Page last updated: 2024-12-04

aceclidine

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

Description

aceclidine: was heading 1975-94; use QUINUCLIDINES to search ACECLIDINE 1975-94; cholinomimetic used to reduce intraocular pressure in glaucoma [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID1979
CHEMBL ID20835
CHEBI ID93847
SCHEMBL ID121393
MeSH IDM0224858
PubMed CID10031478
CHEMBL ID487297
SCHEMBL ID14665337
MeSH IDM0224858

Synonyms (108)

Synonym
aceclidina [inn-spanish]
3-quinuclidinol acetate
einecs 212-574-1
1-azabicyclo(2.2.2)octan-3-ol, acetate
glaucostat
aceclidinum [inn-latin]
aceclidine [usan:inn]
1-azabicyclo(2.2.2)octan-3-ol, acetate (ester)
3-quinuclidinol acetate (ester)
al 304
aceclidina
unii-0578k3elio
0578k3elio ,
aceclidinum
nsc 657843
acetic acid 1-aza-bicyclo[2.2.2]oct-3-yl ester
aceclidine,s(+)
acetic acid 1-aza-bicyclo[2.2.2]oct-3-yl ester(aceclidine)
bdbm50034625
aceclidine,r(-)
BRD-A32673558-003-02-1
DIVK1C_000180
KBIO1_000180
NCI60_020173
NCI60_020184
3-acetoxyquinuclidine
nsc657843
nsc-657843
glaucostat (tn)
827-61-2
D02750
aceclidine (usan/inn)
quinuclidin-3-yl acetate
1-azabicyclo[2.2.2]octan-3-ol, acetate (ester)
3-quinuclidinol, acetate (ester)
aceclidine
SPECTRUM_001338
SPECTRUM5_001301
IDI1_000180
BSPBIO_002911
NCGC00024733-02
KBIO2_006954
KBIOSS_001818
KBIOGR_000742
KBIO2_001818
KBIO2_004386
KBIO3_002411
SPBIO_001110
SPECTRUM3_001446
SPECTRUM4_000421
SPECTRUM2_001235
NINDS_000180
NCGC00024733-03
L023942
nsc-758239
CHEMBL20835 ,
3-quinuclidinol dl-form acetate (ester)
1-azabicyclo[2.2.2]octan-3-yl acetate
A840430
NCGC00024733-04
HMS3264B20
AKOS006281409
nsc758239
pharmakon1600-01501124
cas-827-61-2
tox21_110921
dtxsid2045658 ,
dtxcid0025658
FT-0607358
BRD-A80567352-003-01-6
aceclidine [who-dd]
aceclidine [usan]
aceclidine [inn]
aceclidine [mart.]
3-quinuclidinol dl-form acetate (ester) [mi]
CCG-212926
CS-B0278
SCHEMBL121393
(+) 3-acetoxy quinuclidine
(rs) 3-acetoxy quinuclidine
(rs)-3-acetoxyquinuclidine
1-azabicyclo[2.2.2]oct-3-yl acetate
STL430459
3-quinuclidinol, acetate
1-azabicyclo[2.2.2]oct-3-yl acetate #
1-azabicyclo[2.2.2]octan-3-ol, acetate
3-quinuclidinyl acetate
acetic acid quinuclidin-3-yl ester
AB00053601_02
AB00053601_03
mfcd00468105
CHEBI:93847
acetic acid 1-azabicyclo[2.2.2]octan-3-yl ester
quinuclidin-3-ylacetate
DS-5025
SY111901
DB13262
Q2362603
BRD-A32673558-001-01-7
EN300-3463436
HY-32067
[(1s)-1-[(6-aminopurin-9-yl)methyl]-2-hydroxy-ethoxy]methyl-(2-octadecoxyethoxy)phosphinic acid
ode-hpmpa
1-octadecyloxyethyl-(s)-hpmpa
ode-(s)-hpmpa
CHEMBL487297
SCHEMBL14665337
[(2s)-1-(6-aminopurin-9-yl)-3-hydroxypropan-2-yl]oxymethyl-(2-octadecoxyethoxy)phosphinic acid

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" However, the ether lipid esters of (S)-HPMPA, hexadecyloxypropyl-[(S)-HPMPA] [HDP-(S)-HPMPA] and octadecyloxyethyl-[(S)-HPMPA] [ODE-(S)-HPMPA], had significantly enhanced activity in vitro and are orally bioavailable in mice."( Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
Beadle, JR; Collins, DJ; Herrod, BP; Hostetler, KY; Keith, KA; Kern, ER; Quenelle, DC; Trahan, J, 2007
)
0.34
" HDP-(S)-HPMPA is orally bioavailable and provides excellent liver exposure to the drug."( Alkoxyalkyl esters of 9-(s)-(3-hydroxy-2-phosphonomethoxypropyl) adenine are potent and selective inhibitors of hepatitis B virus (HBV) replication in vitro and in HBV transgenic mice in vivo.
Beadle, JR; Hostetler, KY; Korba, BE; Morrey, JD; Wyles, DL, 2009
)
0.35

Dosage Studied

ExcerptRelevanceReference
" Oxotremorine generated dose-response curves that were similar in both the circular and longitudinal vectors and intermediate to those previously reported for carbachol and aceclidine."( The effect of muscarinic agonists and selective receptor subtype antagonists on the contractile response of the isolated rhesus monkey ciliary muscle.
Gabelt, BT; Kaufman, PL; Poyer, JF, 1994
)
0.48
" Dose-response curves for steady-state pupil size and for behavioral phase shifts were constructed for 3 pupil conditions (dilated, constricted, and control)."( Photic sensitivity ranges of hamster pupillary and circadian phase responses do not overlap.
Cooper, HM; Hut, RA; Oklejewicz, M; Rieux, C, 2008
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
quinuclidines
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
regulator of G-protein signaling 4Homo sapiens (human)Potency0.04230.531815.435837.6858AID504845
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency3.61250.005612.367736.1254AID624032
[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)
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC50 (µMol)0.51000.00052.773925.1700AID104017
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki8.26000.00010.579710.0000AID142348
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC50 (µMol)0.51000.00052.891925.1700AID104017
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki8.26000.00011.48339.1400AID142348
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC50 (µMol)0.51000.00052.747825.1700AID104017
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Ki8.26000.00010.68688.2600AID142348
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC50 (µMol)0.51000.00052.780225.1700AID104017
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Ki8.26000.00010.66618.2600AID142348
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC50 (µMol)0.51000.00053.314249.5000AID104017
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki8.26000.00010.58908.2600AID142348
Muscarinic acetylcholine receptor DM1Drosophila melanogaster (fruit fly)Ki122.00000.00051.42495.2000AID1090601; AID1090602
[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)
Muscarinic acetylcholine receptor M1Homo sapiens (human)EC50 (µMol)4.46600.00161.304310.0000AID141971
Muscarinic acetylcholine receptor M3Mus musculus (house mouse)EC50 (µMol)10.00009.90009.950010.0000AID141597
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (19)

Processvia Protein(s)Taxonomy
positive regulation of monoatomic ion transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
neuromuscular synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M1Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M1Homo sapiens (human)
cognitionMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of postsynaptic membrane potentialMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of glial cell proliferationMuscarinic acetylcholine receptor M1Homo sapiens (human)
positive regulation of intracellular protein transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M1Homo sapiens (human)
Schaffer collateral - CA1 synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic density membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M1Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Mus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (108)

Assay IDTitleYearJournalArticle
AID141452Binding affinity for muscarinic acetylcholine receptor M1 using [3H]oxotremorine-M (Oxo-M) radioligand in rat hippocampus membranes1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists.
AID175669Effective concentration of compound that can stimulate phosphoinositol metabolism in rat hippocampus1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists.
AID1090601Displacement of [3H]QNB from Drosophila melanogaster mAChR by scintillation counting2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID142348Binding affinity against muscarinic acetylcholine receptor from rat brain crude membrane, using [3H]-NMS (N-Methylscopolamine) as the radioligand.1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
In vitro muscarinic activity of spiromuscarones and related analogs.
AID197273Maximum stimulation of phosphatidyl inositol in rat hippocampal tissue, activity is expressed as percent of carbachol response1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
In vitro muscarinic activity of spiromuscarones and related analogs.
AID1090595Toxicity to Musca domestica (house fly) assessed as mortality at 25 ug/fly measured after 2.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID180116Inhibition of the response (stimulation of phosphoinositol metabolism in rat hippocampus) to 10 uM of compound by AF-DX 1161993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists.
AID180118Inhibition of the response (stimulation of phosphoinositol metabolism in rat hippocampus) to 10 uM of compound by pirenzepine1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists.
AID104017Inhibition of [3H]-(R)-QNB binding to muscarinic receptors of rat brain membranes.1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists.
AID141978Maximum stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the muscarinic acetylcholine receptor M1 at 100 uM1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists.
AID230727Ratio of the Ki (NMS) value to that of Ki (Oxo-M).1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
In vitro muscarinic activity of spiromuscarones and related analogs.
AID1090593Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured after 0.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID180117Inhibition of the response (stimulation of phosphoinositol metabolism in rat hippocampus) to 10 uM of compound by p-F-hexahydrosiladifenidol1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists.
AID1090597Toxicity to Musca domestica (house fly) assessed as mortality at 25 ug/fly measured after 1 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID141971Effective concentration required for stimulation of phosphoinositol (PI) hydrolysis in the A9 L cell line transfected with the Muscarinic acetylcholine receptor M1.1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists.
AID1090589Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured after 24 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID119570Compound at an intraperitoneal dose of 10 mg/Kg was tested for salivation in mice expressed as score; 2=Marked salivation or tremor1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists.
AID1090591Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured after 1.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID142488Inhibition of specific [3H](R)-QNB binding to Muscarinic acetylcholine receptor in rat brain membranes1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
Synthesis and biological characterization of 1,4,5,6-tetrahydropyrimidine and 2-amino-3,4,5,6-tetrahydropyridine derivatives as selective m1 agonists.
AID1090592Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured after 1 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID142349Binding affinity against muscarinic acetylcholine receptor from rat brain crude membrane, using [3H]OXO-M (oxotremorine) as the radioligand.1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
In vitro muscarinic activity of spiromuscarones and related analogs.
AID141451Binding affinity for muscarinic acetylcholine receptor M1 using [3H]pirenzepine (Pz) radioligand in rat hippocampus membranes.1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists.
AID1090594Toxicity to Musca domestica (house fly) assessed as mortality at 25 ug/fly measured after 24 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID1090598Toxicity to Musca domestica (house fly) assessed as mortality at 25 ug/fly measured after 0.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID1090590Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured after 2.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID186265Ability to stimulate phosphoinisitol metabolism was examined in the rat hippocampus1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists.
AID189455Ability to stimulate phosphoinositol metabolism was examined in the rat cerebral cortex at 100 uM1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists.
AID141597Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
Synthesis and biological characterization of 1,4,5,6-tetrahydropyrimidine and 2-amino-3,4,5,6-tetrahydropyridine derivatives as selective m1 agonists.
AID141602Maximum stimulation at Muscarinic acetylcholine receptor M3 expressed in A9 L cells1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
Synthesis and biological characterization of 1,4,5,6-tetrahydropyrimidine and 2-amino-3,4,5,6-tetrahydropyridine derivatives as selective m1 agonists.
AID1090602Displacement of [3H]AF-DX 384 from Drosophila melanogaster mAChR by scintillation counting2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID196226Tested for agonist activity through assays of phosphoinositide (PI) metabolism in slices from rat cerebral cortex1997Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8
Synthesis and biological characterization of 1,4,5,6-tetrahydropyrimidine and 2-amino-3,4,5,6-tetrahydropyridine derivatives as selective m1 agonists.
AID1090596Toxicity to Musca domestica (house fly) assessed as mortality at 25 ug/fly measured after 1.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
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.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID373253Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mean death day at 3 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373442Antiviral activity against Vaccinia virus WR in HFF cells assessed as reduction of viral replication after 3 days2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373246Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as log reduction of viral titer per gram of liver at 30 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373415Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mortality at 10 mg/kg, po treated for 5 days after 48 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373416Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mortality at 30 mg/kg, po treated for 5 days after 48 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373441Antiviral activity against Cowpox virus Brighton in HFF cells assessed as reduction of viral replication after 3 days2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373403Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mean death day at 10 mg/kg, po treated for 5 days after 72 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID556388Cytotoxicity against human Huh7.5 cells administered for 3 days measured 24 hrs after last dose by neutral red dye uptake assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
The octadecyloxyethyl ester of (S)-9-[3-hydroxy-2-(phosphonomethoxy) propyl]adenine is a potent and selective inhibitor of hepatitis C virus replication in genotype 1A, 1B, and 2A replicons.
AID560900Antiviral activity against HBV infected in human HepG2(2.2.15) cells assessed as decrease in extracellular viral DNA level after 24 hrs by blot hybridization assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Alkoxyalkyl esters of 9-(s)-(3-hydroxy-2-phosphonomethoxypropyl) adenine are potent and selective inhibitors of hepatitis B virus (HBV) replication in vitro and in HBV transgenic mice in vivo.
AID556387Antiviral activity against HCV2A SGR-JFH-1 infected in human Huh7.5 cells assessed as decrease in intracellular viral RNA treated for 3 days measured 24 hrs after last dose by luciferase reporter gene-based blot hybridization2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
The octadecyloxyethyl ester of (S)-9-[3-hydroxy-2-(phosphonomethoxy) propyl]adenine is a potent and selective inhibitor of hepatitis C virus replication in genotype 1A, 1B, and 2A replicons.
AID556390Selectivity index, ratio of CC50 for human Huh7.5 cells to EC50 for HCV genotype 2A SGR-JFH-1 infected in human Huh7.5 cells2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
The octadecyloxyethyl ester of (S)-9-[3-hydroxy-2-(phosphonomethoxy) propyl]adenine is a potent and selective inhibitor of hepatitis C virus replication in genotype 1A, 1B, and 2A replicons.
AID373243Toxicity in Vaccinia virus WR infected BALB/c mouse assessed as survival at 30 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373407Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mean death day at 30 mg/kg, po treated for 5 days after 48 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373255Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mean death day at 30 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373447Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as log reduction of viral titer per gram of liver at 30 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373409Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mean death day at 30 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID563683Antischistosomal activity against Schistosoma mansoni isolated from infected Syrian golden hamsters assessed as worm mortality at 25 uM treated for overnight followed by drug washout measured on day 5 relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Antischistosomal activity of hexadecyloxypropyl cyclic 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]adenine and other alkoxyalkyl esters of acyclic nucleoside phosphonates assessed by schistosome worm killing in vitro.
AID373444Selectivity index, ratio of CC50 for HFF cells to EC50 for Vaccinia virus Copenhagen2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID556386Antiviral activity against HCV1B BM4-5 infected in human Huh7.5 cells assessed as decrease in intracellular viral RNA treated for 3 days measured 24 hrs after last dose by luciferase reporter gene-based blot hybridization2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
The octadecyloxyethyl ester of (S)-9-[3-hydroxy-2-(phosphonomethoxy) propyl]adenine is a potent and selective inhibitor of hepatitis C virus replication in genotype 1A, 1B, and 2A replicons.
AID373405Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mean death day at 3 mg/kg, po treated for 5 days after 48 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373254Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mean death day at 10 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID520605Cytotoxicity against human WI38 cells by neutral red assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Anti-BK virus activity of nucleoside analogs.
AID373443Antiviral activity against Vaccinia virus Copenhagen in HFF cells assessed as reduction of viral replication after 3 days2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373248Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mean death day at 10 mg/kg, po treated for 5 days after 72 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373448Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as log reduction of viral titer per gram of spleen at 30 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID563685Antischistosomal activity against Schistosoma mansoni isolated from infected Syrian golden hamsters assessed as worm mortality at 5 uM treated for overnight followed by drug washout measured on day 52009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Antischistosomal activity of hexadecyloxypropyl cyclic 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]adenine and other alkoxyalkyl esters of acyclic nucleoside phosphonates assessed by schistosome worm killing in vitro.
AID373450Toxicity in Cowpox virus Brighton infected BALB/c mouse assessed as survival at 30 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID560901Cytotoxicity against human HepG2(2.2.15) cells after 24 hrs by neutral red assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Alkoxyalkyl esters of 9-(s)-(3-hydroxy-2-phosphonomethoxypropyl) adenine are potent and selective inhibitors of hepatitis B virus (HBV) replication in vitro and in HBV transgenic mice in vivo.
AID373445Cytotoxicity against HFF cells after 7 days2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID560964Antiviral activity against HBV infected in transgenic mouse assessed as decrease in liver viral DNA level at 4 mg/kg, po administered daily for 14 days measured post last dose2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Alkoxyalkyl esters of 9-(s)-(3-hydroxy-2-phosphonomethoxypropyl) adenine are potent and selective inhibitors of hepatitis B virus (HBV) replication in vitro and in HBV transgenic mice in vivo.
AID373439Selectivity index, ratio of CC50 for HFF cells to EC50 for Cowpox virus Brighton2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID563684Antischistosomal activity against Schistosoma mansoni isolated from infected Syrian golden hamsters assessed as worm mortality at 12.5 uM treated for overnight followed by drug washout measured on day 5 relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Antischistosomal activity of hexadecyloxypropyl cyclic 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]adenine and other alkoxyalkyl esters of acyclic nucleoside phosphonates assessed by schistosome worm killing in vitro.
AID373258Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mortality at 30 mg/kg, po treated for 5 days after 72 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373250Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mean death day at 3 mg/kg, po treated for 5 days after 48 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373245Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as log reduction of viral titer per gram of spleen at 30 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373419Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mortality at 10 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373402Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mean death day at 3 mg/kg, po treated for 5 days after 72 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373406Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mean death day at 10 mg/kg, po treated for 5 days after 48 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373393Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mortality at 30 mg/kg, po treated for 5 days after 48 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373408Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mean death day at 3 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID520606Selectivity index, ratio of CC50 for human WI38 cells to EC50 for BK polyomavirus ATCC VR8372008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Anti-BK virus activity of nucleoside analogs.
AID373244Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as log reduction of viral titer per gram of kidney at 30 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373414Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mortality at 3 mg/kg, po treated for 5 days after 48 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373411Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mortality at 10 mg/kg, po treated for 5 days after 72 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID563681Antischistosomal activity against Schistosoma mansoni isolated from infected Syrian golden hamsters assessed as worm mortality at 75 uM treated for overnight followed by drug washout measured on day 5 relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Antischistosomal activity of hexadecyloxypropyl cyclic 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]adenine and other alkoxyalkyl esters of acyclic nucleoside phosphonates assessed by schistosome worm killing in vitro.
AID563686Antischistosomal activity against Schistosoma mansoni isolated from infected Syrian golden hamsters assessed as worm mortality treated for overnight followed by drug washout measured on day 52009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Antischistosomal activity of hexadecyloxypropyl cyclic 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]adenine and other alkoxyalkyl esters of acyclic nucleoside phosphonates assessed by schistosome worm killing in vitro.
AID373261Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mortality at 10 mg/kg, po treated for 5 days after 48 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373397Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mortality at 30 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID563682Antischistosomal activity against Schistosoma mansoni isolated from infected Syrian golden hamsters assessed as worm mortality at 50 uM treated for overnight followed by drug washout measured on day 5 relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Antischistosomal activity of hexadecyloxypropyl cyclic 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]adenine and other alkoxyalkyl esters of acyclic nucleoside phosphonates assessed by schistosome worm killing in vitro.
AID563680Antischistosomal activity against Schistosoma mansoni isolated from infected Syrian golden hamsters assessed as worm mortality at 100 uM treated for overnight followed by drug washout measured on day 5 relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Antischistosomal activity of hexadecyloxypropyl cyclic 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]adenine and other alkoxyalkyl esters of acyclic nucleoside phosphonates assessed by schistosome worm killing in vitro.
AID520604Antimicrobial activity against BK polyomavirus ATCC VR837 infected in human WI38 cells assessed as reduction in viral titer after 7 days by PCR analysis2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Anti-BK virus activity of nucleoside analogs.
AID373395Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mortality at 3 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373251Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mean death day at 10 mg/kg, po treated for 5 days after 48 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID556389Selectivity index, ratio of CC50 for human Huh7.5 cells to EC50 for HCV genotype 1B BM4-5 infected in human Huh7.5 cells2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
The octadecyloxyethyl ester of (S)-9-[3-hydroxy-2-(phosphonomethoxy) propyl]adenine is a potent and selective inhibitor of hepatitis C virus replication in genotype 1A, 1B, and 2A replicons.
AID373252Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mean death day at 30 mg/kg, po treated for 5 days after 48 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID560902Selectivity index, ratio of CC50 for human HepG2(2.2.15) cells to EC50 for HBV infected in human HepG2(2.2.15) cells2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Alkoxyalkyl esters of 9-(s)-(3-hydroxy-2-phosphonomethoxypropyl) adenine are potent and selective inhibitors of hepatitis B virus (HBV) replication in vitro and in HBV transgenic mice in vivo.
AID373451Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as reduction of virus titer in lung at 30 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373260Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mortality at 3 mg/kg, po treated for 5 days after 48 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373257Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mortality at 10 mg/kg, po treated for 5 days after 72 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373449Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as log reduction of viral titer per gram of kidney at 30 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373412Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mortality at 30 mg/kg, po treated for 5 days after 72 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373452Toxicity in BALB/c mouse at 30 mg/kg, po2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373256Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mortality at 3 mg/kg, po treated for 5 days after 72 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373420Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mortality at 30 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373247Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mean death day at 3 mg/kg, po treated for 5 days after 72 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373404Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mean death day at 30 mg/kg, po treated for 5 days after 72 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373418Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mortality at 3 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373440Selectivity index, ratio of CC50 for HFF cells to EC50 for Vaccinia virus WR2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373396Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mortality at 10 mg/kg, po treated for 5 days after 24 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373249Antiviral activity against Cowpox virus Brighton infected BALB/c mouse assessed as mean death day at 30 mg/kg, po treated for 5 days after 72 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
AID373410Antiviral activity against Vaccinia virus WR infected BALB/c mouse assessed as mortality at 3 mg/kg, po treated for 5 days after 72 hrs of viral inoculation2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Effect of oral treatment with hexadecyloxypropyl-[(S)-9-(3-hydroxy-2- phosphonylmethoxypropyl)adenine] [(S)-HPMPA] or octadecyloxyethyl-(S)-HPMPA on cowpox or vaccinia virus infections in mice.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (34)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (2.94)18.7374
1990's13 (38.24)18.2507
2000's15 (44.12)29.6817
2010's4 (11.76)24.3611
2020's1 (2.94)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 38.40

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 Index38.40 (24.57)
Research Supply Index3.53 (2.92)
Research Growth Index5.67 (4.65)
Search Engine Demand Index51.48 (26.88)
Search Engine Supply Index2.06 (0.95)

This Compound (38.40)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (3.13%)5.53%
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other31 (96.88%)84.16%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (8)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Single-Center, Double-Masked Evaluation of the Efficacy and Safety of PRX-100 in the Treatment of Early to Moderate Presbyopia [NCT03201562]Phase 258 participants (Actual)Interventional2017-04-30Completed
A Multicenter, Double-Masked Evaluation of the Safety and Effectiveness of Aceclidine + Brimonidine (LNZ101) and Aceclidine (LNZ100) in the Treatment of Presbyopia [NCT05431543]Phase 258 participants (Actual)Interventional2022-08-06Completed
Safety Study: A Multi-Center, Double-Masked Phase 3 Safety Study Evaluation of the Long-Term Safety of LNZ101 in Presbyopic Subjects [NCT05753189]Phase 3361 participants (Actual)Interventional2023-02-21Active, not recruiting
A Multi-Center, Double-Masked Phase 3 Evaluation of the Safety and Efficacy of LNZ101 for the Treatment of Presbyopia [NCT05656027]Phase 3469 participants (Actual)Interventional2022-12-19Active, not recruiting
A Prospective, Single-Center, Open-Label, Study of the Plasma Pharmacokinetics and Safety Following Topical Administration of LNZ101 and LNZ100 Ophthalmic Solutions in Healthy Adult Subjects With Presbyopia [NCT05936489]Phase 130 participants (Actual)Interventional2023-07-06Completed
A Multi-Center, Double-Masked Phase 3 Evaluation of the Safety and Efficacy of LNZ101 for the Treatment of Presbyopia [NCT05728944]Phase 3229 participants (Actual)Interventional2023-04-24Active, not recruiting
A Multi-Center, Randomized, Double-Masked, Placebo-Controlled Phase 3 Evaluation of the Efficacy and Safety of LNZ101 and LNZ100 for the Treatment of Presbyopia [NCT06045299]Phase 3300 participants (Anticipated)Interventional2023-09-27Recruiting
A Multicenter, Double-Masked Evaluation of the Safety and Effectiveness of Aceclidine /Brimonidine (LNZ101) and Aceclidine (LNZ100) in the Treatment of Presbyopia [NCT05294328]Phase 262 participants (Actual)Interventional2022-05-05Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT03201562 (1) [back to overview]Proportion of Subjects With at Least a 3 Line (15 Letter) Improvement in Near Visual Acuity in the Study Eye

Proportion of Subjects With at Least a 3 Line (15 Letter) Improvement in Near Visual Acuity in the Study Eye

Proportion of subjects with at least a 3 line (15 letter) improvement in near visual acuity in the study eye at 1 hour post-treatment in the mITT population (NCT03201562)
Timeframe: 1 hour post-treatment

Interventionpercentage of participants (Number)
Aceclidine+Tropicamide Combination47.22
Aceclidine47.22
Vehicle2.38

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