Page last updated: 2024-12-05

proxymetacaine

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

Description

Proxymetacaine is a topical anesthetic that is commonly used in ophthalmic solutions for procedures such as eye surgery. Its synthesis involves the reaction of 2-amino-4-propylphenol with 2,6-dimethylbenzoic acid chloride. Proxymetacaine is known to have rapid onset of action and relatively short duration of effect. Its primary mechanism of action is blocking sodium channels in nerve membranes, thus preventing the transmission of pain signals. Its effectiveness and short duration make it ideal for ophthalmic procedures. Proxymetacaine is studied extensively for its potential to provide effective anesthesia during ophthalmic procedures while minimizing the risk of complications, particularly in patients with pre-existing conditions or allergies. '
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proxymetacaine: RN given refers to parent cpd; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID517321
CHEMBL ID1200464
SCHEMBL ID93880
MeSH IDM0047456
PubMed CID4935
CHEMBL ID1196
CHEBI ID8485
SCHEMBL ID23334
MeSH IDM0047456

Synonyms (162)

Synonym
AC-3399
smr000875264
MLS002154072
AKOS015844989
2-(diethylamino)ethyl 3-amino-4-propoxybenzoate monohydrochloride
ophthain
einecs 227-541-7
2-diethylaminoethyl 3-amino-4-propoxybenzoate hydrochloride
3-amino-4-propoxybenzoic acid 2-(diethylamino)ethyl ester hydrochloride
proparacaine hydrochloride
benzoic acid, 3-amino-4-propoxy-, 2-(diethylamino)ethyl ester, hydrochloride
proxymetacaine hydrochloride
benzoic acid, 3-amino-4-propoxy-, 2-(diethylamino)ethyl ester, monohydrochloride
chibro-heracaine
proxymetacaine monohydrochloride
proparacaine hcl
beta-(diethylamino)ethyl 3-amino-4-n-propoxybenzoate hydrochloride
keracaine
MLS001333067
MLS001333068
alcaine (tn)
proparacaine hydrochloride (usp)
D02098
5875-06-9
ophthetic (tn)
ak-taine
CHEMBL1200464
nsc-759896
HMS1570P20
A832009
2-(diethylamino)ethyl 3-amino-4-propoxy-benzoate hydrochloride;proparacaine hcl
benzoic acid, 3-amino-4-propoxy-, 2-(diethylamino)ethyl ester, monohydrochloride*benzoic acid, 3-amino-4-propoxy-, 2-(diethylamino)ethyl ester, monohydrochloride
dtxcid1028948
dtxsid0049022 ,
cas-5875-06-9
tox21_113547
nsc759896
pharmakon1600-01505688
unii-u96ol57goy
nsc 759896
u96ol57goy ,
proparacaine hydrochloride [usp]
2-(diethylamino)ethyl 3-amino-4-propoxybenzoate hydrochloride
proparacaine hydrochloride [usp monograph]
proparacaine hydrochloride [mi]
proparacaine hydrochloride [usp-rs]
proparacaine hydrochloride [green book]
proxymetacaine hydrochloride [who-dd]
proparacaine hydrochloride [orange book]
proparacaine hydrochloride [vandf]
proxymetacaine hydrochloride [mart.]
S1828
CCG-213513
proparacaine (hydrochloride)
HY-66012
SCHEMBL93880
NC00586
tox21_113547_1
NCGC00016991-05
proxymetacaine hydrochloride, proparacaine
KS-5058
P2156
benzoic acid,3-amino-4-propoxy-,2-(diethylamino)ethyl ester
mfcd00083467
proparacaine hydrochloride, united states pharmacopeia (usp) reference standard
BFUUJUGQJUTPAF-UHFFFAOYSA-N
SR-05000001759-3
C75748
proparacaine hydrochloride, analytical standard
2-(diethylamino)ethyl 3-amino-4-propoxybenzoate hcl
SW197338-3
benzoic acid, 3-amino-4-propoxy-, 2-(diethylamino)ethyl ester,monohydrochloride
2-diethylaminoethyl3-amino-4-propoxy-benzoatehydrochloride
proparacainehydrochloride
2-(diethylamino)ethyl 3-amino-4-propoxybenzoate;hydrochloride
proparacaine, hcl
Q27290947
proparacaine hydrochloride (usp-rs)
ophthaine solution
proparacaine hydrochloride (usp monograph)
proxymetacaine hydrochloride (mart.)
AC-13440
proximetacaina
unii-b4ob0jhi1x
proxymetacainum
b4ob0jhi1x ,
prossimetacaina
BRD-K79116891-003-03-7
proximetacaina [inn-spanish]
benzoic acid, 3-amino-4-propoxy-, 2-(diethylamino)ethyl ester
paracaine
proxymetacaine [inn:ban]
alcaine
prossimetacaina [dcit]
proximetacainum
2-(diethylamino)ethyl 3-amino-4-propoxybenzoate
kainair
3-amino-4-propoxybenzoic acid 2-(diethylamino)ethyl ester
einecs 207-884-9
brn 2745891
ophthetic
proxymetacainum [inn-latin]
beta-(diethylamino)ethyl 4-n-propoxybenzoate
ophthaine
NCGC00016991-01
cas-1452000
BSPBIO_000958
PRESTWICK2_000959
BPBIO1_001054
PRESTWICK3_000959
AB00444123
499-67-2
proparacaine
proxymetacaine
C07383
DB00807
PRESTWICK0_000959
PRESTWICK1_000959
SPBIO_003107
NCGC00016991-02
CHEMBL1196
chebi:8485 ,
D08448
proxymetacaine (inn)
FT-0658833
A24938
AKOS005457804
BBL003355
proxymethacaine
STK520616
NCGC00016991-03
FT-0674059
NCGC00016991-06
proxymetacaine [who-dd]
proxymetacaine [inn]
proparacaine [vandf]
proparacaine [mi]
gtpl7283
SCHEMBL23334
MLS006011856
3-amino-4-propoxy-benzoic acid 2-diethylamino-ethyl ester, hydrochloride
smr000857219
.beta.-(diethylamino)ethyl 4-n-propoxybenzoate
KCLANYCVBBTKTO-UHFFFAOYSA-N
HMS3604H05
AB00444123_07
AB00444123_08
DTXSID30198146 ,
J-017667
SBI-0206900.P001
MRF-0000607
BCP22476
Q600867
bdbm50225500
2,5-dibromopyridine-3-boronicacid
3-amino-4-propoxy-,2-(diethylamino)ethyl ester benzoic acid
NCGC00016991-13
dtxcid60120637
proxymetacainum (inn-latin)
proximetacaina (inn-spanish)
s01ha04
EN300-22731623

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"The penetration of sulforhodamine B (SRB) into the two corneas of a freshly killed mouse was measured after one eye was briefly exposed to a solution of a possibly toxic substance."( A permeability test for acute corneal toxicity.
Maurice, D; Singh, T, 1986
)
0.27
"A drug registry was established at Southern California College of Optometry (SCCO) to study use rates and incidence of adverse side effects of the nine pharmaceutical agents in the California optometry law."( Use of diagnostic pharmaceutical agents and incidence of adverse effects.
Applebaum, M; Jaanus, SD, 1983
)
0.27
" Synthetic local anesthetics such as tetracaine and proparacaine were developed which were more potent and less toxic than cocaine, but still produced corneal epithelium defects if used chronically."( Comparative toxicity of tetracaine, proparacaine and cocaine evaluated with primary cultures of rabbit corneal epithelial cells.
Acosta, D; Grant, RL, 1994
)
0.29
" Proparacaine was statistically more toxic than were the others."( Corneal endothelial toxicity of topical anesthesia.
Judge, AJ; Lee, DA; Miller, KM; Najafi, K, 1997
)
0.3
"Both tetracaine and proparacaine had toxic effects on stromal keratocytes related not only to drug concentrations but also to time exposure."( Toxicity of topical anesthetic agents to human keratocytes in vivo.
Kasetsuwan, N; LaBree, L; McDonnell, PJ; Moreira, LB; Sanchez, D; Shah, SS, 1999
)
0.3
" All six studies demonstrated that a short course of dilute topical anesthetic provided efficacious analgesia without adverse effects or delayed epithelial healing."( The Safety of Topical Anesthetics in the Treatment of Corneal Abrasions: A Review.
Milne, K; Otterness, K; Rezaie, S; Swaminathan, A, 2015
)
0.42
" The drug was found safe and devoid of any EC and EI potential."( Prediction of Ocular Toxicity of Potential Degradation Products of Proparacaine Hydrochloride Subjected under ICH Recommended Stress Conditions.
Coelho, A; Fernandes, A; Mahajan, A; Pissurlenkar, R; Tagalpallewar, A, 2023
)
0.91

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
" The greater bioavailability achieved by this vehicle allows much lower drug concentrations to be used, reducing the likelihood of systemic adverse reactions."( A comparison of the efficacy and duration of action of topically applied proxymetacaine using a novel ophthalmic delivery system versus eye drops in healthy young volunteers.
Barnard, NA; Burns, JM; Edgar, DF; Geraint, M; Gudgeon, AC; Lawrenson, JG, 1993
)
0.52
" Such host-guest complexes were investigated in view of their potential use as new therapeutic formulations, designed to increase the bioavailability and/or to decrease the systemic toxicity of proparacaine in anesthesia procedures."( Proparacaine complexation with beta-cyclodextrin and p-sulfonic acid calix[6]arene, as evaluated by varied (1)H-NMR approaches.
Arantes, LM; de Paula, E; Fernandes, SA; Marsaioli, AJ; Scarelli, C, 2009
)
0.35
"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

Dosage Studied

ExcerptRelevanceReference
" After rats were injected intrathecally with proxymetacaine, oxybuprocaine, bupivacaine, and lidocane, dose-response curves were constructed."( Intrathecal oxybuprocaine and proxymetacaine produced potent and long-lasting spinal anesthesia in rats.
Chen, YC; Chen, YW; Chu, CC; Hung, CH; Wang, JJ, 2009
)
0.9
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzoate esterEsters of benzoic acid or substituted benzoic acids.
[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]

Pathways (1)

PathwayProteinsCompounds
Proparacaine Action Pathway3111

Protein Targets (36)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency0.63100.044717.8581100.0000AID485294
acetylcholinesteraseHomo sapiens (human)Potency34.67130.002541.796015,848.9004AID1347398
glp-1 receptor, partialHomo sapiens (human)Potency19.95260.01846.806014.1254AID624417
GLS proteinHomo sapiens (human)Potency8.91250.35487.935539.8107AID624170
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency14.54170.001022.650876.6163AID1224838; AID1224893
cytochrome P450 2D6Homo sapiens (human)Potency6.16550.00108.379861.1304AID1645840
aryl hydrocarbon receptorHomo sapiens (human)Potency2.24750.000723.06741,258.9301AID743085; AID743122
chromobox protein homolog 1Homo sapiens (human)Potency89.12510.006026.168889.1251AID540317
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency31.67040.000323.4451159.6830AID743065; AID743067
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency33.48890.000627.21521,122.0200AID743202
DNA polymerase eta isoform 1Homo sapiens (human)Potency89.12510.100028.9256213.3130AID588591
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
DNA polymerase kappa isoform 1Homo sapiens (human)Potency100.00000.031622.3146100.0000AID588579
USP1 protein, partialHomo sapiens (human)Potency39.81070.031637.5844354.8130AID504865
GLS proteinHomo sapiens (human)Potency15.84890.35487.935539.8107AID624170
cytochrome P450 2D6Homo sapiens (human)Potency6.74120.00108.379861.1304AID1645840
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency6.30960.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency3.98110.00255.840031.6228AID899
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency1.25890.031610.279239.8107AID884; AID885
lethal factor (plasmid)Bacillus anthracis str. A2012Potency3.16230.020010.786931.6228AID912
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency1.25891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency1.25891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency1.25891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency1.25891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency1.25891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency1.25891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency1.25891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency1.25891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency1.25891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency1.25891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency1.25891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency1.25891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency1.25891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency1.25891.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency1.25891.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency1.25891.000012.224831.6228AID885
[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)
Amine oxidase [flavin-containing] AHomo sapiens (human)IC50 (µMol)1.77700.00002.37899.7700AID625150
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC50 (µMol)0.23800.00030.70285.3660AID625223
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.10000.00000.490110.0000AID625223
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (8)

Processvia Protein(s)Taxonomy
biogenic amine metabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
positive regulation of signal transductionAmine oxidase [flavin-containing] AHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
protein bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] AHomo sapiens (human)
cytosolAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (96)

Assay IDTitleYearJournalArticle
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
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.
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.
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.
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.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
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.
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.
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.
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.
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.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID450273Lipophilicity, log P of the compound2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Ligand-based design and synthesis of novel sodium channel blockers from a combined phenytoin-lidocaine pharmacophore.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID450269Displacement of [3H]-BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Ligand-based design and synthesis of novel sodium channel blockers from a combined phenytoin-lidocaine pharmacophore.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID205267Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (240)

TimeframeStudies, This Drug (%)All Drugs %
pre-199038 (15.83)18.7374
1990's57 (23.75)18.2507
2000's55 (22.92)29.6817
2010's67 (27.92)24.3611
2020's23 (9.58)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 40.05

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 Index40.05 (24.57)
Research Supply Index5.73 (2.92)
Research Growth Index4.68 (4.65)
Search Engine Demand Index68.16 (26.88)
Search Engine Supply Index2.26 (0.95)

This Compound (40.05)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials57 (22.71%)5.53%
Reviews0 (0.00%)6.00%
Reviews8 (3.19%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies23 (9.16%)4.05%
Observational0 (0.00%)0.25%
Observational1 (0.40%)0.25%
Other15 (100.00%)84.16%
Other162 (64.54%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (20)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Neurosensory Abnormalities in SymptomAtic Ocular Surface Patients (NASA) [NCT04838223]1,000 participants (Anticipated)Observational2021-07-02Enrolling by invitation
Does Proparacaine Enhance Strabismus Recovery [NCT03672435]140 participants (Actual)Observational [Patient Registry]2010-07-29Completed
VisuMax Femtosecond Laser Small Incision Lenticule Extraction for the Correction of High Myopia [NCT02528123]187 participants (Anticipated)Interventional2016-04-30Active, not recruiting
Challenging the Dogma: Topical Proparacaine is Safe and Effective for the Emergency Department Management of Acute Traumatic Corneal Injuries [NCT00620997]Phase 143 participants (Actual)Interventional2005-10-31Completed
Comparison of In-the-bag Stability Between Single-piece and Three-piece Intraocular Lens Via Scheimpflug Imaging System [NCT02609997]65 participants (Actual)Interventional2012-09-30Completed
A Randomized, Single-Masked, Active-Controlled, Parallel-Group Evaluation of Safety and the Local Anesthetic Effect of Articaine Sterile Topical Ophthalmic Solution (AG-920) in a Pediatric Population [NCT05325853]Phase 361 participants (Actual)Interventional2022-04-06Completed
Patient Assessment of Topical Anesthetic Effectiveness for Intravitreal Injections [NCT01027611]Phase 3120 participants (Actual)Interventional2009-10-31Completed
Does Administration of Proparacaine Hydrochloride 0.5% Ophthalmic Solution Prior to Canalicular Probing and Irrigation Decrease Patient Discomfort? [NCT05663684]Phase 4145 participants (Anticipated)Interventional2020-06-30Recruiting
Efficacy and Safety of Anesthetic Impregnated Bandage Soft Contact Lens (BSCL) in Pain Management After Photorefractive Keratectomy (PRK). [NCT04283331]Phase 430 participants (Anticipated)Interventional2020-06-01Recruiting
Laser Peripheral Iridotomy Plus Laser Peripheral Iridoplasty for Primary Angle Closure With Multi-mechanism Based on UBM: A Randomized Controlled Trial [NCT02613013]240 participants (Anticipated)Interventional2015-10-31Recruiting
Comparison Between Ropivacaine and Bupivacaine in Deep Topical Fornix Nerve Block Anesthesia in Patients Undergoing Cataract Surgery by Phacoemulsification. [NCT02925832]100 participants (Actual)Interventional2016-10-31Completed
Randomized Control Trial of the Effects of Proparacaine on the Pain Response to Mydriatic Eye Drops [NCT01266824]5 participants (Actual)Interventional2010-12-31Terminated(stopped due to Recruitment for the study has been terminated due to poor enrollment)
Topical Proparacaine Eye Drops to Improve the Experience of Patients Undergoing Intravitreal Injections [NCT02951351]36 participants (Actual)Interventional2016-10-12Completed
The Wearing-Off Period of Pharmacological Dilation: An Addendum to the Management of Anisocoria [NCT05238233]Phase 411 participants (Actual)Interventional2022-04-01Completed
Subfoveal Choroidal Thickness After Femtosecond Laser-assisted Cataract Surgery for Age-related Cataracts [NCT02895074]40 participants (Actual)Interventional2014-08-31Completed
Pilot Study: A Randomized Trial Of Anesthetic Agents For Intravitreal Injection [NCT00769392]28 participants (Actual)Interventional2008-09-30Completed
Does Administration of Proparacaine Hydrochloride 0.5% Ophthalmic Solution Prior to Canalicular Probing and Irrigation Decrease Patient Discomfort [NCT04229771]Phase 42 participants (Actual)Interventional2020-06-30Terminated(stopped due to slow enrollment)
Influence of Surgical Pleth Index-guided Analgesia Using Different Techniques on the Perioperative Outcomes in Patients Undergoing Vitreoretinal Surgery Under General Anaesthesia: Randomised, Controlled Trial [NCT02973581]176 participants (Actual)Interventional2016-02-29Completed
Topical Lidocaine Gel With and Without Subconjunctival Lidocaine Injection for Intravitreal Injection: a Within-patient Study [NCT01640171]57 participants (Actual)Interventional2012-07-31Completed
[NCT03049163]30 participants (Anticipated)Interventional2016-10-31Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00769392 (2) [back to overview]Discomfort Associated With the Intravitreal Injection
NCT00769392 (2) [back to overview]Discomfort From Anesthesia Used Prior to Intravitreal Injections
NCT01640171 (3) [back to overview]Likert Like Pain Scale Number of Participants Who Said the Topical Eye Hurt Much More Than the Subconjunctival Eye at Time of Intravitreal Injection
NCT01640171 (3) [back to overview]Number of Participants Who Preferred Subconjunctival Anesthetic at the Third Follow-up Visit
NCT01640171 (3) [back to overview]Number of Participatns With Level 10 Pain on Wong-Baker Pain Scale In Subconjunctival Eye At Time of Intravitreal Injection
NCT02951351 (8) [back to overview]Comfort With Intravitreal Injection Standard Procedure
NCT02951351 (8) [back to overview]Expectation Intravitreal Injection Will Have Negative Consequences on Subject Health
NCT02951351 (8) [back to overview]Expectation the Injection Will Contribute to Curing/Improving Eye Condition
NCT02951351 (8) [back to overview]Impression of Pre-injection Preparations
NCT02951351 (8) [back to overview]Number of Study Participants With Positive Conjunctival Culture
NCT02951351 (8) [back to overview]Overall Impression of Visit for Intravitreal Injection
NCT02951351 (8) [back to overview]Pain at the Time of Injection
NCT02951351 (8) [back to overview]Residual Pain From Intravitreal Injection
NCT04229771 (1) [back to overview]Count of Participants Who Report of Less Discomfort in the Eye That Received the Proparacaine Hydrochloride Anesthetic During Probing
NCT05238233 (1) [back to overview]Number of Participants With Constricting Response to Pilocarpine 1% in the Pharmacologically Dilated Eye
NCT05325853 (2) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT05325853 (2) [back to overview]The Proportion of Participants in Which an Eye Exam Was Able to be Performed

Discomfort Associated With the Intravitreal Injection

Discomfort Associated With the Intravitreal Injection using a Subjective Analog Pain Scale (0-10); no pain (0) and severe pain (10) (NCT00769392)
Timeframe: 16 weeks

Interventionunits on a scale (Mean)
Lidocaine 4%Lidocaine 2% Injectable SolutionProparacaine OphthalmicTetracaine Ophthalmic
All Participants32.32.83.1

[back to top]

Discomfort From Anesthesia Used Prior to Intravitreal Injections

Discomfort from Anesthesia used prior to Intravitreal Injections using a Subjective Analog Pain Scale (0-10); no pain (0) and severe pain (10). (NCT00769392)
Timeframe: 16 weeks

Interventionunits on a scale (Mean)
Lidocaine 4%Lidocaine 2% Injectable SolutionProparacaine OphthalmicTetracaine Ophthalmic
All Participants1.41.60.71.0

[back to top]

Likert Like Pain Scale Number of Participants Who Said the Topical Eye Hurt Much More Than the Subconjunctival Eye at Time of Intravitreal Injection

The patient was asked to compare the two eyes in the way described in the study protocol on a five point scale. If one eye hurt a lot more or a little more than the other or if the two eyes were equal (neither hurt more than the other). (NCT01640171)
Timeframe: 24 hours

Interventionparticipants (Number)
Topical Anesthesia 1 Eye, SC 1 Eye19

[back to top]

Number of Participants Who Preferred Subconjunctival Anesthetic at the Third Follow-up Visit

Participants received anesthetic over several treatment visits. They were allowed to change there preference at each visit. The final outcome was the preference indicated at the third follow-up visit. (NCT01640171)
Timeframe: up to 6 months

Interventionparticipants (Number)
Topical Anesthesia 1 Eye, SC 1 Eye50

[back to top]

Number of Participatns With Level 10 Pain on Wong-Baker Pain Scale In Subconjunctival Eye At Time of Intravitreal Injection

Pain was rated on a 10 point standardized pain scale, zero was the least pain and 10 was the worst pain. The patient was questioned using a script and shown a pain scale as well as told how the pain scale worked. Then the patient gave the number that characterized their pain. (NCT01640171)
Timeframe: 24 hours

Interventionparticipants (Number)
Topical Anesthesia 1 Eye, SC 1 Eye0

[back to top]

Comfort With Intravitreal Injection Standard Procedure

Subjects were asked to complete a survey about their experience with intravitreal injections after the procedure was completed. The survey was scored on a 0 to 10 numeric rating scale (NRS) where 0 was a positive response and 10 was a negative response. The lower the score, the more comfortable the subject was with the procedure, the higher the score, the less comfortable the subject was with the procedure. (NCT02951351)
Timeframe: post-injection

Interventionscore on a scale (Median)
Standard Procedure + Culture0
Proparacaine + Culture0

[back to top]

Expectation Intravitreal Injection Will Have Negative Consequences on Subject Health

Subjects were asked to complete a survey about their experience with intravitreal injections after the procedure was completed. The survey was scored on a 0 to 10 numeric rating scale (NRS) where 0 was a positive response and 10 was a negative response. A lower score indicated subjects did not expect the injection would negatively affect their overall health. Higher scores indicated subjects expected the injection would negatively affect their overall health. (NCT02951351)
Timeframe: post-injection

Interventionscore on a scale (Median)
Standard Procedure + Culture0
Proparacaine + Culture0

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Expectation the Injection Will Contribute to Curing/Improving Eye Condition

Patients were asked to rate their expectation on the extent to which the intravitreal injections would contribute to curing or improving their eye condition. The question was scored on a 0 to 10 numeric rating scale (NRS) where 0 was a negative response (not at all) and 10 was a positive response (to a large extent). A low score indicated the subject did not expect the injection would contribute to curing or improving the eye condition while a high score indicated the subject did expect the injection will help to cure or improve the eye condition. (NCT02951351)
Timeframe: post-injection

Interventionscore on a scale (Median)
Standard Procedure + Culture8
Proparacaine + Culture10

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Impression of Pre-injection Preparations

Subjects were asked to complete a survey about their experience with intravitreal injections after the procedure was completed. The survey consisted of 6 questions and was scored on a 0 to 10 numeric rating scale (NRS) where 0 was a positive response and 10 was a negative response. The lower the score, the more positive impression of the preparation process, the higher the score, the less positive impression of the preparation process.. (NCT02951351)
Timeframe: post-injection

Interventionscore on a scale (Median)
Standard Procedure + Culture0
Proparacaine + Culture0

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Number of Study Participants With Positive Conjunctival Culture

Conjunctival samples were collected after participants received either an additional drop of proparacaine or povidone iodine. Bacterial cultures were performed from conjunctival samples by the Mayo Clinic Microbiology laboratory. Bacterial species identification was performed on any and all bacteria that grew. (NCT02951351)
Timeframe: pre-injection

InterventionParticipants (Count of Participants)
Standard Procedure + Culture1
Proparacaine + Culture1

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Overall Impression of Visit for Intravitreal Injection

Subjects were asked to complete a survey about their experience with intravitreal injections after the procedure was completed. The survey was scored on a 0 to 10 numeric rating scale (NRS) where 0 was a positive response and 10 was a negative response. The lower the score, the more positive impression of the visit, the higher the score, the less positive impression of the visit. (NCT02951351)
Timeframe: post-injection

Interventionscore on a scale (Median)
Standard Procedure + Culture0
Proparacaine + Culture0

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Pain at the Time of Injection

Subjects were asked to complete a survey about their experience with intravitreal injections after the procedure was completed. The survey was scored on a 0 to 10 numeric rating scale (NRS) where 0 was a positive response and 10 was a negative response. The lower the score, the lesser the perceived pain, the higher the score, the higher the perceived pain. (NCT02951351)
Timeframe: post-injection

Interventionscore on a scale (Median)
Standard Procedure + Culture2
Proparacaine + Culture1

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Residual Pain From Intravitreal Injection

Subjects were asked to complete a survey about their experience with intravitreal injections after the procedure was completed. The survey was scored on a 0 to 10 numeric rating scale (NRS) where 0 was a positive response and 10 was a negative response. The lower the score, the lesser the residual pain, the higher the score, the higher the residual pain. (NCT02951351)
Timeframe: post-injection

Interventionscore on a scale (Median)
Standard Procedure + Culture1
Proparacaine + Culture0

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Count of Participants Who Report of Less Discomfort in the Eye That Received the Proparacaine Hydrochloride Anesthetic During Probing

Participants completed a survey which asked which procedure was more uncomfortable (left or right). Assignment to receive proparacaine hydrochloride was compared to survey results. When the participant reported less discomfort in the eye that received the proparacaine hydrochloride medication, this is is reported as concordance between reduction of pain/discomfort and anesthetic use. (NCT04229771)
Timeframe: 1 minute

InterventionParticipants (Count of Participants)
Participants Who Received Proparacaine Hydrochloride Solution in Left Eye and Placebo in Right Eye1
Participants Who Received Proparacaine Hydrochloride Solution in Right Eye and Placebo in Left Eye0

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Number of Participants With Constricting Response to Pilocarpine 1% in the Pharmacologically Dilated Eye

Measurement of pupil diameter (NCT05238233)
Timeframe: 4 hours

InterventionParticipants (Count of Participants)
Eye Dilation and Constriction3

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Number of Participants With Treatment Emergent Adverse Events (TEAEs)

TEAEs will be summarized by treatment group using frequency and percent for each system, organ, class (SOC) and preferred term within each SOC. Summaries will be presented separately for ocular and non-ocular Adverse Events (AEs). (NCT05325853)
Timeframe: From randomization through study completion (up to 4 days following treatment)

InterventionParticipants (Count of Participants)
AG-9200
Proparacaine0

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The Proportion of Participants in Which an Eye Exam Was Able to be Performed

Was the investigator was able to perform the eye examination without additional anesthesia (NCT05325853)
Timeframe: Two to four minutes following treatment (last drop) of IMP

InterventionParticipants (Count of Participants)
AG-92030
Proparacaine30

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