Page last updated: 2024-11-04

pleconaril

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

Description

WIN 63843: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID1684
CHEMBL ID29609
SCHEMBL ID49383
MeSH IDM0296763

Synonyms (70)

Synonym
win-63843
sr-263843
vp-63843
picovir
sr-63843
D05528
pleconaril (usan/inn)
153168-05-9
W11 ,
3-{3,5-dimethyl-4-[3-(3-methyl-isoxazol-5-yl)-propoxy]-phenyl}-5-trifluoromethyl-[1,2,4]oxadiazole
3-[3,5-dimethyl-4-[3-(3-methylisoxazol-5-yl)propoxy]phenyl]-5-(trifluoromethyl)-1,2,4-oxadiazole
pleconaril
1,3-dimethyl-2-[3-(3-methylisoxazol-5-yl)propoxy]-5-[5-(trifluoromethyl)(1,2,4-oxadiazol-3-yl)]benzene
vp63843
win63843
1,2,4-oxadiazole, 3-(3,5-dimethyl-4-(3-(3-methyl-5-isoxazolyl)propoxy)phenyl)-5-(trifluoromethyl)-
pleconaril [usan:inn]
3-(4-(3-(3-methyl-5-isoxazolyl)propoxy)-3,5-xylyl)-5-trifluoromethyl)-1,2,4-oxadizole
vp 63843
win 63843
3-(3,5-dimethyl-4-(3-(3-methyl-5-isoxazolyl)propoxy)phenyl)-5-(trifluoromethyl)-1,2,4-oxadiazole
3-(3,5-dimethyl-4((3-(3-methyl-5-isoxazolyl)propyl)phenyl)-5-trifluoromethyl)-1,2,4-oxadiazole
CHEMBL29609 ,
bdbm50111469
5-[3-[2,6-dimethyl-4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenoxy]propyl]-3-methylisoxazole
3-(3,5-dimethyl-4-(3-(3-methylisoxazol-5-yl)propoxy)phenyl)-5-(trifluoromethyl)-1,2,4-oxadiazole
pleconaril3-{3,5-dimethyl-4-[3-(3-methyl-isoxazol-5-yl)-propoxy]-phenyl}-5-trifluoromethyl-[1,2,4]oxadiazole
3-{3,5-dimethyl-4-[3-(3-methyl-isoxazol-5-yl)-propoxy]-phenyl}-5-trifluoromethyl-[1,2,4]oxadiazole(pleconaril)
pleconaril-d8
3-[3,5-dimethyl-4-[3-(3-methyl-1,2-oxazol-5-yl)propoxy]phenyl]-5-(trifluoromethyl)-1,2,4-oxadiazole
AKOS016005860
FT-0673965
FT-0673964
9h4570q89d ,
unii-9h4570q89d
3-[3,5-dimethyl-4-[3-(3-methyl-5-isoxazolyl)propoxy]phenyl]-5-(trifluoromethyl)-1,2,4-oxadiazole
pleconaril [mi]
pleconaril [mart.]
pleconaril [who-dd]
pleconaril [usan]
pleconaril [inn]
DB05105
SCHEMBL49383
tox21_113756
dtxsid8057649 ,
dtxcid9031438
NCGC00253627-01
cas-153168-05-9
HY-19952
CS-5475
sr-01000945059
SR-01000945059-1
pleconaril, >=98% (hplc)
3-[3,5-dimethyl-4-[3-(3-methyl-5-isoxazolyl)propoxy]phenyl]-5-(trifluoromethyl)-1,2,4-oxadiazole; picovir; pleconaril; vp 63843; win 63843
J-008988
pleconarilis
3-{3,5-dimethyl-4-[3-(3-methylisoxazol-5-yl)propoxy]phenyl}-5-(trifluoromethyl)-1,2,4-oxadiazole
BCP20819
F20826
pleconaril;vp 63843;win 63843
EX-A1448
3-(3,5-dimethyl-4-(3-(3-methyl-1,2-oxazol-5-yl)propoxy)phenyl)-5-(trifluoromethyl)-1,2,4-oxadiazole
Q770293
mfcd00923611
A847822
AC-36849
pleconaril 100 microg/ml in acetonitrile
AS-77268
kqoxlkojhvftrn-uhfffaoysa-n
3-(3,5-dimethyl-4-[3-(3-methylisoxazol-5-yl)propoxy]phenyl)-5-(trifluoromethyl)-1,2,4-oxadiazole

Research Excerpts

Overview

Pleconaril is a novel antiviral drug being developed by Schering-Plough to treat Picornaviridae infections. The drug is in its late clinical trials stage. Pleconarill is a broad-spectrum antirhinovirus and antienterovirus compound.

ExcerptReferenceRelevance
"Pleconaril is a capsid inhibitor used previously to treat enterovirus infections. "( Genetic and antigenic structural characterization for resistance of echovirus 11 to pleconaril in an immunocompromised patient.
Benschop, KSM; Koen, G; Minnaar, RP; Pajkrt, D; van den Broek, PJ; van Hemert, FJ; Vossen, ACTM; Westerhuis, BM; Wildenbeest, JG; Wolthers, KC, 2015
)
2.08
"Pleconaril is an antiviral agent with in vitro activity against HEVs that has been used in the treatment of HEV infections."( Pleconaril revisited: clinical course of chronic enteroviral meningoencephalitis after treatment correlates with in vitro susceptibility.
Benschop, KS; Koen, G; Kuijpers, TW; van den Broek, PJ; Vossen, AC; Wierenga, PC; Wildenbeest, JG; Wolthers, KC, 2012
)
2.54
"Pleconaril is a novel antiviral drug being developed by Schering-Plough to treat Picornaviridae infections, and is in its late clinical trials stage."( In-Silico screening of Pleconaril and its novel substituted derivatives with Neuraminidase of H1N1 Influenza strain.
Hussain Basha, S; Prasad, RN, 2012
)
1.41
"Pleconaril is a novel, orally available, systemically acting molecule whose pharmacokinetics are characterized by a two-compartment open model with first-order absorption and with a safety profile similar to that of placebo."( Pleconaril, a novel antipicornaviral agent.
Florea, NR; Maglio, D; Nicolau, DP, 2003
)
2.48
"Pleconaril is a new orally acting antiviral drug with broad anti-picornavirus activity, which provides to treat rhinoviral and enteroviral infections."( [Polio-like myelitis due to Coxsackie-Virus B 3: Course under treatment with pleconaril].
Burtzlaff, C; Friedrich, B; Lauffer, H; Utzig, N,
)
1.08
"Pleconaril is an investigational agent that inhibits viral attachment to host cell receptors and uncoating of viral nucleic acid."( Presentation, diagnosis, and management of enterovirus infections in neonates.
Abzug, MJ, 2004
)
1.04
"Pleconaril is a broad-spectrum antirhinovirus and antienterovirus compound that binds into a hydrophobic pocket within viral protein 1, stabilizing the capsid and resulting in the inhibition of cell attachment and RNA uncoating. "( Structural and virological studies of the stages of virus replication that are affected by antirhinovirus compounds.
Bator, CM; Chakravarty, S; Demenczuk, TM; Ledford, RM; Pevear, DC; Rossmann, MG; Simpson, AA; Skochko, GA; Watanyar, A; Zhang, Y, 2004
)
1.77
"Pleconaril is a novel capsid inhibitor of HRVs."( Insights into the genetic basis for natural phenotypic resistance of human rhinoviruses to pleconaril.
Collett, MS; Ledford, RM; Pevear, DC, 2005
)
1.27
"Pleconaril is a viral capsid inhibitor under evaluation for treatment of infections caused by rhinoviruses and enteroviruses. "( The effect of oral pleconaril on hepatic cytochrome P450 3A activity in healthy adults using intravenous midazolam as a probe.
Bertino, JS; Gartung, AM; Liu, S; Ma, JD; Nafziger, AN; Rhodes, G, 2006
)
2.1
"Pleconaril is an orally active broad-spectrum antipicornaviral agent which demonstrates excellent penetration into the central nervous system, liver, and nasal epithelium. "( Single-dose pharmacokinetics of a pleconaril (VP63843) oral solution and effect of food.
Abdel-Rahman, SM; Kearns, GL, 1998
)
2.02
"Pleconaril is an orally active, broad-spectrum antipicornaviral agent which demonstrates excellent penetration into the central nervous system, liver, and nasal epithelium. "( Single-dose pharmacokinetics of a pleconaril (VP63843) oral solution in children and adolescents. Pediatric Pharmacology Research Unit Network.
Abdel-Rahman, SM; Blowey, DL; Jacobs, RF; James, LP; Kearns, GL; Marshall, JD; Wells, TG, 1999
)
2.03
"Pleconaril (VP 63843) is a novel orally bioavailable small molecule with broad antipicornavirus (enterovirus and rhinovirus) activity. "( Attenuated virulence of pleconaril-resistant coxsackievirus B3 variants.
Groarke, JM; Pevear, DC, 1999
)
2.05
"Pleconaril is an orally active broad-spectrum antipicornaviral agent with excellent penetration into the central nervous system and nasal epithelium. "( Single oral dose escalation pharmacokinetics of pleconaril (VP 63843) capsules in adults.
Abdel-Rahman, SM; Kearns, GL, 1999
)
2
"Pleconaril is an orally active, broad spectrum antipicornaviral agent with activity against nonpolio enteroviruses. "( Single dose pharmacokinetics of pleconaril in neonates. Pediatric Pharmacology Research Unit Network.
Abdel-Rahman, SM; Bradley, JS; Capparelli, EV; Jacobs, RF; James, LP; Johnson, KM; Kearns, GL, 2000
)
2.03
"Pleconaril is a novel compound that integrates into the capsid of picornaviruses, including enteroviruses and rhinoviruses, preventing the virus from attaching to cellular receptors and uncoating to release RNA into the cell."( Treatment of potentially life-threatening enterovirus infections with pleconaril.
Rotbart, HA; Webster, AD, 2001
)
1.27
"Pleconaril appears to be a promising drug for the treatment of enteroviral and rhinoviral infections."( Pleconaril: a novel antipicornaviral drug.
Romero, JR, 2001
)
2.47
"Pleconaril is an oral antiviral agent being developed by ViroPharma and Sanofi-Synthélabo (formerly Sterling Winthrop) for the potential treatment of several picornavirus-induced infections, including respiratory diseases and viral meningitis. "( Pleconaril Sanofi Synthélabo/ViroPharma.
Billich, A, 2000
)
3.19

Effects

ExcerptReferenceRelevance
"Pleconaril has demonstrated an excellent safety profile in dose escalation and clinical studies."( Pleconaril: a novel antipicornaviral drug.
Romero, JR, 2001
)
2.47

Treatment

Oral pleconaril treatment was studied in 2 parallel randomized, double-blind, placebo-controlled trials. Treatment increased the survival rate in all three models for both prophylactic and therapeutic dosing regimens.

ExcerptReferenceRelevance
"Oral pleconaril treatment was studied in 2 parallel randomized, double-blind, placebo-controlled trials."( Efficacy and safety of oral pleconaril for treatment of colds due to picornaviruses in adults: results of 2 double-blind, randomized, placebo-controlled trials.
Coats, TL; Collett, M; Cooper, EC; Hayden, FG; Herrington, DT; Hudson, S; Kim, K; Liu, S; McKinlay, M; Pevear, DC; Villano, SA, 2003
)
1.07
"Pleconaril treatment was associated with a more rapid loss of culturable virus."( Relationship of pleconaril susceptibility and clinical outcomes in treatment of common colds caused by rhinoviruses.
Barone, LR; Collett, MS; Demenczuk, TM; Hayden, FG; McKinlay, MA; Pevear, DC, 2005
)
1.4
"Pleconaril treatment reduced the beta-cells' insulin secretion in response to glucose stimulation in some experiments and induced slight morphological changes to the islets compared to untreated controls."( Antiviral treatment of Coxsackie B virus infection in human pancreatic islets.
Berg, AK; Frisk, G; Korsgren, O; Olsson, A, 2007
)
1.06
"Treatment with pleconaril increased the survival rate in all three models for both prophylactic and therapeutic dosing regimens."( Activity of pleconaril against enteroviruses.
Groarke, JM; Pevear, DC; Seipel, ME; Tull, TM, 1999
)
1.02

Pharmacokinetics

ExcerptReferenceRelevance
" Plasma concentration-versus-time data were curve fitted for each subject by using a nonlinear weighted least-squares algorithm, and pharmacokinetic parameters were determined from the polyexponential estimates."( Single-dose pharmacokinetics of a pleconaril (VP63843) oral solution and effect of food.
Abdel-Rahman, SM; Kearns, GL, 1998
)
0.58
" Plasma drug concentration-time data for each subject were fitted to the curve by using a nonlinear, weighted (weight = 1/Ycalc) least-squares algorithm, and model-dependent pharmacokinetic parameters were determined from the polyexponential parameter estimates."( Single-dose pharmacokinetics of a pleconaril (VP63843) oral solution in children and adolescents. Pediatric Pharmacology Research Unit Network.
Abdel-Rahman, SM; Blowey, DL; Jacobs, RF; James, LP; Kearns, GL; Marshall, JD; Wells, TG, 1999
)
0.58
" A significant difference in both Cmax and AUC was observed between study groups; however, this difference became insignificant when the parameters were corrected for dose."( Single oral dose escalation pharmacokinetics of pleconaril (VP 63843) capsules in adults.
Abdel-Rahman, SM; Kearns, GL, 1999
)
0.56
" Pharmacokinetic parameter estimates were determined by noncompartmental methods and compared between doses and with similar data obtained from a previous study of pleconaril disposition in children (n = 18, 2 to 12 years)."( Single dose pharmacokinetics of pleconaril in neonates. Pediatric Pharmacology Research Unit Network.
Abdel-Rahman, SM; Bradley, JS; Capparelli, EV; Jacobs, RF; James, LP; Johnson, KM; Kearns, GL, 2000
)
0.79

Bioavailability

Pleconaril is orally bioavailable and achieves serum concentrations in excess of those required to inhibit 90% of clinical rhino- and enteroviral isolates in vitro. The apparent age-dependent differences in the pharmacokinetics of ple Conaril may in part be related to increased bioavailability of the drug in older children and adults.

ExcerptReferenceRelevance
" The apparent bioavailability of pleconaril oral solution was significantly increased with the administration of food."( Single-dose pharmacokinetics of a pleconaril (VP63843) oral solution and effect of food.
Abdel-Rahman, SM; Kearns, GL, 1998
)
0.86
"Pleconaril (VP 63843) is a novel orally bioavailable small molecule with broad antipicornavirus (enterovirus and rhinovirus) activity."( Attenuated virulence of pleconaril-resistant coxsackievirus B3 variants.
Groarke, JM; Pevear, DC, 1999
)
2.05
"The apparent age-dependent differences in the pharmacokinetics of pleconaril may in part be related to increased bioavailability of the drug in older children and adults than in neonates."( Single dose pharmacokinetics of pleconaril in neonates. Pediatric Pharmacology Research Unit Network.
Abdel-Rahman, SM; Bradley, JS; Capparelli, EV; Jacobs, RF; James, LP; Johnson, KM; Kearns, GL, 2000
)
0.83
" Pleconaril is orally bioavailable and achieves serum concentrations in excess of those required to inhibit 90% of clinical rhino- and enteroviral isolates in vitro."( Pleconaril: a novel antipicornaviral drug.
Romero, JR, 2001
)
2.66

Dosage Studied

ExcerptRelevanceReference
" Treatment with pleconaril increased the survival rate in all three models for both prophylactic and therapeutic dosing regimens."( Activity of pleconaril against enteroviruses.
Groarke, JM; Pevear, DC; Seipel, ME; Tull, TM, 1999
)
1.03
" One 2-pyridone-containing 3CP inhibitor is shown to be bioavailable in the dog after oral dosing (F = 48%)."( Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 6. Structure-activity studies of orally bioavailable, 2-pyridone-containing peptidomimetics.
Batugo, MR; Brown, EL; Chen, L; Dragovich, PS; Ferre, RA; Fuhrman, SA; Gleeson, JP; Guzman, MC; Hendrickson, TF; Kosa, MB; Lee, CA; Liu, B; Maldonado, FC; Matthews, DA; Meador, JW; Patick, AK; Prins, TJ; Sakata, SK; Tuntland, T; Worland, ST; Zalman, LS; Zhou, R, 2002
)
0.31
" The infected subjects from the corresponding active and placebo groups (three-times daily dosing regimens) were combined for analysis."( Oral pleconaril treatment of picornavirus-associated viral respiratory illness in adults: efficacy and tolerability in phase II clinical trials.
Blatter, MM; Coats, T; Hassman, HA; Hayden, FG; Kim, K; Liu, S; Zhang, B, 2002
)
0.83
" Blood samples were collected during each day of midazolam dosing to determine plasma midazolam concentrations."( Duration of pleconaril effect on cytochrome P450 3A activity in healthy adults using the oral biomarker midazolam.
Bertino, JS; Liu, S; Ma, JD; Nafziger, AN; Rhodes, G, 2006
)
0.71
" Median effective dose was interpolated from the triplicated experiments and the dose-response curves were generated for each drug-virus combination."( A preclinical assessment to repurpose drugs to target type 1 diabetes-associated type B coxsackieviruses.
Honkimaa, A; Hyöty, H; Sioofy-Khojine, AB, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (24)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AR proteinHomo sapiens (human)Potency23.86750.000221.22318,912.5098AID1259243; AID1259247
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency20.45910.001022.650876.6163AID1224838; AID1224839; AID1224893
progesterone receptorHomo sapiens (human)Potency26.60320.000417.946075.1148AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency38.90180.01237.983543.2770AID1645841
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency23.71010.003041.611522,387.1992AID1159552; AID1159555
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency28.76730.001530.607315,848.9004AID1224848; AID1224849; AID1259403
pregnane X nuclear receptorHomo sapiens (human)Potency21.13170.005428.02631,258.9301AID1346982
GVesicular stomatitis virusPotency19.49710.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency21.87610.00108.379861.1304AID1645840
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency6.68190.001024.504861.6448AID743212
thyroid stimulating hormone receptorHomo sapiens (human)Potency14.18550.001628.015177.1139AID1259385; AID1259395
Interferon betaHomo sapiens (human)Potency19.49710.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency19.49710.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency19.49710.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency19.49710.01238.964839.8107AID1645842
[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)
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)30.05930.00011.774010.0000AID622597; AID622602
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)28.21410.00011.753610.0000AID622601; AID622606
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)25.68880.00002.015110.0000AID622600; AID622605
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)30.05930.00002.800510.0000AID622598; AID622603
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)30.05930.00002.398310.0000AID622599; AID622604
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC50 (µMol)0.25120.00203.519610.0000AID622607
Genome polyprotein Human rhinovirus sp.EC50 (µMol)0.05800.00500.09320.4400AID161553
Genome polyprotein Human rhinovirus 1AEC50 (µMol)16.09150.00400.10460.4900AID1386531; AID1386534; AID1386535; AID1386536; AID1386537; AID1386538; AID1386539; AID1386540
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

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

Biological Processes (96)

Processvia Protein(s)Taxonomy
negative regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic metabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
signal transductionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
steroid metabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of gene expressionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic catabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic transportNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group I member 2Homo sapiens (human)
cell differentiationNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group I member 2Homo sapiens (human)
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)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (59)

Processvia Protein(s)Taxonomy
RNA polymerase II transcription regulatory region sequence-specific DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear receptor activityNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
protein bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
zinc ion bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear receptor bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
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)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (29)

Processvia Protein(s)Taxonomy
nucleoplasmNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
transcription regulator complexNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear bodyNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
intermediate filament cytoskeletonNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
chromatinNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nucleusNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (292)

Assay IDTitleYearJournalArticle
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745855NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS 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.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745854NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1427855Cytotoxicity against African green monkey Vero cells assessed as growth inhibition after 48 hrs
AID84577Anti-HRV activity against HRV serotype 862003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
AID84570Anti-HRV activity against HRV serotype 452003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
AID1890694Cytotoxicity against human H1-HeLa cells assessed as reduction in cell viability by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID760198Antienteroviral activity against Human rhinovirus 39 infected in human HeLa Rh cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID1890711Antiviral activity against Human rhinovirus B14 infected in human H1-HeLa cells assessed as reduction in viral replication by measuring viral production measured 3 days post infection by crystal violet staining based plaque reduction assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID84564Anti-HRV activity against HRV serotype 142003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
AID1352178Antiviral activity against Coxsackievirus B5 Ohio-1 ATCC VR 29 infected in African green monkey Vero 76 cells after 3 days by plaque reduction assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Quinoxaline derivatives as new inhibitors of coxsackievirus B5.
AID1380017Cytotoxicity in un-infected human HeLa Rh cells assessed as reduction in cell viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Heterocyclic pharmacochemistry of new rhinovirus antiviral agents: A combined computational and experimental study.
AID674368Antiviral activity against Coxsackievirus B3 assessed as inhibition of viral replication2012Journal of natural products, Jun-22, Volume: 75, Issue:6
Alkaloids from the root of Isatis indigotica.
AID1445128Resistance index, ratio of EC50 for Human rhinovirus B14 harboring VP1 C199Y mutant infected in human HeLa Rh cells to EC50 for Human rhinovirus B14 infected in human H1HeLa cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID673872Antirhinoviral activity against Human rhinovirus B infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus.
AID161553Inhibition of HRV Protease 3CP (serotype 14).2002Journal of medicinal chemistry, Apr-11, Volume: 45, Issue:8
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 6. Structure-activity studies of orally bioavailable, 2-pyridone-containing peptidomimetics.
AID1503325Antiviral activity against Human enterovirus B Faulkner ATCC VR 185 infected in African green monkey Vero 76 cells assessed as protection against virus-induced cytopathic effect after 3 days by crystal violet staining-based plaque reduction assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Inhibitors of Yellow Fever Virus replication based on 1,3,5-triphenyl-4,5-dihydropyrazole scaffold: Design, synthesis and antiviral evaluation.
AID1386533Selectivity index, ratio of CC50 for human HeLa Rh cells to EC50 for Rhinovirus B14 capsid infected in human HeLa Rh cells2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID1386544Inhibition of Rhinovirus B14 capsid infected in human HeLa Rh cells assessed as number of wells with full cytopathic effect at 4 times EC50 concentration after 1st passage measured after 3 days by MTS assay relative to control2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID622604Time dependent inhibition of CYP2C192011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID1454151Antiviral activity against human rhinovirus 71 infected in human H1HeLa cells assessed as reduction in virus-induced cytopathicity incubated for 3 days by MTT assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Enterovirus inhibitory activity of C-8-tert-butyl substituted 4-aryl-6,7,8,9-tetrahydrobenzo[4,5]thieno[3,2-e][1,2,4]triazolo[4,3-a]pyrimidin-5(4H)-ones.
AID161529cytotoxicity against HRV Protease 3CP (serotype 14)2002Journal of medicinal chemistry, Apr-11, Volume: 45, Issue:8
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 6. Structure-activity studies of orally bioavailable, 2-pyridone-containing peptidomimetics.
AID1384981Antiviral activity against Human rhinovirus A71 infected in human H1HeLa cells assessed as inhibition of viral replication after 3 days by MTT assay2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
3-Aryl-1,2,4-oxadiazole Derivatives Active Against Human Rhinovirus.
AID1386534Inhibition of Rhinovirus A02 capsid infected in human HeLa Rh cells assessed as reduction in virus-induced cytopathic effect after 3 days by MTS assay2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID246109Effective concentration against HRV serotype 86 (assay was run at least six times)2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID1384979Antiviral activity against Human rhinovirus B14 infected in human H1HeLa cells assessed as inhibition of viral replication after 3 days by MTT assay2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
3-Aryl-1,2,4-oxadiazole Derivatives Active Against Human Rhinovirus.
AID1917974Selectivity index, ratio of CC50 for human RD cells to EC50 for Enterovirus-D68 STL-2014-12 infected in human RD cells to
AID316860Inhibition of HRV2 replication cycle progression2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Structure-based virtual screening for the discovery of natural inhibitors for human rhinovirus coat protein.
AID1386552Inhibition of Rhinovirus B14 capsid infected in human HeLa Rh cells assessed as number of wells with full cytopathic effect at EC50 concentration after 3rd passage measured after 3 days by MTS assay relative to control2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID1386537Inhibition of Rhinovirus A85 capsid infected in human HeLa Rh cells assessed as reduction in virus-induced cytopathic effect after 3 days by MTS assay2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID84567Anti-HRV activity against HRV serotype 22003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
AID84571Anti-HRV activity against HRV serotype 512003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
AID84578Anti-HRV activity against HRV serotype 892003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
AID1386543Antiviral activity against Rhinovirus B14 infected in human HeLa Rh cells assessed as reduction in viral replication at 1 uM administered at >= 2 hrs post infection measured after 8 hrs post infection by RT-qPCR analysis2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID760194Antienteroviral activity against Human rhinovirus 59 infected in human HeLa Rh cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID246106Effective concentration against HRV serotype 70 (assay was run at least six times)2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID760199Antienteroviral activity against Human rhinovirus 29 infected in human HeLa Rh cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID1261313Antiviral activity against YFV infected in BHK-21 cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1445119Antiviral activity against Human rhinovirus B14 infected in H1HeLa cells assessed as decrease in viral dsRNA at 6 times EC50 treated 1 hr prior to infection by DAPI staining based immunofluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID1736126Antiviral activity against pleconaril-resistant Coxsackievirus B3 97927 11207T/I1092 mutant infected in human HeLa cell line assessed as inhibition of virus-induced cytopathic effect measured after 48 hrs by crystal violet uptake assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel pleconaril derivatives: Influence of substituents in the isoxazole and phenyl rings on the antiviral activity against enteroviruses.
AID622589Antiviral activity against Human rhinovirus 2 infected in human HeLa Ohio cells assessed as inhibition of virus-induced cytopathic effect by CellTiter-Glo assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID1386541Inhibition of Rhinovirus B14 capsid infected in human HeLa Rh cells assessed as reduction in viral replication at 1 uM administered 2 hrs before infection measured after 8 hrs post infection by RT-qPCR analysis2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID1736143Induction of CYP3A4 (unknown origin) in hepatocytes using midazolam as substrate at 10 uM relative to control2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel pleconaril derivatives: Influence of substituents in the isoxazole and phenyl rings on the antiviral activity against enteroviruses.
AID316852Antiviral activity against HRV14 in HeLa cells2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Structure-based virtual screening for the discovery of natural inhibitors for human rhinovirus coat protein.
AID760208Antienteroviral activity against Human rhinovirus 14 infected in human HeLa cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID84574Anti-HRV activity against HRV serotype 702003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
AID1454150Antiviral activity against human rhinovirus 21 infected in human H1HeLa cells assessed as reduction in virus-induced cytopathicity incubated for 3 days by MTT assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Enterovirus inhibitory activity of C-8-tert-butyl substituted 4-aryl-6,7,8,9-tetrahydrobenzo[4,5]thieno[3,2-e][1,2,4]triazolo[4,3-a]pyrimidin-5(4H)-ones.
AID622592Unbound fraction in rat plasma2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID1503725Antiviral activity against Human rhinovirus serotype 14 infected in human HeLa cells assessed as reduction in virus-induced cytopathic effect after 24 to 36 hrs by MTT assay2017Journal of natural products, 10-27, Volume: 80, Issue:10
Phenylpropenoids from Bupleurum fruticosum as Anti-Human Rhinovirus Species A Selective Capsid Binders.
AID1654872Cytotoxicity in African green monkey Vero cells assessed as reduction in cell viability2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
2-((4-Arylpiperazin-1-yl)methyl)benzonitrile Derivatives as Orally Available Inhibitors of Hepatitis C Virus with a Novel Mechanism of Action.
AID622676Activation of human PXR expressed in african green monkey CV1 cells transfected with pSG5-hPXRDATG and (ER6)3-tk-CAT reporter assessed as maximal activation relative to control2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID1386549Inhibition of Rhinovirus B14 capsid infected in human HeLa Rh cells assessed as number of wells with full cytopathic effect at EC50 concentration after 2nd passage measured after 3 days by MTS assay relative to control2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID1503324Cytotoxicity against African green monkey Vero 76 cells assessed as decrease in cell viability after 48 to 96 hrs by MTT assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Inhibitors of Yellow Fever Virus replication based on 1,3,5-triphenyl-4,5-dihydropyrazole scaffold: Design, synthesis and antiviral evaluation.
AID1380016Antiviral activity against Human rhinovirus B14 infected in human HeLa Rh cells assessed as protection against virus induced cytopathic effect after 3 days in presence of 10% inactivated FBS by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Heterocyclic pharmacochemistry of new rhinovirus antiviral agents: A combined computational and experimental study.
AID316861Inhibition of HRV16 replication cycle progression2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Structure-based virtual screening for the discovery of natural inhibitors for human rhinovirus coat protein.
AID1445115Antiviral activity against Human poliovirus 3 infected in human HeLa cells assessed as protection against virus induced cytopathic effect after 2 days by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID1917977Selectivity index, ratio of CC50 for human RD cells to EC50 for Enterovirus-D68 US/KY/14-18953 infected in human RD cells
AID1261312Antiviral activity against BVDV infected in MDBK cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1917979Antiviral activity against Enterovirus-D68 US/MO/14-18947 infected in human RD cells assessed as reduction in virus induced cytopathic effect by measuring ATP level incubated for 72 hrs by cell titer-glo luminescent cell viability assay
AID1386536Inhibition of Rhinovirus A28 capsid infected in human HeLa Rh cells assessed as reduction in virus-induced cytopathic effect after 3 days by MTS assay2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID1890701Antiviral activity against Rhinovirus A33 infected in human H1-HeLa cells assessed as reduction in virus induced cytopathic effect incubated for 3 days by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID568502Antiviral activity against HRV-142011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Pharmacophore-based design, synthesis, and biological evaluation of novel chloro-pyridazine piperazines as human rhinovirus (HRV-3) inhibitors.
AID1386548Inhibition of Rhinovirus B14 capsid infected in human HeLa Rh cells assessed as number of wells with full cytopathic effect at 2 times EC50 concentration after 2nd passage measured after 3 days by MTS assay relative to control2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID1454149Antiviral activity against human rhinovirus 14 infected in human H1HeLa cells assessed as reduction in virus-induced cytopathicity incubated for 3 days by MTT assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Enterovirus inhibitory activity of C-8-tert-butyl substituted 4-aryl-6,7,8,9-tetrahydrobenzo[4,5]thieno[3,2-e][1,2,4]triazolo[4,3-a]pyrimidin-5(4H)-ones.
AID622602Time dependent inhibition of CYP1A22011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID1503327Antiviral activity against Enterovirus C Sabin ATCC VR 534 infected in African green monkey Vero 76 cells assessed as protection against virus-induced cytopathic effect after 2 days by crystal violet staining-based plaque reduction assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Inhibitors of Yellow Fever Virus replication based on 1,3,5-triphenyl-4,5-dihydropyrazole scaffold: Design, synthesis and antiviral evaluation.
AID246104Effective concentration against HRV serotype 59 (assay was run at least six times)2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID622603Time dependent inhibition of CYP2C92011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID1386546Inhibition of Rhinovirus B14 capsid infected in human HeLa Rh cells assessed as number of wells with full cytopathic effect at EC50 concentration after 1st passage measured after 3 days by MTS assay relative to control2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID673876Antirhinoviral activity against minor receptor-resistant Human rhinovirus infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus.
AID1890691Antiviral activity against Human rhinovirus B14 infected in human H1-HeLa cells assessed as reduction in virus induced cytopathic effect incubated for 3 days by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID1917980Selectivity index, ratio of CC50 for human RD cells to EC50 for Enterovirus-D68 US/MO/14-18947 infected in human RD cells
AID673877Ratio of EC50 for Human rhinovirus B to EC50 for Human rhinovirus A2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus.
AID1386554Inhibition of Rhinovirus B14 capsid infected in human HeLa Rh cells assessed as number of wells with full cytopathic effect at 2 times EC50 concentration after 4th passage measured after 3 days by MTS assay relative to control2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID760190Antienteroviral activity against Human rhinovirus 85 infected in human HeLa Rh cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID1445129Cytotoxicity against human HeLa Rh cells assessed as decrease in cell viability after 3 days by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID622596Apparent permeability of compound by PAMPA2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID1890693Antiviral activity against Human rhinovirus A71 infected in human H1-HeLa cells assessed as reduction in virus induced cytopathic effect incubated for 3 days by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID1386540Inhibition of Rhinovirus B70 capsid infected in human HeLa Rh cells assessed as reduction in virus-induced cytopathic effect after 3 days by MTS assay2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID1890699Antiviral activity against Human rhinovirus 2 infected in human H1-HeLa cells assessed as reduction in virus induced cytopathic effect incubated for 3 days by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID1890692Antiviral activity against Human rhinovirus A21 infected in human H1-HeLa cells assessed as reduction in virus induced cytopathic effect incubated for 3 days by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID760185Antienteroviral activity against poliovirus 3 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID1736124Antiviral activity against pleconaril-resistant Coxsackievirus B3 97927 11207K/I1092 mutant infected in human HeLa cell line assessed as inhibition of virus-induced cytopathic effect measured after 48 hrs by crystal violet uptake assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel pleconaril derivatives: Influence of substituents in the isoxazole and phenyl rings on the antiviral activity against enteroviruses.
AID84565Anti-HRV activity against HRV serotype 152003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
AID760189Antienteroviral activity against Human rhinovirus 86 infected in human HeLa Rh cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID1386539Inhibition of Rhinovirus B42 capsid infected in human HeLa Rh cells assessed as reduction in virus-induced cytopathic effect after 3 days by MTS assay2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID622588Antiviral activity against Human rhinovirus 14 infected in human HeLa Ohio cells assessed as inhibition of virus-induced cytopathic effect by CellTiter-Glo assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID1445127Resistance index, ratio of EC50 for Human rhinovirus B14 harboring VP1 A150V/E276K double mutant infected in human HeLa Rh cells to EC50 for Human rhinovirus B14 infected in human H1HeLa cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID760206Antienteroviral activity against Coxsackievirus B3 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID246084Effective concentration against HRV serotype 9 (assay was run at least six times)2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID1917970Antiviral activity against Enterovirus-D68 infected in human HeLa cells assessed as reduction in virus induced cytopathic effect incubated for 4 hrs by plaque reduction assay
AID297238Selectivity index, ratio of CC50 for HeLa cells to IC50 for HRV22007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Quantitative structure-activity relationship studies of [(biphenyloxy)propyl]isoxazole derivatives. Inhibitors of human rhinovirus 2 replication.
AID1890695Selectivity index, ratio of CC50 for cytotoxicity against human H1-HeLa cells to EC50 for antiviral activity against Human rhinovirus B14 infected in human H1-HeLa cells2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID1654869Antiviral activity against Coxsackievirus B3 infected in Vero cells assessed as reduction in virus-induced cytopathic effect incubated for 48 hrs by Reed-Muench method2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
2-((4-Arylpiperazin-1-yl)methyl)benzonitrile Derivatives as Orally Available Inhibitors of Hepatitis C Virus with a Novel Mechanism of Action.
AID760191Antienteroviral activity against Human rhinovirus 72 infected in human HeLa Rh cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID1386531Inhibition of Rhinovirus B14 capsid infected in human HeLa Rh cells assessed as reduction in virus-induced cytopathic effect after 3 days by MTS assay2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID1917973Cytotoxicity against human RD cells assessed as inhibition of cell viability by measuring ATP level incubated for 72 hrs by cell titer-glo luminescent cell viability assay
AID673879Ratio of EC50 for major receptor-resistant Human rhinovirus B to EC50 for minor receptor-resistant Human rhinovirus A2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus.
AID1235016Cytotoxicity against African green monkey Vero cells assessed as growth inhibition by CPE assay2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Bioactive Sesquiterpenes and Lignans from the Fruits of Xanthium sibiricum.
AID1445122Antiviral activity against Human rhinovirus A16 infected in H1HeLa cells assessed as decrease in viral dsRNA at 6 times EC50 treated 1 hr prior to infection by DAPI staining based immunofluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID622601Inhibition of CYP3A42011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID316851Antiviral activity against HRV1A in HeLa cells2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Structure-based virtual screening for the discovery of natural inhibitors for human rhinovirus coat protein.
AID1562985Cytotoxicity against human HeLa cells after 3 days by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Back to the future: Advances in development of broad-spectrum capsid-binding inhibitors of enteroviruses.
AID1890698Antiviral activity against Rhinovirus A1B infected in human H1-HeLa cells assessed as reduction in virus induced cytopathic effect incubated for 3 days by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID1890705Antiviral activity against Human rhinovirus 86 infected in human H1-HeLa cells assessed as reduction in virus induced cytopathic effect incubated for 3 days by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID1736129Antiviral activity against Rhinovirus B14 infected in human HeLa cell line assessed as inhibition of virus-induced cytopathic effect measured after 72 hrs by crystal violet uptake assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel pleconaril derivatives: Influence of substituents in the isoxazole and phenyl rings on the antiviral activity against enteroviruses.
AID1445111Antiviral activity against Human rhinovirus A71 infected in human H1HeLa cells assessed as protection against virus induced cytopathic effect after 3 days by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID246083Effective concentration against HRV serotype 2 (assay was run at least six times)2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID1917975Antiviral activity against Enterovirus-D68 US/KY/14-18953 infected in human RD cells assessed as reduction in virus induced cytopathic effect by measuring ATP level incubated for 72 hrs by cell titer-glo luminescent cell viability assay
AID760201Antienteroviral activity against Human rhinovirus 9 infected in human HeLa Rh cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID622606Time dependent inhibition of CYP3A42011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID84572Anti-HRV activity against HRV serotype 592003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
AID1736128Antiviral activity against Rhinovirus B5 infected in human HeLa cell line assessed as inhibition of virus-induced cytopathic effect measured after 72 hrs by crystal violet uptake assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel pleconaril derivatives: Influence of substituents in the isoxazole and phenyl rings on the antiviral activity against enteroviruses.
AID1736125Antiviral activity against pleconaril-resistant Coxsackievirus B3 97927 11207M/I1092 mutant infected in human HeLa cell line assessed as inhibition of virus-induced cytopathic effect measured after 48 hrs by crystal violet uptake assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel pleconaril derivatives: Influence of substituents in the isoxazole and phenyl rings on the antiviral activity against enteroviruses.
AID1386550Inhibition of Rhinovirus B14 capsid infected in human HeLa Rh cells assessed as number of wells with full cytopathic effect at 4 times EC50 concentration after 3rd passage measured after 3 days by MTS assay relative to control2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID84576Anti-HRV activity against HRV serotype 852003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
AID1261342Antiviral activity against Vaccinia virus2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1454144Antiviral activity against human poliovirus 3 infected in human HeLa cells assessed as reduction in virus-induced cytopathicity incubated for 3 days by MTT assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Enterovirus inhibitory activity of C-8-tert-butyl substituted 4-aryl-6,7,8,9-tetrahydrobenzo[4,5]thieno[3,2-e][1,2,4]triazolo[4,3-a]pyrimidin-5(4H)-ones.
AID1890702Antiviral activity against Rhinovirus A98 infected in human H1-HeLa cells assessed as reduction in virus induced cytopathic effect incubated for 3 days by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID760187Antienteroviral activity against Coxsackievirus A9 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID1352177Cytotoxicity against African green monkey Vero 76 cells assessed as reduction in cell viability after 48 to 96 hrs by MTT assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Quinoxaline derivatives as new inhibitors of coxsackievirus B5.
AID1261324Antiviral activity against HIV-1 infected in MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID760192Antienteroviral activity against Human rhinovirus 70 infected in human HeLa Rh cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID673874Antirhinoviral activity against antiviral-resistant Human rhinovirus B infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus.
AID163808Inhibitory activity against human rhinovirus-14 3C protease; Not applicable2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 8. Pharmacological optimization of orally bioavailable 2-pyridone-containing peptidomimetics.
AID316858Inhibition of HRV2 absorption on HeLa cells assessed as reduction in plaques at 0.25 ug/ml after 2 hrs2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Structure-based virtual screening for the discovery of natural inhibitors for human rhinovirus coat protein.
AID1261328Antiviral activity against WNV infected in BHK-21 cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1294752Antiviral activity against Human Rhinovirus A serotype 2 infected in HeLa Rh cells assessed as reduction of virus-induced cytopathic effect after 3 days by MTS assay2016European journal of medicinal chemistry, Jun-10, Volume: 115VP1 crystal structure-guided exploration and optimization of 4,5-dimethoxybenzene-based inhibitors of rhinovirus 14 infection.
AID246098Effective concentration against HRV serotype 15 (assay was run at least six times)2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID1204080Antiviral activity against Coxsackievirus B5 infected in African green monkey Vero 76 cells after 3 days by plaque reduction assay2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
N-((1,3-Diphenyl-1H-pyrazol-4-yl)methyl)anilines: A novel class of anti-RSV agents.
AID1445113Selectivity index, ratio of CC50 for human H1HeLa cells to EC50 for Human rhinovirus A21 infected in human H1HeLa cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID760200Antienteroviral activity against Human rhinovirus 15 infected in human HeLa Rh cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID84566Anti-HRV activity against HRV serotype 162003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
AID1445125Antiviral activity against Human rhinovirus B14 harboring VP1 A150V/E276K double mutant infected in human HeLa Rh cells assessed as protection against virus induced cytopathic effect after 3 days by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID622681Lipophilicity, log D of the compound2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID84569Anti-HRV activity against HRV serotype 392003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
AID1386551Inhibition of Rhinovirus B14 capsid infected in human HeLa Rh cells assessed as number of wells with full cytopathic effect at 2 times EC50 concentration after 3rd passage measured after 3 days by MTS assay relative to control2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID622607Activation of human PXR expressed in african green monkey CV1 cells transfected with pSG5-hPXRDATG and (ER6)3-tk-CAT reporter2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID246103Effective concentration against HRV serotype 51 (assay was run at least six times)2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID1204074Cytotoxicity against African green monkey Vero 76 cells assessed as cell viability after 48 to 96 hrs by MTT method2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
N-((1,3-Diphenyl-1H-pyrazol-4-yl)methyl)anilines: A novel class of anti-RSV agents.
AID246110Effective concentration against HRV serotype 89 (assay was run at least six times)2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID246060Median effective concentration against HRV serotypes; Number of serotypes 162005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID1261308Cytotoxicity against human MT4 cells assessed as cell viability after 96 hrs by MTT assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID760195Antienteroviral activity against Human rhinovirus 45 infected in human HeLa Rh cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID622594Intrinsic clearance in Sprague-Dawley rat hepatocytes assessed per 10'6 cells preincubated for 5 mins measured after 90 mins2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID1454146Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 3 days by MTT assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Enterovirus inhibitory activity of C-8-tert-butyl substituted 4-aryl-6,7,8,9-tetrahydrobenzo[4,5]thieno[3,2-e][1,2,4]triazolo[4,3-a]pyrimidin-5(4H)-ones.
AID316853Antiviral activity against HRV16 in HeLa cells2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Structure-based virtual screening for the discovery of natural inhibitors for human rhinovirus coat protein.
AID1261315Antiviral activity against human CVB5 infected in african green monkey Vero76 cells assessed as inhibition of virus-induced cytopathogenicity after 3 days by plaque reduction assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1454145Antiviral activity against human coxsackievirus B3 infected in human HeLa cells assessed as reduction in virus-induced cytopathicity incubated for 3 days by MTT assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Enterovirus inhibitory activity of C-8-tert-butyl substituted 4-aryl-6,7,8,9-tetrahydrobenzo[4,5]thieno[3,2-e][1,2,4]triazolo[4,3-a]pyrimidin-5(4H)-ones.
AID1386542Antiviral activity against Rhinovirus B14 infected in human HeLa Rh cells assessed as reduction in viral replication at 1 uM administered at the time of infection measured after 8 hrs post infection by RT-qPCR analysis2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID1454148Cytotoxicity in human H1HeLa cells assessed as reduction in cell viability incubated for 3 days by MTT assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Enterovirus inhibitory activity of C-8-tert-butyl substituted 4-aryl-6,7,8,9-tetrahydrobenzo[4,5]thieno[3,2-e][1,2,4]triazolo[4,3-a]pyrimidin-5(4H)-ones.
AID622599Inhibition of CYP2C192011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID1654875Selectivity index, ratio of CC50 for cytotoxicity in African green monkey Vero cells to EC50 for Antiviral activity against Coxsackievirus B3 infected in Vero cells2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
2-((4-Arylpiperazin-1-yl)methyl)benzonitrile Derivatives as Orally Available Inhibitors of Hepatitis C Virus with a Novel Mechanism of Action.
AID1890714Antiviral activity against Human rhinovirus B14 infected in human H1-HeLa cells assessed as reduction in viral titre at 1 uM pretreated for 1 hr followed by viral infection and measured immediately by time-of-addition assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID622595Chemical stability of compound assessed as half life2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID1917976Antiviral activity against Enterovirus-D68 fermon infected in human RD cells assessed as reduction in virus induced cytopathic effect by measuring ATP level incubated for 72 hrs by cell titer-glo luminescent cell viability assay
AID1204081Antiviral activity against Poliovirus Sb-1 infected in African green monkey Vero 76 cells after 2 days by plaque reduction assay2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
N-((1,3-Diphenyl-1H-pyrazol-4-yl)methyl)anilines: A novel class of anti-RSV agents.
AID622593Intrinsic clearance in human microsomes after 45 mins by HPLC method2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID1890700Antiviral activity against Human rhinovirus 16 infected in human H1-HeLa cells assessed as reduction in virus induced cytopathic effect incubated for 3 days by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID23851t1/2 in monkey liver microsomes1995Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8
Picornavirus inhibitors: trifluoromethyl substitution provides a global protective effect against hepatic metabolism.
AID1445112Selectivity index, ratio of CC50 for human H1HeLa cells to EC50 for Human rhinovirus B14 infected in human H1HeLa cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID316855Selectivity index, ratio of CC50 for HeLa cells to IC50 for HRV2 in HeLa cells2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Structure-based virtual screening for the discovery of natural inhibitors for human rhinovirus coat protein.
AID1235015Antiviral activity against Coxsackievirus B3 infected in African green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Bioactive Sesquiterpenes and Lignans from the Fruits of Xanthium sibiricum.
AID1445110Cytotoxicity against human H1HeLa cells assessed as decrease in cell viability after 3 days by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID1427861Selectivity index, ratio of TC50 for African green monkey Vero cells to IC50 for Coxsackievirus B3 infected in African green monkey Vero cells
AID1445120Antiviral activity against Human rhinovirus B14 infected in H1HeLa cells assessed as decrease in viral dsRNA at 6 times EC50 treated simultaneously with infection by DAPI staining based immunofluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID246105Effective concentration against HRV serotype 63 (assay was run at least six times)2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID1427860Antiviral activity against Coxsackievirus B3 infected in African green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect
AID1503326Selectivity index, ratio of CC50 for African green monkey Vero 76 cells to EC50 for Human coxsackievirus B5 Faulkner2017European journal of medicinal chemistry, Dec-01, Volume: 141Inhibitors of Yellow Fever Virus replication based on 1,3,5-triphenyl-4,5-dihydropyrazole scaffold: Design, synthesis and antiviral evaluation.
AID1736121Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs measured by crystal violet based micro plate reader method2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel pleconaril derivatives: Influence of substituents in the isoxazole and phenyl rings on the antiviral activity against enteroviruses.
AID1386555Inhibition of Rhinovirus B14 capsid infected in human HeLa Rh cells assessed as number of wells with full cytopathic effect at EC50 concentration after 4th passage measured after 3 days by MTS assay relative to control2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID84573Anti-HRV activity against HRV serotype 632003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
AID1261310Cytotoxicity against BHK cells assessed as cell viability after 48 to 96 hrs by MTT assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID760196Antienteroviral activity against Human rhinovirus 42 infected in human HeLa Rh cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID1917978Selectivity index, ratio of CC50 for human RD cells to EC50 for Enterovirus-D68 fermon infected in human RD cells
AID1454147Antiviral activity against human coxsackievirus B1 infected in human HeLa cells assessed as reduction in virus-induced cytopathicity incubated for 3 days by MTT assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Enterovirus inhibitory activity of C-8-tert-butyl substituted 4-aryl-6,7,8,9-tetrahydrobenzo[4,5]thieno[3,2-e][1,2,4]triazolo[4,3-a]pyrimidin-5(4H)-ones.
AID316856Inactivation of HRV2 assessed as reduction in plaque at 0.25 ug/ml after 1 hr2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Structure-based virtual screening for the discovery of natural inhibitors for human rhinovirus coat protein.
AID1386532Cytotoxicity against human HeLa Rh cells assessed as reduction in cell viability after 3 days by MTS assay2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID622587Antiviral activity against Human rhinovirus 16 infected in human HeLa Ohio cells assessed as inhibition of virus-induced cytopathic effect by CellTiter-Glo assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID246102Effective concentration against HRV serotype 45 (assay was run at least six times)2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID760186Antienteroviral activity against poliovirus 2 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID1445117Selectivity index, ratio of CC50 for human HeLa cells to EC50 for human poliovirus 3 infected in human HeLa cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID1386545Inhibition of Rhinovirus B14 capsid infected in human HeLa Rh cells assessed as number of wells with full cytopathic effect at 2 times EC50 concentration after 1st passage measured after 3 days by MTS assay relative to control2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID760202Antienteroviral activity against Human rhinovirus 2 infected in human HeLa Rh cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID1890706Antiviral activity against Rhinovirus B91 infected in human H1-HeLa cells assessed as reduction in virus induced cytopathic effect incubated for 3 days by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID1261340Antiviral activity against HSV12015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID84568Anti-HRV activity against HRV serotype 292003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
AID1261314Antiviral activity against Reo-1 virus infected in BHK-21 cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1294749Antiviral activity against Human Rhinovirus B serotype 14 infected in HeLa Rh cells assessed as reduction of virus-induced cytopathic effect after 3 days by MTS assay2016European journal of medicinal chemistry, Jun-10, Volume: 115VP1 crystal structure-guided exploration and optimization of 4,5-dimethoxybenzene-based inhibitors of rhinovirus 14 infection.
AID1386547Inhibition of Rhinovirus B14 capsid infected in human HeLa Rh cells assessed as number of wells with full cytopathic effect at 4 times EC50 concentration after 2nd passage measured after 3 days by MTS assay relative to control2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID316862Selectivity for HRV2 over HRV162008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Structure-based virtual screening for the discovery of natural inhibitors for human rhinovirus coat protein.
AID1261341Antiviral activity against VSV2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1890696Selectivity index, ratio of CC50 for cytotoxicity against human H1-HeLa cells to EC50 for antiviral activity against Human rhinovirus A21 infected in human H1-HeLa cells2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID1294750Cytotoxicity against human HeLa Rh cells assessed as cell viability by light microscopy2016European journal of medicinal chemistry, Jun-10, Volume: 115VP1 crystal structure-guided exploration and optimization of 4,5-dimethoxybenzene-based inhibitors of rhinovirus 14 infection.
AID297237Antiviral activity against HRV2 in HeLa cells by CPE assay2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Quantitative structure-activity relationship studies of [(biphenyloxy)propyl]isoxazole derivatives. Inhibitors of human rhinovirus 2 replication.
AID1503724Cytotoxicity against human HeLa cells assessed as decrease in cell viability after 72 hrs by MTT assay2017Journal of natural products, 10-27, Volume: 80, Issue:10
Phenylpropenoids from Bupleurum fruticosum as Anti-Human Rhinovirus Species A Selective Capsid Binders.
AID622590Aqueous equilibrium solubility of the compound by shake-flask technique2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID673878Ratio of EC50 for antiviral-resistant Human rhinovirus B to EC50 for antiviral-resistant Human rhinovirus A2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus.
AID1890704Antiviral activity against Human rhinovirus 42 infected in human H1-HeLa cells assessed as reduction in virus induced cytopathic effect incubated for 3 days by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID316854Cytotoxicity against human HeLa cells after 72 hrs2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Structure-based virtual screening for the discovery of natural inhibitors for human rhinovirus coat protein.
AID84561In vitro anti-rhinoviral activity against human rhinovirus serotypes 2,3,9,14,16,25 and 392003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 8. Pharmacological optimization of orally bioavailable 2-pyridone-containing peptidomimetics.
AID622591Unbound fraction in human plasma2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID246097Effective concentration against HRV serotype 14 (assay was run at least six times)2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID1384980Antiviral activity against Human rhinovirus A21 infected in human H1HeLa cells assessed as inhibition of viral replication after 3 days by MTT assay2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
3-Aryl-1,2,4-oxadiazole Derivatives Active Against Human Rhinovirus.
AID1736123Antiviral activity against wild type Coxsackievirus B3 97927 infected in human HeLa cell line assessed as inhibition of virus-induced cytopathic effect measured after 48 hrs by crystal violet uptake assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel pleconaril derivatives: Influence of substituents in the isoxazole and phenyl rings on the antiviral activity against enteroviruses.
AID1445126Antiviral activity against Human rhinovirus B14 harboring VP1 C199Y mutant infected in human HeLa Rh cells assessed as protection against virus induced cytopathic effect after 3 days by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID84579Anti-HRV activity against HRV serotype 92003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
AID1445116Cytotoxicity aganist human HeLa cells assessed as decrease in cell viability after 2 days by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID1384978Cytotoxicity against human H1HeLa cells assessed as reduction in cell viability after 3 days by MTT assay2018ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7
3-Aryl-1,2,4-oxadiazole Derivatives Active Against Human Rhinovirus.
AID19547Tested for pharmacokinetic parameter in fasted Beagle dogs (Half-life) iv administration.1995Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8
Picornavirus inhibitors: trifluoromethyl substitution provides a global protective effect against hepatic metabolism.
AID1261323Selectivity index, ratio of CC50 for african green monkey Vero76 cells to EC50 for human Sb-12015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1736127Antiviral activity against Rhinovirus A2 infected in human HeLa cell line assessed as inhibition of virus-induced cytopathic effect measured after 72 hrs by crystal violet uptake assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel pleconaril derivatives: Influence of substituents in the isoxazole and phenyl rings on the antiviral activity against enteroviruses.
AID14911Tested for pharmacokinetic parameter in fasted Beagle dogs (Area Under Curve value) iv administration.1995Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8
Picornavirus inhibitors: trifluoromethyl substitution provides a global protective effect against hepatic metabolism.
AID1445109Antiviral activity against Human rhinovirus A21 infected in human H1HeLa cells assessed as protection against virus induced cytopathic effect after 3 days by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID246100Effective concentration against HRV serotype 29 (assay was run at least six times)2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID673875Antirhinoviral activity against major receptor-resistant Human rhinovirus infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus.
AID1503726Antiviral activity against Human rhinovirus serotype 39 infected in human HeLa cells assessed as reduction in virus-induced cytopathic effect after 24 to 36 hrs by MTT assay2017Journal of natural products, 10-27, Volume: 80, Issue:10
Phenylpropenoids from Bupleurum fruticosum as Anti-Human Rhinovirus Species A Selective Capsid Binders.
AID760193Antienteroviral activity against Human rhinovirus 63 infected in human HeLa Rh cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID246101Effective concentration against HRV serotype 39 (assay was run at least six times)2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID622600Inhibition of CYP2D62011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID1261311Cytotoxicity against african green monkey Vero 76 cells assessed as cell viability after 48 to 96 hrs by crystal violet staining method2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID760197Antienteroviral activity against Human rhinovirus 41 infected in human HeLa Rh cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID1562984Antiviral activity against Enterovirus clinical isolate2019European journal of medicinal chemistry, Sep-15, Volume: 178Back to the future: Advances in development of broad-spectrum capsid-binding inhibitors of enteroviruses.
AID1445107Antiviral activity against Human rhinovirus B14 infected in H1HeLa cells assessed as decrease in viral dsRNA at 6 times EC50 treated every 1 hr for 9 hrs after infection by DAPI staining based immunofluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID622597Inhibition of CYP1A22011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID1235017Selectivity index, ratio of TC50 for African green monkey Vero cells to IC50 for Coxsackievirus B3-induced cytopathic effect in African green monkey Vero cells2015Journal of natural products, Jul-24, Volume: 78, Issue:7
Bioactive Sesquiterpenes and Lignans from the Fruits of Xanthium sibiricum.
AID1918004Antiviral activity against Enterovirus D68 infected in human RD cells assessed as reduction in thermal inactivation of virus at 55 degreeC at 12.5 uM incubated for 72 hrs by TCID50 assay
AID1736144Induction of CYP3A4 (unknown origin) in hepatocytes using midazolam as substrate at 1 uM relative to control2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel pleconaril derivatives: Influence of substituents in the isoxazole and phenyl rings on the antiviral activity against enteroviruses.
AID760188Antienteroviral activity against Human rhinovirus 89 infected in human HeLa Rh cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID84575Anti-HRV activity against HRV serotype 722003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
AID1261309Cytotoxicity against MDBK cells assessed as cell viability after 48 to 96 hrs by MTT assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1056521Antiviral activity against Coxsackie virus B3 assessed as inhibition of viral replication2013Journal of natural products, Dec-27, Volume: 76, Issue:12
Homosecoiridoid alkaloids with amino acid units from the flower buds of Lonicera japonica.
AID1445114Selectivity index, ratio of CC50 for human H1HeLa cells to EC50 for Human rhinovirus A71 infected in human H1HeLa cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID1261326Antiviral activity against DENV-2 infected in BHK-21 cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID760205Antienteroviral activity against poliovirus 1 infected in african green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID1379348Inhibition of Enterovirus 71 Shenzhen/120F1/09 capsid infected in human RD cells assessed as reduction in virus-induced cell death after 72 hrs by CCK-8 assay2017ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
Discovery of Potent EV71 Capsid Inhibitors for Treatment of HFMD.
AID1890697Selectivity index, ratio of CC50 for cytotoxicity against human H1-HeLa cells to EC50 for antiviral activity against Human rhinovirus A71 infected in human H1-HeLa cells2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID297239Cytotoxicity against human HeLa cells2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Quantitative structure-activity relationship studies of [(biphenyloxy)propyl]isoxazole derivatives. Inhibitors of human rhinovirus 2 replication.
AID1386553Inhibition of Rhinovirus B14 capsid infected in human HeLa Rh cells assessed as number of wells with full cytopathic effect at 4 times EC50 concentration after 4th passage measured after 3 days by MTS assay relative to control2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID1445123Antiviral activity against Human rhinovirus A16 infected in H1HeLa cells assessed as decrease in viral dsRNA at 6 times EC50 treated simultaneously with infection by DAPI staining based immunofluorescence assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID246107Effective concentration against HRV serotype 72 (assay was run at least six times)2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID1445108Antiviral activity against Human rhinovirus B14 infected in human H1HeLa cells assessed as protection against virus induced cytopathic effect after 3 days by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID1261317Antiviral activity against Human poliovirus 1 Sabin infected in african green monkey Vero76 cells assessed as inhibition of virus-induced cytopathogenicity by plaque reduction assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID673873Antirhinoviral activity against antiviral-resistant Human rhinovirus A infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus.
AID1380018Selectivity index, ratio of CC50 for un-infected human HeLa Rh cells to EC50 for Human rhinovirus B14 infected in human HeLa Rh cells2017European journal of medicinal chemistry, Nov-10, Volume: 140Heterocyclic pharmacochemistry of new rhinovirus antiviral agents: A combined computational and experimental study.
AID246108Effective concentration against HRV serotype 85 (assay was run at least six times)2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID1386535Inhibition of Rhinovirus A08 capsid infected in human HeLa Rh cells assessed as reduction in virus-induced cytopathic effect after 3 days by MTS assay2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID246099Effective concentration against HRV serotype 16 (assay was run at least six times)2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
2-Ethoxybenzoxazole as a bioisosteric replacement of an ethyl benzoate group in a human rhinovirus (HRV) capsid binder.
AID1261319Selectivity index, ratio of CC50 for BHK-21 cells to EC50 for YFV2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID1917972Antiviral activity against Enterovirus-D68 STL-2014-12 infected in human RD cells assessed as reduction in virus induced cytopathic effect by measuring ATP level incubated for 72 hrs by cell titer-glo luminescent cell viability assay
AID256497Cytostatic concentration against WI-38 cells2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Pharmacophore modeling, docking, and principal component analysis based clustering: combined computer-assisted approaches to identify new inhibitors of the human rhinovirus coat protein.
AID622605Time dependent inhibition of CYP2D62011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
AID316850Antiviral activity against HRV2 in HeLa cells2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Structure-based virtual screening for the discovery of natural inhibitors for human rhinovirus coat protein.
AID1261316Antiviral activity against human RSV infected in african green monkey Vero76 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by plaque reduction assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.
AID673871Antirhinoviral activity against Human rhinovirus A infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012ACS medicinal chemistry letters, Apr-12, Volume: 3, Issue:4
An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus.
AID1445118Antiviral activity against Human rhinovirus A16 infected in human H1HeLa cells assessed as protection against virus induced cytopathic effect after 3 days by MTT assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication.
AID15655Tested for pharmacokinetic parameter in fasted Beagle dogs (Clearance value of the compound) iv administration.1995Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8
Picornavirus inhibitors: trifluoromethyl substitution provides a global protective effect against hepatic metabolism.
AID760203Antienteroviral activity against Enterovirus 71 infected in human RD cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTS assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
AID1890703Antiviral activity against Rhinovirus B27 infected in human H1-HeLa cells assessed as reduction in virus induced cytopathic effect incubated for 3 days by MTT assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode.
AID1386538Inhibition of Rhinovirus A89 capsid infected in human HeLa Rh cells assessed as reduction in virus-induced cytopathic effect after 3 days by MTS assay2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.
AID1736122Antiviral activity against Coxsackievirus B3 Nancy infected in human HeLa cell line assessed as inhibition of virus-induced cytopathic effect measured after 48 hrs by crystal violet uptake assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel pleconaril derivatives: Influence of substituents in the isoxazole and phenyl rings on the antiviral activity against enteroviruses.
AID622598Inhibition of CYP2C92011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (136)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's14 (10.29)18.2507
2000's51 (37.50)29.6817
2010's53 (38.97)24.3611
2020's18 (13.24)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 46.00

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

MetricThis Compound (vs All)
Research Demand Index46.00 (24.57)
Research Supply Index5.06 (2.92)
Research Growth Index4.79 (4.65)
Search Engine Demand Index70.86 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (46.00)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials16 (11.43%)5.53%
Reviews21 (15.00%)6.00%
Case Studies10 (7.14%)4.05%
Observational0 (0.00%)0.25%
Other93 (66.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Double-Blind, Placebo-Controlled, Virologic Efficacy Trial of Pleconaril in the Treatment of Neonates With Enteroviral Sepsis Syndrome [NCT00031512]Phase 261 participants (Actual)Interventional2001-06-30Completed
A Placebo-Controlled Study of the Effects of Pleconaril Nasal Spray on Common Cold Symptoms and Asthma Exacerbations Following Rhinovirus Exposure [NCT00394914]Phase 2311 participants (Actual)Interventional2006-08-31Completed
The Diabetes Virus Detection and Intervention Trial [NCT04838145]Phase 296 participants (Actual)Interventional2018-08-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00394914 (10) [back to overview]Percentage of Participants With Asthma Exacerbations Together With Rhinovirus-Positive PCR
NCT00394914 (10) [back to overview]Percentage of Participants With Rhinovirus PCR-Positive Colds
NCT00394914 (10) [back to overview]LS Mean Change From Baseline in Asthma-Related Sleep Interference
NCT00394914 (10) [back to overview]LS Mean Change From Baseline in Forced Expiratory Volume in 1 Second (FEV1)
NCT00394914 (10) [back to overview]LS Mean Change From Baseline in Peak Expiratory Flow (PEF) in AM
NCT00394914 (10) [back to overview]LS Mean Change From Baseline in Peak Expiratory Flow (PEF) in PM
NCT00394914 (10) [back to overview]LS Mean Change From Baseline in Short-acting Beta-Agonist (SABA) Rescue Medication Usage
NCT00394914 (10) [back to overview]LS Mean Change From Baseline in the Asthma Control Questionnaire (ACQ)
NCT00394914 (10) [back to overview]LS Mean Change From Baseline in Total Asthma Symptom Score
NCT00394914 (10) [back to overview]LS Mean Change From Baseline in Total Cold Symptom Score

Percentage of Participants With Asthma Exacerbations Together With Rhinovirus-Positive PCR

"Asthma exacerbation was defined as a participant having one of the following:~0.5 point or more increase in the Asthma Control Questionnaire (ACQ) from Baseline at Day 7. The ACQ is a validated instrument containing 7 questions to assess asthma control which incorporates symptoms, beta-agonist use, and spirometry. Participants recall their experiences during the previous 7 days and respond to each question using a 7-point scale. The items are equally weighted and the ACQ score is the mean of the 7 items and therefore ranges between 0 (well controlled) and 6 (extremely poorly controlled). The ACQ completed on the day of exposure was the Baseline ACQ.~Any change to asthma treatment as prescribed by a physician, unscheduled contact (either office visit or phone contact where medication was changed for asthma symptoms), emergency room visit, or hospitalization.~PCR+ was defined as positive or equivocal outcome of the picornavirus test any time after randomization." (NCT00394914)
Timeframe: From time of exposure to index case to end of Follow-up Period (21 days)

Interventionpercentage of participants (Number)
Pleconaril1.3
Placebo2.5

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Percentage of Participants With Rhinovirus PCR-Positive Colds

The common cold was defined as moderate or severe rhinorrhea and at least one other cold symptom of moderate to severe intensity for at least 1 day, together with rhinovirus-positive polymerase chain reaction (PCR), after a participant had temporal exposure to an index case. PCR+ was defined as positive or equivocal outcome of the picornavirus test any time after randomization. (NCT00394914)
Timeframe: From time of exposure to index case to end of Follow-up Period (21 days)

Interventionpercentage of participants (Number)
Pleconaril2.6
Placebo2.5

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LS Mean Change From Baseline in Forced Expiratory Volume in 1 Second (FEV1)

FEV1 is the volume of air that can forcibly be blown out in one second, after full inspiration. Pooled SDs and LS means were calculated based on an ANOVA model. (NCT00394914)
Timeframe: Baseline through the Final Visit (Day 21)

,
Interventionliters (Least Squares Mean)
Baseline (n=152, n=156)Change From BL to Day 2 (n=111, n=115)Change From BL to Day 4 (n=97, n=102)Change From BL to Day 8 (n=132, n=135)Change From BL to Day 10 (n=116, n=120)Change From BL to Day 14 (n=140, n=139)Change From BL to Day 21 (n=141, n=146)Change From BL to Final Visit (n=152, n=156)
Placebo2.214-0.100-0.141-0.121-0.109-0.090-0.133-0.141
Pleconaril2.335-0.091-0.059-0.070-0.090-0.063-0.080-0.076

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LS Mean Change From Baseline in Peak Expiratory Flow (PEF) in AM

PEF is a person's maximum speed of expiration as measured with a peak flow meter and was measured twice daily in the morning (AM) and evening (PM). Pooled SDs and LS means were calculated based on an ANOVA model. (NCT00394914)
Timeframe: Baseline through the Final Visit (Day 21)

,
InterventionL/min (Least Squares Mean)
Baseline (n=124, n=136)Change From BL to Day 2 (n=108, n=123)Change From BL to Day 3 (n=103, n=120)Change From BL to Day 4 (n=103, n=118)Change From BL to Day 5 (n=96, n=122)Change From BL to Day 6 (n=104, n=114)Change From BL to Day 7 (n=102, n=112)Change From BL to Day 8 (n=102, n=116)Change From BL to Day 9 (n=105, n=114)Change From BL to Day 10 (n=90, n=102)Change From BL to Day 11 (n=95, n=108)Change From BL to Day 12 (n=94, n=102)Change From BL to Day 13 (n=88, n=97)Change From BL to Day 14 (n=90, n=103)Change From BL to Day 15 (n=91, n=107)Change From BL to Day 16 (n=92, n=101)Change From BL to Day 17 (n=74, n=93)Change From BL to Day 18 (n=80, n=98)Change From BL to Day 19 (n=81, n=102)Change From BL to Day 20 (n=76, n=88)Change From BL to Day 21 (n=62, n=85)Change From BL to Final Day (n=124, n=136)Change From BL to Week 1 (n=122, n=136)Change From BL to Week 2 (n=119, n=134)Change From BL to Week 3 (n=109, n=127)Change From BL to Final Week (n=124, n=136)
Placebo284.0-1.96.1-1.1-3.42.5-4.0-0.98.10.6-0.611.57.723.53.9-1.7-6.910.84.110.4-1.4-5.2-2.24.5-1.1-3.8
Pleconaril306.2-0.19.95.10.20.22.5-0.613.67.7-3.93.24.73.4-3.24.46.00.71.210.210.54.6-0.71.45.22.3

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LS Mean Change From Baseline in Peak Expiratory Flow (PEF) in PM

PEF is a person's maximum speed of expiration as measured with a peak flow meter and was measured twice daily in the morning (AM) and evening (PM). Pooled SDs and LS means were calculated based on an ANOVA model. (NCT00394914)
Timeframe: Baseline through the Final Visit (Day 21)

,
InterventionL/min (Least Squares Mean)
Baseline (n=119, n=128)Change From BL to Day 1 (n=93, n=105)Change From BL to Day 2 (n=102, n=115)Change From BL to Day 3 (n=98, n=112)Change From BL to Day 4 (n=98, n=108)Change From BL to Day 5 (n=105, n=109)Change From BL to Day 6 (n=98, n=108)Change From BL to Day 7 (n=95, n=106)Change From BL to Day 8 (n=94, n=106)Change From BL to Day 9 (n=91, n=103)Change From BL to Day 10 (n=91, n=99)Change From BL to Day 11 (n=83, n=97)Change From BL to Day 12 (n=82, n=90)Change From BL to Day 13 (n=85, n=98)Change From BL to Day 14 (n=80, n=98)Change From BL to Day 15 (n=88, n=89)Change From BL to Day 16 (n=82, n=84)Change From BL to Day 17 (n=81, n=93)Change From BL to Day 18 (n=84, n=97)Change From BL to Day 19 (n=80, n=93)Change From BL to Day 20 (n=78, n=80)Change From BL to Day 21 (n=47, n=63)Change From BL to Final Day (n=119, n=128)Change From BL to Week 1 (n=116, n=127)Change From BL to Week 2 (n=113, n=124)Change From BL to Week 3 (n=103, n=117)Change From BL to Final Week (n=119, n=128)
Placebo293.41.00.4-14.73.11.6-9.8-1.620.2-3.49.11.08.98.11.7-9.0-6.1-1.13.712.312.612.314.7-2.06.03.58.1
Pleconaril310.90.42.02.38.2-3.7-3.510.011.23.59.2-3.0-2.69.32.4-0.2-6.8-1.13.2-1.016.2-7.510.42.53.4-3.53.1

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LS Mean Change From Baseline in Short-acting Beta-Agonist (SABA) Rescue Medication Usage

SABAs such as albuterol were permitted during the study as rescue medication and required a 6-hour washout prior to each visit. Participants entered their asthma medication use into an e-diary twice daily beginning at the Screening Visit through completion of the study. The Baseline for diary symptoms was the average of the last seven assessments prior to Randomization. Pooled SDs and LS means were calculated based on an ANOVA model. (NCT00394914)
Timeframe: Baseline through the Final Visit (Day 21)

,
Interventionnumber of puffs of SABA (Least Squares Mean)
Baseline (n=143, n=148)Change From BL to Day 1 (n=131, n=138)Change From BL to Day 2 (n=137, n=146)Change From BL to Day 3 (n=135, n=146)Change From BL to Day 4 (n=137, n=147)Change From BL to Day 5 (n=135, n=147)Change From BL to Day 6 (n=131, n=146)Change From BL to Day 7 (n=135, n=144)Change From BL to Day 8 (n=129, n=141)Change From BL to Day 9 (n=131, n=142)Change From BL to Day 10 (n=130, n=144)Change From BL to Day 11 (n=128, n=141)Change From BL to Day 12 (n=129, n=139)Change From BL to Day 13 (n=130, n=139)Change From BL to Day 14 (n=131, n=140)Change From BL to Day 15 (n=126, n=137)Change From BL to Day 16 (n=126, n=136)Change From BL to Day 17 (n=127, n=138)Change From BL to Day 18 (n=130, n=139)Change From BL to Day 19 (n=121, n=133)Change From BL to Day 20 (n=108, n=118)Change From BL to Day 21 (n=78, n=83)Change From BL to Final Day (n=143, n=148)Change From BL to Week 1 (n=142, n=148)Change From BL to Week 2 (n=139, n=146)Change From BL to Week 3 (n=135, n=145)Change From BL to Final Week (n=143, n=148)
Placebo0.81-0.15-0.160.030.230.270.120.190.06-0.14-0.14-0.05-0.12-0.14-0.07-0.110.260.010.070.110.390.110.120.08-0.120.220.21
Pleconaril0.990.150.190.290.170.04-0.050.17-0.09-0.24-0.26-0.130.010.030.200.400.32-0.00-0.300.100.190.25-0.050.150.060.080.09

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LS Mean Change From Baseline in the Asthma Control Questionnaire (ACQ)

The ACQ is a validated instrument containing 7 questions to assess asthma control which incorporates symptoms, beta-agonist use, and spirometry. Participants recall their experiences during the previous 7 days and respond to each question using a 7-point scale. The items are equally weighted and the ACQ score is the mean of the 7 items and therefore ranges between 0 (well controlled) and 6 (extremely poorly controlled). The ACQ completed on the day of exposure was the Baseline ACQ. Pooled standard deviations (SDs) and least square (LS) means were calculated based on an analysis of variates (ANOVA) model. (NCT00394914)
Timeframe: Baseline through the Final Visit (Day 21)

,
Interventionunits on a scale (Least Squares Mean)
Baseline (n=126, n=127)Change From BL to Day 8 (n=120, n=124)Change From BL to Day 14 (n=94, n=96)Change From BL to Day 21 (n=89, n=96)Change From BL to Final Visit (n=126, n=127)
Placebo0.87-0.06-0.15-0.02-0.00
Pleconaril0.86-0.11-0.09-0.12-0.09

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LS Mean Change From Baseline in Total Asthma Symptom Score

Participants entered their asthma symptoms into an e-diary twice daily beginning at the Screening Visit through completion of the study. The total asthma symptom score was the sum of 3 scores for wheeze, cough, and dyspnea. Each symptom is scored as follows: 0 = none-sign/symptom is not present, 1 = mild-sign/symptom noticeable but did not bother me or interfere with my normal daily activities/sleep, 2 = moderate- sign/symptom annoying and may have interfered with my normal daily activities/sleep, or 3 = severe-symptom very uncomfortable and interfered with most or all of my normal daily activities/sleep. The total score ranges from 0 to 9, with increasing scores reflecting more severe asthma. Baseline values were defined as the average of the last seven assessments prior to randomization (before exposure to an index case). Pooled SDs and LS means were calculated based on an ANOVA model. (NCT00394914)
Timeframe: Baseline through the Final Visit (Day 21)

,
Interventionunits on a scale (Least Squares Mean)
Baseline (n=147, n=153)Change From BL to Day 1 (n=135, n=143)Change From BL to Day 2 (n=143, n=152)Change From BL to Day 3 (n=141, n=152)Change From BL to Day 4 (n=142, n=152)Change From BL to Day 5 (n=140, n=152)Change From BL to Day 6 (n=136, n=152)Change From BL to Day 7 (n=139, n=150)Change From BL to Day 8 (n=139, n=149)Change From BL to Day 9 (n=138, n=150)Change From BL to Day 10 (n=139, n=150)Change From BL to Day 11 (n=137, n=149)Change From BL to Day 12 (n=137, n=148)Change From BL to Day 13 (n=136, n=146)Change From BL to Day 14 (n=138, n=146)Change From BL to Day 15 (n=135, n=144)Change From BL to Day 16 (n=132, n=144)Change From BL to Day 17 (n=133, n=145)Change From BL to Day 18 (n=137, n=146)Change From BL to Day 19 (n=132, n=145)Change From BL to Day 20 (n=126, n=136)Change From BL to Day 21 (n=108, n=121)Change From BL to Final Day (n=147, n=153)
Placebo0.560.080.070.090.090.150.150.180.120.100.150.170.090.020.030.080.040.00-0.05-0.04-0.010.060.03
Pleconaril0.670.020.050.04-0.04-0.10-0.10-0.07-0.07-0.07-0.01-0.05-0.02-0.06-0.07-0.11-0.16-0.18-0.14-0.14-0.15-0.10-0.09

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LS Mean Change From Baseline in Total Cold Symptom Score

Participants entered their cold symptoms into an e-diary twice daily beginning at the Screening Visit through completion of the study. The total cold symptom score was the sum of 6 scores for rhinorrhea, nasal congestion, cough, score throat, malaise, and myalgia. Each symptom is scored as follows: 0 = none-sign/symptom is not present, 1 = mild-sign/symptom noticeable but did not bother me or interfere with my normal daily activities/sleep, 2 = moderate- sign/symptom annoying and may have interfered with my normal daily activities/sleep, or 3 = severe-symptom very uncomfortable and interfered with most or all of my normal daily activities/sleep. The total score ranges from 0 to 18, with increasing scores reflecting more severe colds. Baseline values were defined as the average of the last seven assessments prior to randomization (before exposure to an index case). Pooled SDs and LS means were calculated based on an ANOVA model. (NCT00394914)
Timeframe: Baseline through the Final Visit (Day 21)

,
Interventionunits on a scale (Least Squares Mean)
Baseline (n=147, n=153)Change From BL to Day 1 (n=135, n=143)Change From BL to Day 2 (n=143, n=152)Change From BL to Day 3 (n=141, n=152)Change From BL to Day 4 (n=142, n=152)Change From BL to Day 5 (n=140, n=152)Change From BL to Day 6 (n=136, n=152)Change From BL to Day 7 (n=139, n=150)Change From BL to Day 8 (n=139, n=149)Change From BL to Day 9 (n=138, n=150)Change From BL to Day 10 (n=139, n=150)Change From BL to Day 11 (n=137, n=149)Change From BL to Day 12 (n=137, n=148)Change From BL to Day 13 (n=136, n=146)Change From BL to Day 14 (n=138, n=146)Change From BL to Day 15 (n=135, n=144)Change From BL to Day 16 (n=132, n=144)Change From BL to Day 17 (n=133, n=145)Change From BL to Day 18 (n=137, n=146)Change From BL to Day 19 (n=132, n=145)Change From BL to Day 20 (n=126, n=136)Change From BL to Day 21 (n=108, n=121)Change From BL to Final Day (n=147, n=153)
Placebo0.990.120.260.350.390.450.400.380.340.290.290.310.250.110.150.180.210.10-0.03-0.040.170.290.23
Pleconaril1.090.030.210.310.140.04-0.010.030.020.040.180.170.07-0.020.050.040.04-0.06-0.17-0.03-0.040.150.18

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