations with different demographic/biochemical variables.

ExcerptReferenceRelevance
" In spite of United States Food and Drug Administration's recent assent of remdesivir as the only approved agent for COVID-19, there is limited information available about the physicochemical, metabolism, transport, pharmacokinetic (PK), and drug-drug interaction (DDI) properties of this drug."( Simulation of Remdesivir Pharmacokinetics and Its Drug Interactions.
Deb, S; Reeves, AA, 2021)		0.62
" Physiologically based pharmacokinetic (PBPK) modeling of GastroPlus was used to simulate different patient populations based on age, weight, liver function, and renal function status."( Simulation of Remdesivir Pharmacokinetics and Its Drug Interactions.
Deb, S; Reeves, AA, 2021)		0.62
"7%, respectively) in mice, which provided good insight into the pharmacokinetic optimization of GS-441524."( Potency and pharmacokinetics of GS-441524 derivatives against SARS-CoV-2.
Aisa, HA; Hu, T; Shen, J; Wei, D; Xie, Y; Xue, H; Zhang, Y; Zheng, W, 2021)		1.12
" Here, we evaluated GS-441524 for Covid-19 treatment based on studies reporting pharmacokinetic parameters of the agent in mice, rats, cats, dogs, monkeys, and the single individual in the first-in-human trial supplemented with information about its activity against severe acute respiratory syndrome coronavirus 2 and safety."( Nucleoside analog GS-441524: pharmacokinetics in different species, safety, and potential effectiveness against Covid-19.
Hansen, PR; Rasmussen, HB; Thomsen, R, 2022)		1.38
" A prospective observational pharmacokinetic study was performed in non-critically ill hospitalized COVID-19 patients with hypoxemia."( Population Pharmacokinetics of Remdesivir and GS-441524 in Hospitalized COVID-19 Patients.
Bosma, LBE; Leegwater, E; Moes, DJAR; Ottens, TH; van der Meer, IM; van Nieuwkoop, C; Wilms, EB, 2022)		0.98
"To study the pharmacokinetic inter-individual variability of remdesivir and its main metabolite GS-441524 in a real-world setting of COVID-19 inpatients and to identify possible associations with different demographic/biochemical variables."( Interpatient variability in the pharmacokinetics of remdesivir and its main metabolite GS-441524 in treated COVID-19 subjects.
Agrati, C; Ascoli Bartoli, T; Benvenuto, D; Marchioni, L; Nicastri, E; Stazi, GV; Tempestilli, M, 2022)		1.16
" Linear regression, logistic regression and multiple linear regression tests were used for statistical comparisons of pharmacokinetic parameters and variables."( Interpatient variability in the pharmacokinetics of remdesivir and its main metabolite GS-441524 in treated COVID-19 subjects.
Agrati, C; Ascoli Bartoli, T; Benvenuto, D; Marchioni, L; Nicastri, E; Stazi, GV; Tempestilli, M, 2022)		0.94

Compound-Compound Interactions

ExcerptReferenceRelevance
" In spite of United States Food and Drug Administration's recent assent of remdesivir as the only approved agent for COVID-19, there is limited information available about the physicochemical, metabolism, transport, pharmacokinetic (PK), and drug-drug interaction (DDI) properties of this drug."( Simulation of Remdesivir Pharmacokinetics and Its Drug Interactions.
Deb, S; Reeves, AA, 2021)		0.62
" Subsequently, these data were used in the Drug-Drug Interaction module to simulate drug interaction potential of remdesivir with other COVID-19 drug regimens and with agents used for comorbidities."( Simulation of Remdesivir Pharmacokinetics and Its Drug Interactions.
Deb, S; Reeves, AA, 2021)		0.62

Bioavailability

Oral-dosed ATV041 resulted in favorable bioavailability and rapid tissue distribution of GS-441524 and ibuprofen. However, the low oral bioavailability poses a challenge to its anti-SARS-CoV-2 efficacy.

ExcerptReferenceRelevance
" Potent orally bioavailable antiviral drugs for early treatment of SARS-CoV-2 infection are urgently needed, and several, including molnupiravir and PF-07321332, are currently in clinical development."( Rethinking Remdesivir: Synthesis, Antiviral Activity, and Pharmacokinetics of Oral Lipid Prodrugs.
Beadle, JR; Carlin, AF; Clark, AE; Garretson, AF; Hostetler, KY; Leibel, SL; McMillan, RE; McVicar, RN; Murphy, J; Schooley, RT; Smith, VI; Valiaeva, N; Xie, J; Zhang, XQ, 2021)		0.62
" However, this nucleoside has a poor oral bioavailability in non-human primates, which may affect its therapeutic efficacy."( Potency and pharmacokinetics of GS-441524 derivatives against SARS-CoV-2.
Aisa, HA; Hu, T; Shen, J; Wei, D; Xie, Y; Xue, H; Zhang, Y; Zheng, W, 2021)		0.9
" An orally bioavailable remdesivir analog may boost therapeutic benefit by facilitating early administration to non-hospitalized patients."( Oral prodrug of remdesivir parent GS-441524 is efficacious against SARS-CoV-2 in ferrets.
Babusis, D; Barrett, KT; Bilello, JP; Chan, J; Chun, K; Cihlar, T; Cox, RM; DuPont, V; Greninger, AL; Kalla, R; Lieber, CM; Lin, MJ; Lye, D; Mackman, RL; Martinez-Sobrido, L; Plemper, RK; Sourimant, J; Wolf, JD; Ye, C, 2021)		0.9
" Using different presumptions, we estimated human oral bioavailability of GS-441524 at 13% and 20%."( Nucleoside analog GS-441524: pharmacokinetics in different species, safety, and potential effectiveness against Covid-19.
Hansen, PR; Rasmussen, HB; Thomsen, R, 2022)		1.29
" In vivo, African green monkeys (AGM) orally dosed with GS-441524 yielded low plasma levels due to limited oral bioavailability of <10%."( Intravenous delivery of GS-441524 is efficacious in the African green monkey model of SARS-CoV-2 infection.
Babusis, D; Bannister, R; Barrett, K; Bilello, JP; Cihlar, T; Kajon, A; Lu, X; Lye, D; Ma, B; Mackman, R; Pitts, J; Porter, DP; Riola, N; Shi, PY; Smith, BJ; Subramanian, R; Toteva, M; Vermillion, MS; Xie, X; Zhao, X, 2022)		1.27
" However, the low oral bioavailability of GS-441524 poses a challenge to its anti-SARS-CoV-2 efficacy."( Oral GS-441524 derivatives: Next-generation inhibitors of SARS-CoV-2 RNA-dependent RNA polymerase.
Song, XQ; Wang, Z; Yang, L, 2022)		1.5
" Oral-dosed ATV041 resulted in favorable bioavailability and rapid tissue distribution of GS-441524 and ibuprofen."( Nonsteroidal anti-inflammatory drugs (NSAIDs) and nucleotide analog GS-441524 conjugates with potent in vivo efficacy against coronaviruses.
Chen, Q; Cong, F; Li, Y; Luo, Y; Qiu, J; Zhang, X; Zhou, Q; Zhu, Y, 2023)		1.37

Dosage Studied

African green monkeys (AGM) orally dosed with GS-441524 yielded low plasma levels due to limited oral bioavailability of <10%. An induction dosage of remdesivir 10 to 15 mg/kg intravenously or subcutaneously q24h was utilized for 4 doses.

ExcerptRelevanceReference
" We describe utilizing the recall antigen assay platform to screen small molecule drug off-target effects on memory T cell expansion/function using a dosing regimen based on adenosine treatment."( Adenosine-related small molecules show utility of recall antigen assay to screen compounds for off-target effects on memory T cells.
Daftarian, PM; George, MV; Kleiman, E; Magcase, D; Mao, B; Sierra, G, 2021)		0.62
" We found that mean (standard deviation) recovery of RDV at 6 hours after dosing was low in both the ECMO (33."( Remdesivir and GS-441524 Extraction by Ex Vivo Extracorporeal Life Support Circuits.
Green, DJ; Imburgia, CE; Kelley, WE; Mcknite, AM; Reilly, CA; Rower, JE; Watt, KM, 2022)		1.07
" A dosing interval of 8 h was considered clinically relevant and used to calculate steady-state plasma concentrations of GS-441524."( Nucleoside analog GS-441524: pharmacokinetics in different species, safety, and potential effectiveness against Covid-19.
Hansen, PR; Rasmussen, HB; Thomsen, R, 2022)		1.26
" In vivo, African green monkeys (AGM) orally dosed with GS-441524 yielded low plasma levels due to limited oral bioavailability of <10%."( Intravenous delivery of GS-441524 is efficacious in the African green monkey model of SARS-CoV-2 infection.
Babusis, D; Bannister, R; Barrett, K; Bilello, JP; Cihlar, T; Kajon, A; Lu, X; Lye, D; Ma, B; Mackman, R; Pitts, J; Porter, DP; Riola, N; Shi, PY; Smith, BJ; Subramanian, R; Toteva, M; Vermillion, MS; Xie, X; Zhao, X, 2022)		1.27
" Alternative dosing regimens were evaluated using Monte Carlo simulations."( Population Pharmacokinetics of Remdesivir and GS-441524 in Hospitalized COVID-19 Patients.
Bosma, LBE; Leegwater, E; Moes, DJAR; Ottens, TH; van der Meer, IM; van Nieuwkoop, C; Wilms, EB, 2022)		0.98
" We conducted animal trials in three dosing groups and found that while GS441524 can effectively reducing the mortality of FIP subjects at a range of doses, GC376 only reducing the mortality rate at high doses."( Better therapeutic effect of oral administration of GS441524 compared with GC376.
Chen, Y; Jiao, Z; Li, J; Li, L; Li, M; Peng, G; Shen, Z; Shi, Y; Wang, G; Yan, Y; Yang, M, 2023)		0.91
"Cats received treatment with different combinations of IV remdesivir, SC remdesivir, and PO GS-441524 at a median (range) dosage of 15 (10-20) mg/kg."( Thirty-two cats with effusive or non-effusive feline infectious peritonitis treated with a combination of remdesivir and GS-441524.
Green, J; Syme, H; Tayler, S, )		0.56
" An induction dosage of remdesivir 10 to 15 mg/kg intravenously or subcutaneously q24h was utilized for 4 doses, with a maintenance dosage of remdesivir (6-15 mg/kg SC) or GS-441524 (10-15 mg/kg per os) every 24 hours continued for at least 84 days."( Outcomes of treatment of cats with feline infectious peritonitis using parenterally administered remdesivir, with or without transition to orally administered GS-441524.
Coggins, SJ; Govendir, M; Hall, EJ; Kimble, B; Malik, R; Norris, JM; Thompson, MF, )		0.52
" Remission was achieved in all 3 after higher dosing (15-20 mg/kg)."( Outcomes of treatment of cats with feline infectious peritonitis using parenterally administered remdesivir, with or without transition to orally administered GS-441524.
Coggins, SJ; Govendir, M; Hall, EJ; Kimble, B; Malik, R; Norris, JM; Thompson, MF, )		0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
drug metabolitenull
antiviral agentA substance that destroys or inhibits replication of viruses.
anticoronaviral agentAny antiviral agent which inhibits the activity of coronaviruses.
[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 (4)

ClassDescription
pyrrolotriazineAny organic heterobicyclic compound containing ortho-fused pyrrolidine and triazine rings.
nitrileA compound having the structure RC#N; thus a C-substituted derivative of hydrocyanic acid, HC#N. In systematic nomenclature, the suffix nitrile denotes the triply bound #N atom, not the carbon atom attached to it.
C-nucleoside
aromatic amineAn amino compound in which the amino group is linked directly to an aromatic system.
[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 (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RNA-directed RNA polymerase IC50 (µMol)5.60000.01902.52798.8000AID1764901
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (131)

Assay IDTitleYearJournalArticle
AID1440653Antiviral activity against GFP-fused Ebolavirus infected in TERT-immortalized HMVEC assessed as reduction in viral replication preincubated with cells followed by viral infection measured after 3 to 4 days by fluorescence assay2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.
AID1898378AUC(0 to t) in Sprague-Dawley rat at 30 mg/kg, ig measured over 48 hrs by HPLC/MS analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1853874Antiviral activity against Nipah M1999 infected in human HeLa cells assessed as reduction in viral replication incubated for 48 to 144 hrs by reporter virus assay2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
AID1764946Drug metabolism in cynomolgus monkey assessed as 1-NTP metabolite concentration in main stem bronchi at 20 mg/kg, iv measured after 24 hrs by LC-MS/MS analysis
AID1898388Toxicity in BALB/c mouse infected with MHV-A59 assessed as change in body weight at 100 mg/kg, ip administered at 0.5 hrs post infection followed by 50 mg/kg administered daily measured upto 14 days2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1750788Antiviral activity against Human coronavirus 229E infected in human embryonic lung fibroblast cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTS cell viability assay2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Betulonic Acid Derivatives Interfering with Human Coronavirus 229E Replication via the nsp15 Endoribonuclease.
AID1853868Antiviral activity against Ebola infected in human macrophages assessed as reduction in viral replication2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
AID656928Antiviral activity against West nile virus NY99 infected in african green monkey Vero cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides.
AID1440652Antiviral activity against Ebolavirus Kikwit infected in human HeLa cells assessed as reduction in viral glycoprotein levels preincubated with cells for 2 hrs followed by viral infection measured after 48 hrs by immunostaining based assay2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.
AID1853902Antiviral activity against MERS-CoV infected in HAE cells assessed as reduction in viral replication at MOI of 0.5 incubated for 3 hrs followed by virus removal measured after 48 hrs by Hoechst 33258 staining based assay2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
AID1898382Tmax in Sprague-Dawley rat at 30 mg/kg, ig measured over 48 hrs by HPLC/MS analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1750810Inhibition of nsp15 T66I drug-resistant mutant in Human coronavirus 229E infected in human embryonic lung fibroblast cells assessed as reduction in virus yield2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Betulonic Acid Derivatives Interfering with Human Coronavirus 229E Replication via the nsp15 Endoribonuclease.
AID1778631Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability incubated for 1 to 2 hrs by MTS assay2021European journal of medicinal chemistry, Oct-05, Volume: 2211,2,4-Triazolo[1,5-a]pyrimidines: Efficient one-step synthesis and functionalization as influenza polymerase PA-PB1 interaction disruptors.
AID1750791Selectivity index, ratio of CC50 for cytotoxicity against mock-infected human embryonic lung fibroblast cells incubated for 5 days by MTS assay to EC50 for antiviral activity against Human coronavirus 229E infected in human embryonic lung fibroblast cells2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Betulonic Acid Derivatives Interfering with Human Coronavirus 229E Replication via the nsp15 Endoribonuclease.
AID656931Antiviral activity against SARS coronavirus Toronto-2 infected in african green monkey Vero cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides.
AID1898373Antiviral activity against SARS-COV 2 infected in human Caco-2 cells assessed as inhibition of viral replication after 48 hrs by qRT-PCR analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1898395Half life in human plasma at 3 to 225 mg, iv administered as 2 hr infusion2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1764900Inhibition of RSV RNP complex transcription incubated for 90 mins by agarose gel electrophoresis assay
AID1764912Oral bioavailability in cynomolgus monkey at 20 mg/kg by LC-MS/MS method
AID1707633Antitrypanosomal activity against Trypanosoma brucei brucei2021European journal of medicinal chemistry, Feb-15, Volume: 212Synthesis and evaluation of a collection of purine-like C-nucleosides as antikinetoplastid agents.
AID1764901Inhibition of HCV NS5B RNA-dependent RNA polymerase using sshRNA template preincubated for 5 mins followed by compound addition and measured after 90 mins
AID1764932Terminal half life in cynomolgus monkey at 20 mg/kg, iv after 30 mins by LC-MS/MS analysis
AID1853882Antiviral activity against SARS-CoV infected in HAE cells assessed as reduction in viral replication at MOI of 0.5 preincubated for 3 hrs followed by virus removal measured after 48 hrs by Hoechst 33258 staining based assay2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
AID1764919Drug metabolism in normal human bronchial epithelial cells assessed as 1-NTP metabolite concentration at 1 uM over 48 hrs by LC-MS/MS analysis
AID1440655Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells preincubated with cells for 3 days followed by viral infection by luciferase assay2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.
AID1766168Antiviral activity against SARS-CoV-2 nCoV-2019BetaCoV/Wuhan/WIV04/ infected in African green monkey Vero E6 cells assessed as inhibition of viral replication when host cells were pretreated for 1 hr followed by viral infection then followed by removal of2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Potency and pharmacokinetics of GS-441524 derivatives against SARS-CoV-2.
AID1766166Antiviral activity against SARS-CoV-2 nCoV-2019BetaCoV/Wuhan/WIV04/ infected in African green monkey Vero E6 cells assessed as inhibition of viral replication at 5 uM when host cells were pretreated for 1 hr followed by viral infection then followed by re2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Potency and pharmacokinetics of GS-441524 derivatives against SARS-CoV-2.
AID1707638Cytotoxicity against mouse primary macrophages assessed as reduction in cell viability2021European journal of medicinal chemistry, Feb-15, Volume: 212Synthesis and evaluation of a collection of purine-like C-nucleosides as antikinetoplastid agents.
AID1764909Permeability across basolateral to apical side in human Caco-2 cells
AID1898379Terminal elimination half life in Sprague-Dawley rat at 30 mg/kg, iv measured over 48 hrs by HPLC/MS analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1467736Cytotoxicity against human HuH7 after 4 to 5 days by Cell-Titer Glo viability assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
The ProTide Prodrug Technology: From the Concept to the Clinic.
AID1880206Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability measured after 1 to 2 hrs by MTS colorimetric assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity.
AID1853878Antiviral activity against Measles Rec.rMVEZGFP(3) infected in human HeLa cells assessed as reduction in viral replication incubated for 48 to 144 hrs by fluorescence based assay2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
AID1898394AUC in human plasma at 3 to 225 mg, iv administered as 2 hr infusion2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1898393Toxicity in BALB/c mouse infected with MHV-A59 assessed as change in body weight at 100 mg/kg, ig administered at 0.5 hrs post infection followed by 50 mg/kg administered daily measured upto 14 days2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1764949Drug metabolism in cynomolgus monkey assessed as 1-NTP metabolite concentration in trachea at 20 mg/kg, iv measured after 24 hrs by LC-MS/MS analysis
AID1898381Tmax in Sprague-Dawley rat at 30 mg/kg, iv measured over 48 hrs by HPLC/MS analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1750789Antiviral activity against Human coronavirus 229E infected in human embryonic lung fibroblast cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by microscopy2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Betulonic Acid Derivatives Interfering with Human Coronavirus 229E Replication via the nsp15 Endoribonuclease.
AID1853894Antiviral activity against SARS-CoV-2 infected in human Calu-3 cells assessed as reduction in viral replication at MOI of 0.01 measured after 72 hrs by qRT-PCR analysis2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
AID1467732Antiviral activity against Ebolavirus infected in human HeLa cells after 48 hrs by immuno-staining assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
The ProTide Prodrug Technology: From the Concept to the Clinic.
AID1467733Antiviral activity against Ebolavirus infected in human HuH7 cells after 3 days by end point dilution assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
The ProTide Prodrug Technology: From the Concept to the Clinic.
AID1707635Antitrypanosomal activity against Trypanosoma cruzi infected in human MRC-5 SV2 cells2021European journal of medicinal chemistry, Feb-15, Volume: 212Synthesis and evaluation of a collection of purine-like C-nucleosides as antikinetoplastid agents.
AID1321300Antiviral activity against Ebolavirus assessed as reduction in viral replication2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
Nucleoside Phosphate and Phosphonate Prodrug Clinical Candidates.
AID656927Antiviral activity against Dengue virus type 2 New Guinea C infected in african green monkey Vero E6 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides.
AID1853884Antiviral activity against SARS-CoV-2 infected in human A549 cells expressing hACE2 assessed as reduction in viral replication at MOI of 0.025 incubated for 48 hrs by luciferase based assay2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
AID1467734Cytotoxicity against human primary macrophages after 4 to 5 days by Cell-Titer Glo viability assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
The ProTide Prodrug Technology: From the Concept to the Clinic.
AID656926Antiviral activity against Yellow fever virus 17D infected in human HeLa cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides.
AID1764940Drug metabolism in cynomolgus monkey assessed as 1-NTP metabolite concentration in lung tissue at 20 mg/kg, iv measured after 24 hrs by LC-MS/MS analysis
AID1440656Cytotoxicity against human Hep2 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.
AID1764920Drug metabolism in HAE cells assessed as 1-NTP metabolite concentration at 1 uM over 48 hrs by LC-MS/MS analysis
AID1898380Terminal elimination half life in Sprague-Dawley rat at 30 mg/kg, ig measured over 48 hrs by HPLC/MS analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID656938Cytotoxicity against human MRC5 cells by MTS assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides.
AID656930Antiviral activity against Parainfluenza 3 C 243 infected in african green monkey Vero cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides.
AID1880208Antiviral activity against HCoV-229E infected in HEL 299 cells assessed as reduction in virus-induced cytopathic effect preincubated with compound followed by viral infection and measured after 7 days by MTS cell viability assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity.
AID1764952Drug metabolism in cynomolgus monkey assessed as total metabolite concentration in liver at 20 mg/kg, iv measured after 24 hrs by LC-MS/MS analysis
AID1764915Selectivity index, ratio of EC50 for HCV 1b infected in human Huh-7 cells to EC50 for RSV A2 infected in HEp-2 cells
AID1764903Cytotoxicity against human HEp-2 cells assessed as reduction in cell viability incubated for 4 to 5 days by CellTiter Glo viability assay
AID1853899Antiviral activity against SARS-CoV-2 infected in human PSC-derived lung epithelial cells assessed as reduction in viral replication2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
AID1764908Permeability across apical to basolateral side in human Caco-2 cells
AID1707634Antitrypanosomal activity against Trypanosoma brucei rhodesiense2021European journal of medicinal chemistry, Feb-15, Volume: 212Synthesis and evaluation of a collection of purine-like C-nucleosides as antikinetoplastid agents.
AID1440654Antiviral activity against Respiratory syncytial virus A2 infected in human Hep2 cells assessed as reduction of virus-induced cytopathic effect after 4 days by Cell-Titer Glo assay2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.
AID1880209Selectivity index, ratio of CC50 for cytotoxicity against HEL 299 cells to EC50 for antiviral activity against HCoV-229E infected in HEL 299 cells2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity.
AID1764937Drug metabolism in cynomolgus monkey assessed as 1-NTP metabolite concentration in PBMC at 20 mg/kg, iv measured after 24 hrs by LC-MS/MS analysis
AID656936Cytotoxicity against human HeLa cells by MTS assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides.
AID656941Cmax in human HuH7 cells assessed as triphosphate concentration per million cells at 10 uM incubated for 24 hrs measured after washout by LC-MS analysis2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides.
AID656937Cytotoxicity against human HuH7 cells by MTS assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides.
AID1898385Oral bioavailability in Sprague-Dawley rat at 30 mg/kg measured over 48 hrs by HPLC/MS analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1898376Cytotoxicity against human Caco-2 cells assessed as reduction in cell viability upto 50 uM measured for 48 hrs by CCK8 assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1853872Antiviral activity against MARV Rec. Bat371-GFP infected in human Huh-7 cells assessed as reduction in viral replication incubated for 48 to 144 hrs by fluorescence based assay2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
AID1880205Antiviral activity against SARS-CoV-2 infected in eGFP expressing African green monkey Vero E6 cells assessed as reduction in virus-induced cytopathic effect measured after 4 days post infection by laser scanning microscopic analysis2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity.
AID1440651Lipophilicity, log D of the compound after 30 mins by HPLC/UV method2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.
AID1467731Antiviral activity against Ebolavirus infected in human primary macrophages after 48 hrs by immuno-staining assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
The ProTide Prodrug Technology: From the Concept to the Clinic.
AID1764934AUCinfinity in cynomolgus monkey at 20 mg/kg, iv after 30 mins by LC-MS/MS analysis
AID1880210Antiviral activity against HCoV-OC43 infected in HEL 299 cells assessed as reduction in virus-induced cytopathic effect preincubated with compound followed by viral infection and measured after 7 days by MTS cell viability assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity.
AID1764930Clearance in cynomolgus monkey at 20 mg/kg, iv after 30 mins by LC-MS/MS analysis
AID1764904Antiviral activity against HCV 1b infected in human Huh-7 cells assessed as reduction in viral replication measured after 3 days by dual-Glo luciferase assay
AID1853886Antiviral activity against SARS-CoV-2 infected in HAEC cells assessed as reduction in viral replication incubated for 1.5 hrs followed by virus removal upto 24 hrs and subsequent replacement of medium containing compound by RT-qPCR analysis2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
AID1707637Cytotoxicity against human MRC-5 SV2 cells assessed as reduction in cell viability2021European journal of medicinal chemistry, Feb-15, Volume: 212Synthesis and evaluation of a collection of purine-like C-nucleosides as antikinetoplastid agents.
AID656934Cytotoxicity against african green monkey Vero cells by MTS assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides.
AID1764955Drug metabolism in cynomolgus monkey assessed as total metabolite concentration in kidney at 20 mg/kg, iv measured after 24 hrs by LC-MS/MS analysis
AID656925Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides.
AID1707636Antileishmanial activity against Leishmania infantum infected in mouse primary macrophages2021European journal of medicinal chemistry, Feb-15, Volume: 212Synthesis and evaluation of a collection of purine-like C-nucleosides as antikinetoplastid agents.
AID1880204Cytotoxicity against HEL 299 cells assessed as reduction in cell viability measured after 1 to 2 hrs by MTS colorimetric assay2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity.
AID1764911Oral bioavailability in dog
AID1750790Cytotoxicity against mock-infected human embryonic lung fibroblast cells incubated for 5 days by MTS assay2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Betulonic Acid Derivatives Interfering with Human Coronavirus 229E Replication via the nsp15 Endoribonuclease.
AID1898386Antiviral activity against SARS-CoV-2 infected in AAV-human ACE2 transduced BALB/c mouse assessed as viral clearance in lungs at 25 mg/kg/day, ip administered 1 day prior to viral infection and measured after 2 days post infection by focus forming assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1764906Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by CellTiter Glo viability assay
AID656939Cytotoxicity against dog MDCK cells by MTS assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides.
AID1898375Cytotoxicity against human Calu-3 cells assessed as reduction in cell viability upto 50 uM measured for 48 hrs by CCK8 assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1853896Antiviral activity against SARS-CoV-2 infected in human Calu-3 2B4 cells assessed as reduction in viral replication at MOI of 0.01 preincubated for 2 hrs followed by viral infection for 30 mins and subsequent virus removal and addition of medium containin2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
AID1853892Antiviral activity against SARS-CoV-2 infected in human Caco-2 cells assessed as reduction in viral replication at MOI of 0.01 measured after 72 hrs by qRT-PCR analysis2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
AID1898377AUC(0 to t) in Sprague-Dawley rat at 30 mg/kg, iv measured over 48 hrs by HPLC/MS analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1440658Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.
AID1467735Cytotoxicity against human HeLa after 4 to 5 days by Cell-Titer Glo viability assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
The ProTide Prodrug Technology: From the Concept to the Clinic.
AID1880207Selectivity index, ratio of CC50 for cytotoxicity against African green monkey Vero E6 cells to EC50 for antiviral activity against SARS-CoV-2 infected in eGFP expressing African green monkey Vero E6 cells2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity.
AID1764943Drug metabolism in cynomolgus monkey assessed as 1-NTP metabolite concentration in lower bronchi at 20 mg/kg, iv measured after 24 hrs by LC-MS/MS analysis
AID1898374Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability upto 50 uM measured for 48 hrs by CCK8 assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1898371Antiviral activity against SARS-COV 2 infected in human Calu-3 cells assessed as inhibition of viral replication after 48 hrs by qRT-PCR analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1764918Drug metabolism in human HEp-2 cells assessed as 1-NTP metabolite concentration at 1 uM over 48 hrs by LC-MS/MS analysis
AID1898383Cmax in Sprague-Dawley rat at 30 mg/kg, iv measured over 48 hrs by HPLC/MS analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1898390Antiviral activity against MHV-A59 infected in BALB/c mouse assessed as improvement in survival at 100 mg/kg, ip administered at 0.5 hrs post infection followed by 50 mg/kg administered daily measured upto 14 days2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1898372Antiviral activity against SARS-COV 2 infected in African green monkey Vero E6 cells assessed as inhibition of viral replication after 48 hrs by qRT-PCR analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1750809Inhibition of nsp15 K60R drug-resistant mutant in Human coronavirus 229E infected in human embryonic lung fibroblast cells assessed as reduction in virus yield2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Betulonic Acid Derivatives Interfering with Human Coronavirus 229E Replication via the nsp15 Endoribonuclease.
AID1853870Antiviral activity against Ebola infected in human HeLa cells assessed as reduction in viral replication2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
AID656932Antiviral activity against Coxsackievirus A7 infected in human MRC5 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides.
AID1764910Oral bioavailability in Sprague-Dawley rat at 8 mg/kg by LC-MS/MS method
AID1440657Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 3 days by calcein-AM dye based fluorescence assay2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.
AID1853880Antiviral activity against Measles virus infected in HMVEC cells assessed as reduction in viral replication2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
AID1764922Drug metabolism in NHBE cells assessed as 1-NTP metabolite concentration at EC50 over 48 hrs by LC-MS/MS analysis
AID1764913Selectivity index, ratio of CC50 for human HEp-2 cells to EC50 for RSV A2 infected in HEp-2 cells
AID1764907Lipophilicity, log D of compound in acetonitrile and water shaken for 30 mins by HPLC/UV analysis
AID1898389Antiviral activity against MHV-A59 infected in BALB/c mouse assessed as improvement in survival at 100 mg/kg, ig administered at 0.5 hrs post infection followed by 50 mg/kg administered daily measured upto 14 days2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID656935Cytotoxicity against african green monkey Vero E6 cells by MTS assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides.
AID1764914Antiviral activity against RSV infected in NHBE cells after 3 days by ONE-Glo luciferase assay
AID1898387Toxicity AAV-human ACE2 transduced BALB/c mouse infected with SARS-COV2 assessed as loss of body weight at 25 mg/kg/day, ip administered 1 day prior to viral infection and treated for 8 days2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1898392Antiviral activity against MHV-A59 infected in BALB/c mouse assessed as reduction in viral titer in liver at 100 mg/kg, ip administered at 0.5 hrs post infection followed by 50 mg/kg administered daily measured upto 14 days by qRT-PCR analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1764933Cmax in cynomolgus monkey at 20 mg/kg, iv after 30 mins by LC-MS/MS analysis
AID1764902Antiviral activity against RSV A2 infected in HEp-2 cells assessed as reduction in virus-induced cytopathic effect after 4 days by CellTiter Glo viability assay
AID1764921Drug metabolism in human HEp-2 cells assessed as 1-NTP metabolite concentration at EC50 over 48 hrs by LC-MS/MS analysis
AID1764931Volume of distribution at steady state in cynomolgus monkey at 20 mg/kg, iv after 30 mins by LC-MS/MS analysis
AID1853876Antiviral activity against Nipah B2004 infected in human NCI-H358 cells assessed as reduction in viral replication incubated for 48 to 144 hrs by reporter virus assay2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
AID1898391Antiviral activity against MHV-A59 infected in BALB/c mouse assessed as reduction in viral titer in liver at 100 mg/kg, ig administered at 0.5 hrs post infection followed by 50 mg/kg administered daily measured upto 14 days by qRT-PCR analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1853890Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in viral replication2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
AID1898384Cmax in Sprague-Dawley rat at 30 mg/kg, ig measured over 48 hrs by HPLC/MS analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Remdesivir Metabolite GS-441524 Effectively Inhibits SARS-CoV-2 Infection in Mouse Models.
AID1880211Selectivity index, ratio of CC50 for cytotoxicity against HEL 299 cells to EC50 for antiviral activity against HCoV-OC43 infected in HEL 299 cells2022ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5
Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity.
AID1764905Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability measured after 3 days by dual-Glo luciferase assay
AID656933Antiviral activity against Coxsackievirus A21 infected in human MRC5 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides.
AID656929Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and antiviral activity of a series of 1'-substituted 4-aza-7,9-dideazaadenosine C-nucleosides.
AID1440673Antiviral activity against Ebolavirus Kikwit infected in human macrophages preincubated with cells for 2 hrs followed by viral infection measured after 48 hrs2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.
AID1778630Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as rescue of virus reduced eGFP signals by SARS-CoV-2 antiviral assay2021European journal of medicinal chemistry, Oct-05, Volume: 2211,2,4-Triazolo[1,5-a]pyrimidines: Efficient one-step synthesis and functionalization as influenza polymerase PA-PB1 interaction disruptors.
AID1853888Antiviral activity against SARS-CoV-2 infected in human Huh-7 cells assessed as reduction in virus-induced cytopathic effect at MOI of 0.0037 measured after 4 days by MTS assay2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (62)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (6.45)24.3611
2020's58 (93.55)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 67.12

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index67.12 (24.57)
Research Supply Index4.19 (2.92)
Research Growth Index5.69 (4.65)
Search Engine Demand Index120.59 (26.88)
Search Engine Supply Index2.19 (0.95)

This Compound (67.12)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (1.56%)5.53%
Reviews7 (10.94%)6.00%
Case Studies1 (1.56%)4.05%
Observational2 (3.13%)0.25%
Other53 (82.81%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		7.7620aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
fluorouracil
Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.		3.2710nucleobase analogue;
organofluorine compound		antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic
miltefosine
miltefosine: hexadecyl phosphocholine derivative of cisplatin; did not substantially activate HIV long terminal repeat; less toxic than cisplatin. miltefosine : A phospholipid that is the hexadecyl monoester of phosphocholine.		2.3110phosphocholines;
phospholipid		anti-inflammatory agent;
anticoronaviral agent;
antifungal agent;
antineoplastic agent;
antiprotozoal drug;
apoptosis inducer;
immunomodulator;
protein kinase inhibitor
hydroxychloroquine
Hydroxychloroquine: A chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa. It inhibits plasmodial heme polymerase. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p970). hydroxychloroquine : An aminoquinoline that is chloroquine in which one of the N-ethyl groups is hydroxylated at position 2. An antimalarial with properties similar to chloroquine that acts against erythrocytic forms of malarial parasites, it is mainly used as the sulfate salt for the treatment of lupus erythematosus, rheumatoid arthritis, and light-sensitive skin eruptions.		7.3110aminoquinoline;
organochlorine compound;
primary alcohol;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
dermatologic drug
ibuprofen
Midol: combination of cinnamedrine, phenacetin, aspirin & caffeine		2.610monocarboxylic acidantipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
radical scavenger;
xenobiotic
alanine
Alanine: A non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases IMMUNITY, and provides energy for muscle tissue, BRAIN, and the CENTRAL NERVOUS SYSTEM.. alanine : An alpha-amino acid that consists of propionic acid bearing an amino substituent at position 2.		7.49270alanine zwitterion;
alanine;
L-alpha-amino acid;
proteinogenic amino acid;
pyruvate family amino acid		EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor;
fundamental metabolite
adenosine diphosphate
Adenosine Diphosphate: Adenosine 5'-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5'-position.		2.610adenosine 5'-phosphate;
purine ribonucleoside 5'-diphosphate		fundamental metabolite;
human metabolite
adenosine monophosphate
Adenosine Monophosphate: Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.		7.49270adenosine 5'-phosphate;
purine ribonucleoside 5'-monophosphate		adenosine A1 receptor agonist;
cofactor;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
EC 3.1.3.11 (fructose-bisphosphatase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical
leucine
Leucine: An essential branched-chain amino acid important for hemoglobin formation.. leucine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isobutyl group.		2.4110amino acid zwitterion;
L-alpha-amino acid;
leucine;
proteinogenic amino acid;
pyruvate family amino acid		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
cytidine
[no description available]		2.4110cytidinesEscherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		7.79151pyrrole;
secondary amine
pyrazines
Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.		2.3110diazine;
pyrazines		Daphnia magna metabolite
benzonidazole
benzonidazole: used in treatment of Chagas' disease. benznidazole : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2-nitroimidazol-1-yl)acetic acid with the aromatic amino group of benzylamine. Used for treatment of Chagas disease.		2.3110C-nitro compound;
imidazoles;
monocarboxylic acid amide		antiprotozoal drug
adenosine diphosphate ribose
Adenosine Diphosphate Ribose: An ester formed between the aldehydic carbon of RIBOSE and the terminal phosphate of ADENOSINE DIPHOSPHATE. It is produced by the hydrolysis of nicotinamide-adenine dinucleotide (NAD) by a variety of enzymes, some of which transfer an ADP-ribosyl group to target proteins.		2.920ADP-sugarEscherichia coli metabolite;
mouse metabolite
ribavirin
Rebetron: Rebetron is tradename		2.31101-ribosyltriazole;
aromatic amide;
monocarboxylic acid amide;
primary carboxamide		anticoronaviral agent;
antiinfective agent;
antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
itraconazole
Itraconazole: A triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.. itraconazole : An N-arylpiperazine that is cis-ketoconazole in which the imidazol-1-yl group is replaced by a 1,2,4-triazol-1-yl group and in which the actyl group attached to the piperazine moiety is replaced by a p-[(+-)1-sec-butyl-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl]phenyl group. A potent P-glycoprotein and CYP3A4 inhibitor, it is used as an antifungal drug for the treatment of various fungal infections, including aspergillosis, blastomycosis, candidiasis, chromoblastomycosis, coccidioidomycosis, cryptococcosis, histoplasmosis, and sporotrichosis.		7.7620aromatic ether;
conazole antifungal drug;
cyclic ketal;
dichlorobenzene;
dioxolane;
N-arylpiperazine;
triazole antifungal drug;
triazoles		EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
Hedgehog signaling pathway inhibitor;
P450 inhibitor
adenosine
quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit		9.94431adenosines;
purines D-ribonucleoside		analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
betulin
betulin: isolated from various white birch bark (BETULA). betulin : A pentacyclic triterpenoid that is lupane having a double bond at position 20(29) as well as 3beta-hydroxy and 28-hydroxymethyl substituents.		2.3110diol;
pentacyclic triterpenoid		analgesic;
anti-inflammatory agent;
antineoplastic agent;
antiviral agent;
metabolite
lopinavir
[no description available]		7.3110amphetamines;
dicarboxylic acid diamide		anticoronaviral agent;
antiviral drug;
HIV protease inhibitor
betulonic acid
betulonic acid: isolated from Rush javanica; strucure in first source		2.3110triterpenoidanticoronaviral agent
proline
Proline: A non-essential amino acid that is synthesized from GLUTAMIC ACID. It is an essential component of COLLAGEN and is important for proper functioning of joints and tendons.. proline : An alpha-amino acid that is pyrrolidine bearing a carboxy substituent at position 2.		2.4110amino acid zwitterion;
glutamine family amino acid;
L-alpha-amino acid;
proline;
proteinogenic amino acid		algal metabolite;
compatible osmolytes;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
n(4)-hydroxycytidine
N(4)-hydroxycytidine : A nucleoside analogue that is cytidine which carries a hydroxy group at the N(4)-positon. It has broad-spectrum antiviral activity against influenza, SARS-CoV , SARS-CoV-2 and MERS-CoV.		2.4110ketoxime;
nucleoside analogue		anticoronaviral agent;
antiviral agent;
drug metabolite;
human xenobiotic metabolite
ritonavir
Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.		7.31101,3-thiazoles;
carbamate ester;
carboxamide;
L-valine derivative;
ureas		antiviral drug;
environmental contaminant;
HIV protease inhibitor;
xenobiotic
betadex
beta-Cyclodextrins: Cyclic GLUCANS consisting of seven (7) glucopyranose units linked by 1,4-glycosidic bonds.		2.9430cyclodextrin
zithromax
Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections.		2.3110macrolide antibioticantibacterial drug;
environmental contaminant;
xenobiotic
cmx 001
[no description available]		3.2310
favipiravir
favipiravir : A member of the class of pyrazines that is pyrazine substituted by aminocarbonyl, hydroxy and fluoro groups at positions 2, 3 and 6, respectively. It is an anti-viral agent that inhibits RNA-dependent RNA polymerase of several RNA viruses and is approved for the treatment of influenza in Japan.		2.7220hydroxypyrazine;
organofluorine compound;
primary carboxamide		anticoronaviral agent;
antiviral drug;
EC 2.7.7.48 (RNA-directed RNA polymerase) inhibitor
N-(7-phenyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)benzamide
[no description available]		2.3110pyrimidines
ssya10-001
SSYA10-001: a helicase inhibitor with antiviral activity; structure in first source		2.4110
bafilomycin a1
bafilomycin A1: from Streptomyces griseus; structure given in first source. bafilomycin A1 : The most used of the bafilomycins, a family of toxic macrolide antibiotics derived from Streptomyces griseus.		2.3110cyclic hemiketal;
macrolide antibiotic;
oxanes		apoptosis inducer;
autophagy inhibitor;
bacterial metabolite;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
EC 3.6.3.14 (H(+)-transporting two-sector ATPase) inhibitor;
ferroptosis inhibitor;
fungicide;
potassium ionophore;
toxin
gs-7340
tenofovir alafenamide: component of Biktarvy. tenofovir alafenamide : An L-alanine derivative that is isopropyl L-alaninate in which one of the amino hydrogens is replaced by an (S)-({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)(phenoxy)phosphoryl group. A prodrug for tenofovir, it is used (as the fumarate salt) in combination therapy for the treatment of HIV-1 infection.		3.27106-aminopurines;
ether;
isopropyl ester;
L-alanine derivative;
phosphoramidate ester		antiviral drug;
HIV-1 reverse transcriptase inhibitor;
prodrug
cellulose
DEAE-Cellulose: Cellulose derivative used in chromatography, as ion-exchange material, and for various industrial applications.		2.4110glycoside
sofosbuvir
Sofosbuvir: A uridine monophosphate analog inhibitor of HEPATITIS C VIRUS (HCV) polymerase NS5B that is used as an ANTIVIRAL AGENT in the treatment of CHRONIC HEPATITIS C.. sofosbuvir : A nucleotide conjugate that is used in combination with ledipasvir (under the trade name Harvoni) for the treatment of chronic hepatitis C genotype 1 infection.		3.2710isopropyl ester;
L-alanyl ester;
nucleotide conjugate;
organofluorine compound;
phosphoramidate ester		antiviral drug;
hepatitis C protease inhibitor;
prodrug
bms-986094
BMS-986094: a prodrug of 2'-C-methylguanosine and antiviral agent		2.4110
GS-443902
GS-441524 triphosphate: intracellular active metabolite of remdesivir. GS-443902 : An organic triphosphate that is GS-441524 in which the 5'-hydroxy group has been replaced by a triphosphate group. It is the active metabolite of remdesivir.		2.5120aromatic amine;
C-nucleoside;
nitrile;
organic triphosphate;
pyrrolotriazine		anticoronaviral agent;
antiviral drug;
drug metabolite
s 8932
[no description available]		9.43341aromatic amine;
C-nucleoside;
carboxylic ester;
nitrile;
phosphoramidate ester;
pyrrolotriazine		anticoronaviral agent;
antiviral drug;
prodrug
molnupiravir
molnupiravir: prodrug that’s metabolized into N4-hydroxycytidine (NHC), a ribonucleoside analog. molnupiravir : A nucleoside analogue that is N(4)-hydroxycytidine in which the 5'-hydroxy group is replaced by a (2-methylpropanoyl)oxy group. It is the prodrug of the active antiviral ribonucleoside analog N(4)-hydroxycytidine (EIDD-1931), has activity against a number of RNA viruses including SARS-CoV-2, MERS-CoV, and seasonal and pandemic influenza viruses. It is currently in phase III trials for the treatment of patients with COVID-19.		2.4110isopropyl ester;
ketoxime;
nucleoside analogue		anticoronaviral agent;
antiviral drug;
prodrug
nirmatrelvir
nirmatrelvir: component of COVID-19 drug Paxlovid. Paxlovid : A mixture containing nirmatrelvir and ritonavir. It is co-administered in tablet form for the treatment and post-exposure prophylaxis of COVID-19.. nirmatrelvir : An azabicyclohexane that is (1R,5S)-3-azabicyclo[3.1.0]hexane substituted by {(1S)-1-cyano-2-[(3S)-2-oxopyrrolidin-3-yl]ethyl}aminoacyl, 3-methyl-N-(trifluoroacetyl)-L-valinamide, methyl and methyl groups at positions 2S, 3, 6 and 6, respectively. It is the first orally administered inhibitor of SARS-CoV-2 main protease developed by Pfizer and used in combination with ritonavir for the treatment of COVID-19.		2.4110azabicyclohexane;
nitrile;
organofluorine compound;
pyrrolidin-2-ones;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary carboxamide		anticoronaviral agent;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Benign Neoplasms
[description not available]		03.0410
Viral Diseases
[description not available]		03.4620
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.		03.0410
Virus Diseases
A general term for diseases caused by viruses.		03.4620
Ebola Hemorrhagic Fever
[description not available]		02.1510
Hemorrhagic Fever, Ebola
A highly fatal, acute hemorrhagic fever caused by EBOLAVIRUS.		02.1510
2019 Novel Coronavirus Disease
[description not available]		05.99180
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.7620
Kidney Diseases
Pathological processes of the KIDNEY or its component tissues.		02.4110
Infections, Coronavirus
[description not available]		03.4550
Feline Infectious Peritonitis
Common coronavirus infection of cats caused by the feline infectious peritonitis virus (CORONAVIRUS, FELINE). The disease is characterized by a long incubation period, fever, depression, loss of appetite, wasting, and progressive abdominal enlargement. Infection of cells of the monocyte-macrophage lineage appears to be essential in FIP pathogenesis.		06.53111
Coronavirus Infections
Virus diseases caused by the CORONAVIRUS genus. Some specifics include transmissible enteritis of turkeys (ENTERITIS, TRANSMISSIBLE, OF TURKEYS); FELINE INFECTIOUS PERITONITIS; and transmissible gastroenteritis of swine (GASTROENTERITIS, TRANSMISSIBLE, OF SWINE).		03.4550
Cat Diseases
Diseases of the domestic cat (Felis catus or F. domesticus). This term does not include diseases of the so-called big cats such as CHEETAHS; LIONS; tigers, cougars, panthers, leopards, and other Felidae for which the heading CARNIVORA is used.		04.4950
Critical Illness
A disease or state in which death is possible or imminent.		02.4110
chronic COVID syndrome
[description not available]		03.3310
Pneumonia, Viral
Inflammation of the lung parenchyma that is caused by a viral infection.		02.6620
MODS
[description not available]		02.2510
Multiple Organ Failure
A progressive condition usually characterized by combined failure of several organs such as the lungs, liver, kidney, along with some clotting mechanisms, usually postinjury or postoperative.		02.2510
Chronic Kidney Failure
[description not available]		03.2310
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.		03.2310
African Swine Fever
A sometimes fatal ASFIVIRUS infection of pigs, characterized by fever, cough, diarrhea, hemorrhagic lymph nodes, and edema of the gallbladder. It is transmitted between domestic swine by direct contact, ingestion of infected meat, or fomites, or mechanically by biting flies or soft ticks (genus Ornithodoros).		07.3110