Page last updated: 2024-12-05

pralidoxime chloride

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

Cross-References

ID SourceID
PubMed CID135445761
CHEBI ID8355
SCHEMBL ID61419
SCHEMBL ID1650343
MeSH IDM0317913

Synonyms (113)

Synonym
MLS001076535
MLS000028727 ,
smr000059189
2-[(e)-(hydroxyimino)methyl]-1-methylpyridinium chloride
1-methyl-2-formylpyridinium chloride oxime
pyridinium, 2-formyl-1-methyl-, chloride, oxime
2-(hydroxyiminomethyl)-1-methylpyridinium chloride
2-pyridine-aldoxime chloride
einecs 200-080-9
pralidoxime chloride [usan]
n-metylpyridinium-2-aldoxime chloride
nsc 164614
cas-51-15-0
NCGC00016226-01
CHEBI:8355 ,
pyridinium, 2-((hydroxyimino)methyl)-1-methyl-, chloride
combopen
protopam
1-methyl-2-pyridinium aldoxime chloride
1-methyl-2-aldoximinopyridinium chloride
51-15-0
pyridine-2-aldoxime methochloride
2-pyridine aldoxime methyl chloride
pyridinium, chloride, oxime
2-formyl-1-methylpyridinium chloride oxime
nsc-164614
n-methylpyridinium-2-aldoxime chloride
pralidoxine chloride
wln: t6kj a1 b1unq &g
pyridinium aldoxime methochloride
n-methylpyridinium chloride 2-aldoxime
2-hydroxyiminomethyl-1-methylpyridinium chloride
n-methylpyridine-2-aldoxime chloride
protopam chloride
pralidoxime chloride
2-formyl-n-methylpyridinium oxime chloride
2-pam chloride
2-pyridinealdoxime methochloride
pam 2cl
pralidoxime (inn)
D00469
protopam (tn)
pralidoxime chloride (usp)
pyridine-2-aldoxime methachloride
MLS002222315
AKOS001094374
HMS1570N08
HMS2097N08
HMS3259I04
A828463
(1-methyl-2-pyridylidene)methyl-oxo-ammonium chloride;pralidoxime chloride
nsc759147
pharmakon1600-01505449
nsc-759147
tox21_110316
dtxsid1023495 ,
dtxcid803495
2-[(1e)-(hydroxyimino)methyl]-1-methylpyridin-1-ium chloride
S4575
MLS003876809
pralidoxime chloride [usan:usp]
pralidoxime chloride [vandf]
duodote component pralidoxime chloride
pralidoxime chloride [orange book]
38X7XS076H ,
2-formyl-l-methylpyridinium chloride oxime
pralidoxime chloride [mart.]
atnaa component pralidoxime chloride
pralidoxime chloride component of atnaa
pralidoxime chloride [green book]
pralidoxime chloride [who-dd]
pralidoxime chloride [usp monograph]
pralidoxime chloride [mi]
14018-50-9
pralidoxime chloride [usp-rs]
pyridinium, 2-((hydroxyimino)methyl)-1-methyl-, chloride (e)-
pralidoxime chloride component of duodote
CCG-220943
SCHEMBL61419
NCGC00178286-05
tox21_110316_1
SCHEMBL1650343
CS-4828
pralidoximchlorid
2-pyridinealdoximemethochloride
Q-201609
HY-B1200
pralidoxime (chloride)
OPERA_ID_228
2-pam (chloride)
mfcd00011981
pyridinium, 2-[(hydroxyimino)methyl]-1-methyl-, chloride (1:1)
pralidoxime chloride, united states pharmacopeia (usp) reference standard
unii-38x7xs076h
HMS3714N08
2-((hydroxyimino)methyl)-1-methylpyridin-1-ium chloride
AS-13850
pralidoxime chloride [usp]
pralidoxime chloride [usan:who-dd]
pyridinium, 2-formyl-1-methyl-, oxime (8ci)
(ne)-n-[(1-methylpyridin-1-ium-2-yl)methylidene]hydroxylamine;chloride
EN300-260536
2-[(hydroxyimino)methyl]-1-methylpyridin-1-ium chloride
BP164283
CS-0369417
(e)-2-((hydroxyimino)methyl)-1-methylpyridin-1-ium chloride
Z57931208
pralidoxime chloride (usp monograph)
2-((e)-(hydroxyimino)methyl)-1-methylpyridinium chloride
pralidoxime chloride (mart.)
pralidoxime chloride (usp-rs)
pralidoxime chloride (autoinjector)
pralidoxime chloride (usan:usp)

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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
cholinesterase reactivatorA drug used to reverse the inactivation of cholinesterase caused by organophosphates or sulfonates.
cholinergic drugAny drug used for its actions on cholinergic systems. Included here are agonists and antagonists, drugs that affect the life cycle of acetylcholine, and drugs that affect the survival of cholinergic neurons.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
pyridinium salt
organic chloride salt
[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 (24)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency0.07940.003245.467312,589.2998AID2517
USP1 protein, partialHomo sapiens (human)Potency79.43280.031637.5844354.8130AID743255
GLS proteinHomo sapiens (human)Potency11.22020.35487.935539.8107AID624170
chromobox protein homolog 1Homo sapiens (human)Potency100.00000.006026.168889.1251AID540317
importin subunit beta-1 isoform 1Homo sapiens (human)Potency0.11585.804836.130665.1308AID540253
snurportin-1Homo sapiens (human)Potency0.11585.804836.130665.1308AID540253
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency0.11585.804816.996225.9290AID540253
gemininHomo sapiens (human)Potency0.70790.004611.374133.4983AID624297
[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)
AcetylcholinesteraseElectrophorus electricus (electric eel)IC50 (µMol)292.50000.00000.94539.9400AID30838; AID30847
AcetylcholinesteraseElectrophorus electricus (electric eel)Ki126.50000.00121.25638.9000AID30840
Neuronal acetylcholine receptor subunit alpha-4Mus musculus (house mouse)IC50 (µMol)1,200.00000.00000.57992.6000AID145513
AcetylcholinesteraseHomo sapiens (human)IC50 (µMol)784.85710.00000.933210.0000AID1140219; AID1311977; AID1732658; AID31028; AID31032; AID31034; AID31166
Acetylcholinesterase Bos taurus (cattle)IC50 (µMol)346.00000.00000.61068.7000AID30683
Choline O-acetyltransferase Rattus norvegicus (Norway rat)IC50 (µMol)184.70000.00530.00530.0053AID30242
Neuronal acetylcholine receptor subunit alpha-7Mus musculus (house mouse)IC50 (µMol)1,200.00000.00400.00400.0040AID145513
Neuronal acetylcholine receptor subunit alpha-5Mus musculus (house mouse)IC50 (µMol)1,200.00000.00400.00400.0040AID145513
Neuronal acetylcholine receptor subunit beta-3Mus musculus (house mouse)IC50 (µMol)1,200.00000.00400.00400.0040AID145513
Neuronal acetylcholine receptor subunit beta-4Mus musculus (house mouse)IC50 (µMol)1,200.00000.00400.60201.2000AID145513
Neuronal acetylcholine receptor subunit alpha-3Mus musculus (house mouse)IC50 (µMol)1,200.00000.00400.00400.0040AID145513
Neuronal acetylcholine receptor subunit alpha-2Mus musculus (house mouse)IC50 (µMol)1,200.00000.00400.00400.0040AID145513
Neuronal acetylcholine receptor subunit beta-2Mus musculus (house mouse)IC50 (µMol)1,200.00000.00400.60201.2000AID145513
Neuronal acetylcholine receptor subunit alpha-6Mus musculus (house mouse)IC50 (µMol)1,200.00000.00400.08170.3110AID145513
TransporterRattus norvegicus (Norway rat)IC50 (µMol)1,200.00000.00081.95628.8000AID145513
[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)
AcetylcholinesteraseHomo sapiens (human)Kd362.63270.00801.77505.3000AID1127118; AID1140212; AID1140213; AID1237001; AID1237002; AID1237003; AID1311971; AID1311972; AID1471800; AID1471803; AID1471806; AID1471809; AID710208; AID710209; AID710210
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AcetylcholinesteraseHomo sapiens (human)Kdiss5.00005.00005.00005.0000AID1859575
AcetylcholinesteraseRattus norvegicus (Norway rat)KR575.00003.00004.50006.0000AID302661
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (25)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processCholinesteraseHomo sapiens (human)
learningCholinesteraseHomo sapiens (human)
negative regulation of cell population proliferationCholinesteraseHomo sapiens (human)
neuroblast differentiationCholinesteraseHomo sapiens (human)
peptide hormone processingCholinesteraseHomo sapiens (human)
response to alkaloidCholinesteraseHomo sapiens (human)
cocaine metabolic processCholinesteraseHomo sapiens (human)
negative regulation of synaptic transmissionCholinesteraseHomo sapiens (human)
response to glucocorticoidCholinesteraseHomo sapiens (human)
response to folic acidCholinesteraseHomo sapiens (human)
choline metabolic processCholinesteraseHomo sapiens (human)
acetylcholine catabolic processCholinesteraseHomo sapiens (human)
acetylcholine catabolic process in synaptic cleftAcetylcholinesteraseHomo sapiens (human)
regulation of receptor recyclingAcetylcholinesteraseHomo sapiens (human)
osteoblast developmentAcetylcholinesteraseHomo sapiens (human)
acetylcholine catabolic processAcetylcholinesteraseHomo sapiens (human)
cell adhesionAcetylcholinesteraseHomo sapiens (human)
nervous system developmentAcetylcholinesteraseHomo sapiens (human)
synapse assemblyAcetylcholinesteraseHomo sapiens (human)
receptor internalizationAcetylcholinesteraseHomo sapiens (human)
negative regulation of synaptic transmission, cholinergicAcetylcholinesteraseHomo sapiens (human)
amyloid precursor protein metabolic processAcetylcholinesteraseHomo sapiens (human)
positive regulation of protein secretionAcetylcholinesteraseHomo sapiens (human)
retina development in camera-type eyeAcetylcholinesteraseHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholinesteraseHomo sapiens (human)
positive regulation of cold-induced thermogenesisAcetylcholinesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
amyloid-beta bindingCholinesteraseHomo sapiens (human)
catalytic activityCholinesteraseHomo sapiens (human)
acetylcholinesterase activityCholinesteraseHomo sapiens (human)
cholinesterase activityCholinesteraseHomo sapiens (human)
protein bindingCholinesteraseHomo sapiens (human)
hydrolase activity, acting on ester bondsCholinesteraseHomo sapiens (human)
enzyme bindingCholinesteraseHomo sapiens (human)
choline bindingCholinesteraseHomo sapiens (human)
identical protein bindingCholinesteraseHomo sapiens (human)
amyloid-beta bindingAcetylcholinesteraseHomo sapiens (human)
acetylcholinesterase activityAcetylcholinesteraseHomo sapiens (human)
cholinesterase activityAcetylcholinesteraseHomo sapiens (human)
protein bindingAcetylcholinesteraseHomo sapiens (human)
collagen bindingAcetylcholinesteraseHomo sapiens (human)
hydrolase activityAcetylcholinesteraseHomo sapiens (human)
serine hydrolase activityAcetylcholinesteraseHomo sapiens (human)
acetylcholine bindingAcetylcholinesteraseHomo sapiens (human)
protein homodimerization activityAcetylcholinesteraseHomo sapiens (human)
laminin bindingAcetylcholinesteraseHomo sapiens (human)
amyloid-beta bindingAcetylcholinesterase Bos taurus (cattle)
protein bindingAcetylcholinesterase Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Processvia Protein(s)Taxonomy
extracellular regionCholinesteraseHomo sapiens (human)
nuclear envelope lumenCholinesteraseHomo sapiens (human)
endoplasmic reticulum lumenCholinesteraseHomo sapiens (human)
blood microparticleCholinesteraseHomo sapiens (human)
plasma membraneCholinesteraseHomo sapiens (human)
extracellular spaceCholinesteraseHomo sapiens (human)
extracellular regionAcetylcholinesteraseHomo sapiens (human)
basement membraneAcetylcholinesteraseHomo sapiens (human)
extracellular spaceAcetylcholinesteraseHomo sapiens (human)
nucleusAcetylcholinesteraseHomo sapiens (human)
Golgi apparatusAcetylcholinesteraseHomo sapiens (human)
plasma membraneAcetylcholinesteraseHomo sapiens (human)
cell surfaceAcetylcholinesteraseHomo sapiens (human)
membraneAcetylcholinesteraseHomo sapiens (human)
neuromuscular junctionAcetylcholinesteraseHomo sapiens (human)
synaptic cleftAcetylcholinesteraseHomo sapiens (human)
synapseAcetylcholinesteraseHomo sapiens (human)
perinuclear region of cytoplasmAcetylcholinesteraseHomo sapiens (human)
side of membraneAcetylcholinesteraseHomo sapiens (human)
synapseAcetylcholinesterase Bos taurus (cattle)
side of membraneAcetylcholinesterase Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (338)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
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.
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.
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.
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.
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.
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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation 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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation 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.
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.
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.
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.
AID135980Number of surviving mice was calculated after the administration of 25 mg/kg compound and 11.2 mg/kg of atropine sulfate and 25 mg/kg (1/4LD50) of 2-PAMCl1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 3. Synthesis and evaluation of (alkenyloxy)-, (alkynyloxy)-, and (aralkyloxy)methyl quaternarized 2-[(hydroxyimino)methyl]-1-alkylimidazolium halides as reactivators and therapy for soman intoxication
AID1144160Drug level in beagle dog whole blood at 5 mg/kg, iv measured after 5 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1471800Reactivation of sarin inhibited human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID117072LD50 value was determined intramuscularly in mouse1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 5. Structure-activity relationships for side-chain nitro-, sulfone-, amino-, and aminosulfonyl-substituted analogues for therapy against anticholinesterase intoxication.
AID1471806Reactivation of tabun inhibited human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID302658Reactivation activity of tabun-inhibited AChE in rat brain at 100 uM after 30 mins2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Design of a potent reactivator of tabun-inhibited acetylcholinesterase--synthesis and evaluation of (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203).
AID120775antidotal activity was measured against tabun in mice and activity expressed as the no. of survivors noted at 24 hr out of population of 10 mice each exposed intramuscularly at the dose 1/4 of 2LD50 of the compound1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 4. Effect of various side-chain substituents on therapeutic activity against anticholinesterase intoxication.
AID710210Binding affinity to VX-human AChE complex2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase.
AID1140216Acidic dissociation constant, pKa of the compound in phosphate/tris/glycine-NaOH containing buffer by UV-vis spectrophotometric analysis2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE).
AID1471798Reactivation of tabun inhibited human erythrocyte AChE assessed as residual activity at 10 to 1000 uM using acetylthiocholine iodide as substrate preincubated for 2 to 120 mins followed by substrate addition measured for 3 mins by Ellman's method2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID1859583Reactivation of VX induced inhibition of BChE in human plasma assessed as dissociation constant using ATCh as substrate incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID17238K2, The intrinsic biomolecular reactivation rate constant on VX at 25 degree Centigrade1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Sulfur derivatives of 2-oxopropanal oxime as reactivators of organophosphate-inhibited acetylcholinesterase in vitro: synthesis and structure-reactivity relationships.
AID118131Antidotal activity measured in mice exposed to soman; activity expressed as the no. of survivors at 24 hr out of population of 10 mice exposed intramuscularly at a dose 1/16 of 2LD50 of the compound1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 5. Structure-activity relationships for side-chain nitro-, sulfone-, amino-, and aminosulfonyl-substituted analogues for therapy against anticholinesterase intoxication.
AID276247Reactivation of paraoxon inhibited AChE from rat brain at 1 mM2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase.
AID263589Reactivation of AChE inhibited by 1 ug TEPP in mouse brain2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Quaternary salts of 4,3' and 4,4' bis-pyridinium monooximes. Part 2: synthesis and biological activity.
AID14124Distribution of rat erythrocytes for tube 1 on rate of aging in 2 mL of cell suspension; Minus (-)1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Synthesis of some quaternary ammonium alkylating agents and their effects on soman-inhibited acetylcholinesterase.
AID1144169Drug excretion in po dosed beagle dog urine1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1127128Ratio of maximal reactivation rate constant to Kd for methylphosphonothioate VX-inhibited recombinant human AChE measured up to 10 mins by Ellman's method2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and biological evaluation of novel tetrahydroacridine pyridine- aldoxime and -amidoxime hybrids as efficient uncharged reactivators of nerve agent-inhibited human acetylcholinesterase.
AID17239K2, The intrinsic biomolecular reactivation rate constant on paraxon at 25 degree Centigrade1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Sulfur derivatives of 2-oxopropanal oxime as reactivators of organophosphate-inhibited acetylcholinesterase in vitro: synthesis and structure-reactivity relationships.
AID1127117Reactivation of methylphosphonothioate VX-inhibited recombinant human AChE assessed as maximal reactivation rate constant measured up to 10 mins by Ellman's method2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and biological evaluation of novel tetrahydroacridine pyridine- aldoxime and -amidoxime hybrids as efficient uncharged reactivators of nerve agent-inhibited human acetylcholinesterase.
AID1144158Drug level in beagle dog whole blood treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 300 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1471801Reactivation of sarin inhibited human erythrocyte AChE assessed as overall bimolecular reactivation rate constant using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID30838Inhibition of eel acetylcholinesterase (AChE) activity by 50% 1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID1859571Reactivation of VX induced inhibition of recombinant human AChE assessed as maximal first-order reactivation rate constant using ATCh as substrate at 100 uM incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1865763Reactivation of CPS-inhibited human recombinant AChE assessed as reactivation rate constant using ATC as substrate at 1 mM followed by substrate addition by Ellman's method based spectrophotometry2021RSC medicinal chemistry, Sep-23, Volume: 12, Issue:9
Dual acting oximes designed for therapeutic decontamination of reactive organophosphates
AID118253Antidotal activity was measured against tabun in mice, activity expressed as the no. of survivors noted at 24 hr out of population of 10 mice each exposed intramuscularly at the dose 1/4 of 2LD50 of the compound1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 5. Structure-activity relationships for side-chain nitro-, sulfone-, amino-, and aminosulfonyl-substituted analogues for therapy against anticholinesterase intoxication.
AID1859567Reactivation of sarin induced inhibition of recombinant human AChE assessed as time needed to achieve maximal reactivation using ATCh as substrate at 100 uM incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1144146Plasma concentration in beagle dog treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 60 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1859586Reactivation of cyclosarin induced inhibition of BChE in human plasma assessed as second-order rate constant using ATCh as substrate incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1859575Reactivation of tabun induced inhibition of recombinant human AChE assessed as maximal achieved reactivation using ATCh as substrate at 100 uM incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1859605Neuroprotective activity against sarin-induced CD-1 mouse assessed as protective agent at 26.4 mg/kg, IM after 24 hrs2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID136848Compound was tested for protection of mice against ethyl p-nitrophenyl methylphosphonate (EPMP) at 5000 ug/kg plus 20 mg/kg atropine sulfate of 25 mg/Kg (1/4 LD50); 1/71989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID1471824Dissociation constant, pKa of the compound in pH 4 to 13 aqueous buffer at 20 mM by 1H NMR analysis2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID615411Reactivation of diisopropyl phosphorofluoridate-inhibited electric eel AChE activity after 40 mins by Ellman's method relative to control2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE).
AID1859600Reactivation of tabun induced inhibition of BChE in human plasma assessed as time needed to achieve maximal reactivation using ATCh as substrate at 1 mM incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1471813Toxicity in Wistar rat assessed as lethality at 32 umol/kg, iv2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID392540Reactivation of paraoxon-inhibited bovine red blood cellular AChE at 5 mM after 1 hr2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
Reactivation potency of fluorinated pyridinium oximes for acetylcholinesterases inhibited by paraoxon organophosphorus agent.
AID30840Compound was tested for the competitive inhibition of phosphorylation of Eel acetylcholinesterase (AChE)1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID1732659Reactivation of paraoxon-inhibited human AChE assessed as increase in enzyme activity at 100 uM incubated for 30 mins by Ellman's method relative to control2021European journal of medicinal chemistry, Apr-05, Volume: 215Molecular modeling-guided optimization of acetylcholinesterase reactivators: A proof for reactivation of covalently inhibited targets.
AID17670Keff is the effective biomolecular rate constant on sarin for reactivation at pH 7.8 at 25 degree Centigrade1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Sulfur derivatives of 2-oxopropanal oxime as reactivators of organophosphate-inhibited acetylcholinesterase in vitro: synthesis and structure-reactivity relationships.
AID184635LD50 expresses the acute toxicity measured after 24 hr in rats1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Sulfur derivatives of 2-oxopropanal oxime as reactivators of organophosphate-inhibited acetylcholinesterase in vitro: synthesis and structure-reactivity relationships.
AID710206Reactivation of paraoxon-inhibited human AChE assessed as reactivation rate constant2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase.
AID31643Effective rate constant for reactivation of AchE in human erythrocytes1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 3. Synthesis and evaluation of (alkenyloxy)-, (alkynyloxy)-, and (aralkyloxy)methyl quaternarized 2-[(hydroxyimino)methyl]-1-alkylimidazolium halides as reactivators and therapy for soman intoxication
AID17668Keff is the effective biomolecular rate constant on VX for reactivation at pH 7.8 at 25 degree Centigrade1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Sulfur derivatives of 2-oxopropanal oxime as reactivators of organophosphate-inhibited acetylcholinesterase in vitro: synthesis and structure-reactivity relationships.
AID1732655Reactivation of VX-inhibited human AChE assessed as increase in enzyme activity at 100 uM incubated for 30 mins by Ellman's method relative to control2021European journal of medicinal chemistry, Apr-05, Volume: 215Molecular modeling-guided optimization of acetylcholinesterase reactivators: A proof for reactivation of covalently inhibited targets.
AID1144192Reactivation of AChE in ICR mouse brain at 50 mg/kg, iv administered 15 mins post DFP challenge measured after 90 mins by Ellman method relative to control1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 3. Delivery of N-methylpyridinium-2-carbaldoxime chloride through the blood-brain barrier in its dihydropyridine pro-drug form.
AID120776antidotal activity was measured against tabun in mice and activity expressed as the no. of survivors noted at 24 hr out of population of 10 mice each exposed intramuscularly at the dose 1/64 of 2LD50 of the compound1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 4. Effect of various side-chain substituents on therapeutic activity against anticholinesterase intoxication.
AID276248Reactivation of paraoxon inhibited AChE from rat brain at 0.1 uM2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase.
AID710211Reactivation of VX-inhibited human AChE assessed as reactivation rate constant2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase.
AID1471804Reactivation of cyclosarin inhibited human erythrocyte AChE assessed as overall bimolecular reactivation rate constant using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's me2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID1144154Drug level in beagle dog whole blood treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 60 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1144174Drug excretion in po dosed beagle dog urine by radiochromatography1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1859569Reactivation of cyclosarin induced inhibition of recombinant human AChE assessed as maximal achieved reactivation using ATCh as substrate at 100 uM incubated for 30 mins by Ellman's method relative to control2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1859580Reactivation of tabun induced inhibition of BChE in human plasma assessed as first-order reactivation rate constant using ATCh as substrate incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1859589Reactivation of sarin induced inhibition of BChE in human plasma assessed as maximal first-order reactivation rate constant using ATCh as substrate at 1 mM incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1732657Reactivation of tabun-inhibited human AChE assessed as increase in enzyme activity at 100 uM incubated for 30 mins by Ellman's method relative to control2021European journal of medicinal chemistry, Apr-05, Volume: 215Molecular modeling-guided optimization of acetylcholinesterase reactivators: A proof for reactivation of covalently inhibited targets.
AID1140213Binding affinity to VX-inhibited hemoglobin free human erythrocyte ghost acetylcholinesterase using acetylthiocholineiodide as substrate measured up to 1 hr by Ellman method2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE).
AID1311974Reactivation of VX-inhibited hemoglobin free erythrocyte ghost human AChE assessed as rate constant for cleavage of P-O bond of VX-AChE conjugate using acetylcholine iodide as substrate measured for 1 hr by spectrophotometry based Ellman method2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE).
AID307194Reactivation of 1000 uM paraoxon-induced inhibition of AChE in rat brain at pH 7.6 after 10 mins2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Novel series of bispyridinium compounds bearing a (Z)-but-2-ene linker--synthesis and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase.
AID17669Keff is the effective biomolecular rate constant on paraxon for reactivation at pH 7.8 at 25 degree Centigrade1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Sulfur derivatives of 2-oxopropanal oxime as reactivators of organophosphate-inhibited acetylcholinesterase in vitro: synthesis and structure-reactivity relationships.
AID1144135Plasma concentration in beagle dog at 5 mg/kg, iv measured after 10 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1144144Plasma concentration in beagle dog treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 30 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1529747Inhibition of electric eel AChE assessed as remaining enzyme activity at 1 uM using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured every 3 mins for 15 mins relative to control2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
Novel tacrine-pyridinium hybrid reactivators of organophosphorus-inhibited acetylcholinesterase: Synthesis, molecular docking, and in vitro reactivation study.
AID117071LD50 value determined intramuscularly in mouse1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 4. Effect of various side-chain substituents on therapeutic activity against anticholinesterase intoxication.
AID302659Reactivation activity of tabun-inhibited AChE in rat brain at 10 uM after 30 mins2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Design of a potent reactivator of tabun-inhibited acetylcholinesterase--synthesis and evaluation of (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203).
AID135977Number of surviving mice was calculated after the administration of 11.2 mg/kg of atropine sulfate, 1/16 LD50 of drug with 2-PAMCl used as base line1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 3. Synthesis and evaluation of (alkenyloxy)-, (alkynyloxy)-, and (aralkyloxy)methyl quaternarized 2-[(hydroxyimino)methyl]-1-alkylimidazolium halides as reactivators and therapy for soman intoxication
AID615406Reactivation of diisopropyl phosphorofluoridate-inhibited electric eel AChE activity at 0.001 M and pH 8 after 10 mins by Ellman's method relative to control2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE).
AID1732660Reactivation of parathion-inhibited human AChE assessed as increase in enzyme activity at 100 uM incubated for 30 mins by Ellman's method relative to control2021European journal of medicinal chemistry, Apr-05, Volume: 215Molecular modeling-guided optimization of acetylcholinesterase reactivators: A proof for reactivation of covalently inhibited targets.
AID352066Reactivation of sarin-inhibited electric eel AChE at 10 uM after 10 mins by Ellman's method relative to control2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
In-vitro regeneration of sarin inhibited electric eel acetylcholinesterase by bis-pyridinium oximes bearing xylene linker.
AID1237007Reactivation of sarin-inhibited human acetylcholinesterase assessed as second order rate constant incubated for 60 mins using ATChI substrate by DTNB dye based UV-visible spectrophotometry2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and in vitro kinetic evaluation of N-thiazolylacetamido monoquaternary pyridinium oximes as reactivators of sarin, O-ethylsarin and VX inhibited human acetylcholinesterase (hAChE).
AID351913Reactivation of diisopropyl phosphorofluoridate-induced electric eel AChE inhibition at 1 mM by Ellman's method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and evaluation of novel bis-pyridinium oximes as reactivators of DFP-inhibited acetylcholinesterase.
AID301219Reactivation of 1 mM tabun-inhibited rat brain AchE2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
Monooxime reactivators of acetylcholinesterase with (E)-but-2-ene linker: preparation and reactivation of tabun- and paraoxon-inhibited acetylcholinesterase.
AID1859572Reactivation of VX induced inhibition of recombinant human AChE assessed as maximal achieved reactivation using ATCh as substrate at 100 uM incubated for 30 mins by Ellman's method relative to control2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1144151Drug level in beagle dog whole blood treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 15 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1144172Drug excretion in po dosed beagle dog urine treated with [14C]-labelled N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride by radiochromatography1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1859585Reactivation of sarin induced inhibition of BChE in human plasma assessed as second-order rate constant using ATCh as substrate incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID30834Effective rate constant for AChE reactivation1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID1144143Plasma concentration in beagle dog treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 15 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID364611Reactivation of 1000 uM tabun inhibited AChE in rat brain homogenate2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Monoquaternary pyridinium salts with modified side chain-synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase.
AID615410Reactivation of sarin-inhibited electric eel AChE activity after 40 mins by Ellman's method relative to control2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE).
AID1859593Reactivation of sarin induced inhibition of BChE in human plasma assessed as maximal achieved reactivation using ATCh as substrate at 1 mM incubated for 30 mins by Ellman's method relative to control2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID89258Concentration of the HOX that inhibits 50% of AChE (Acetylcholinesterase) activity1984Journal of medicinal chemistry, Nov, Volume: 27, Issue:11
Structure-activity relationships for reactivators of organophosphorus-inhibited acetylcholinesterase: quaternary salts of 2-[(hydroxyimino)methyl]imidazole.
AID1144183Ratio of drug level in whole blood to plasma in beagle dog treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 45 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1144156Drug level in beagle dog whole blood treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 180 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID302660Toxicity in intramuscular dosed rat after 24 hrs2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Design of a potent reactivator of tabun-inhibited acetylcholinesterase--synthesis and evaluation of (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203).
AID1144155Drug level in beagle dog whole blood treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 120 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1237005Reactivation of O-ethylsarin-inhibited human acetylcholinesterase assessed as reactivity rate constant incubated for 60 mins using ATChI substrate by DTNB dye based UV-visible spectrophotometry2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and in vitro kinetic evaluation of N-thiazolylacetamido monoquaternary pyridinium oximes as reactivators of sarin, O-ethylsarin and VX inhibited human acetylcholinesterase (hAChE).
AID30830Maximal displacement of GD from acetylcholinesterase (AChE) of bovine erythrocytes1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID32123In vitro dissociation constant of rat brain Acetylcholinesterase (AChE)-reactivator complex was determined2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis of a new reactivator of tabun-inhibited acetylcholinesterase.
AID1859577Reactivation of sarin induced inhibition of BChE in human plasma assessed as first-order reactivation rate constant using ATCh as substrate incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1144147Plasma concentration in beagle dog treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 180 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID352067Reactivation of sarin-inhibited electric eel AChE at 100 uM after 10 mins by Ellman's method relative to control2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
In-vitro regeneration of sarin inhibited electric eel acetylcholinesterase by bis-pyridinium oximes bearing xylene linker.
AID276245Reactivation of tabun inhibited AChE from rat brain at 1 mM2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase.
AID1859533Drug metabolism in PBS at pH 7.4 assessed as oxamate formation2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID30841Percentage of maximum reactivation of GD-inhibited AChE activity in eel1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID1140218Reactivation of VX-inhibited hemoglobin free human erythrocyte ghost acetylcholinesterase using acetylthiocholineiodide as substrate assessed as second order rate constant measured up to 1 hr by Ellman method2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE).
AID1144137Plasma concentration in beagle dog at 5 mg/kg, iv measured after 30 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1237006Reactivation of VX-inhibited human acetylcholinesterase assessed as reactivity rate constant incubated for 60 mins using ATChI substrate by DTNB dye based UV-visible spectrophotometry2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and in vitro kinetic evaluation of N-thiazolylacetamido monoquaternary pyridinium oximes as reactivators of sarin, O-ethylsarin and VX inhibited human acetylcholinesterase (hAChE).
AID1859573Reactivation of VX induced inhibition of recombinant human AChE assessed as time needed to achieve maximal reactivation using ATCh as substrate at 100 uM incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1859565Reactivation of sarin induced inhibition of recombinant human AChE assessed as maximal first-order reactivation rate constant using ATCh as substrate at 100 uM incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1859596Reactivation of tabun induced inhibition of BChE in human plasma assessed as maximal achieved reactivation using ATCh as substrate at 1 mM incubated for 30 mins by Ellman's method relative to control2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID451160Reactivation of organophosphate-inhibited house fly AChE activity at 5 mM by Ellman's method2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Fluorinated pyridinium oximes as potential reactivators for acetylcholinesterases inhibited by paraoxon organophosphorus agent.
AID307193Reactivation of 10 uM tabun-induced inhibition of AChE in rat brain at pH 7.6 after 10 mins2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Novel series of bispyridinium compounds bearing a (Z)-but-2-ene linker--synthesis and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase.
AID1144180Ratio of drug level in whole blood to plasma in beagle dog treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 10 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1471814Toxicity in Wistar rat assessed as sensitivity to light at 16 umol/kg, iv2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID120774antidotal activity was measured against tabun in mice and activity expressed as the no. of survivors noted at 24 h out of population of 10 mice each exposed intramuscularly at the dose 1/16 of 2LD50 of the compound1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 4. Effect of various side-chain substituents on therapeutic activity against anticholinesterase intoxication.
AID1144138Plasma concentration in beagle dog at 5 mg/kg, iv measured after 45 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID31166In vitro concentration of compound required for reversibly inhibiting 50% of human anticholinesterase activity1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 4. Effect of various side-chain substituents on therapeutic activity against anticholinesterase intoxication.
AID118132antidotal activity measured in mice exposed to soman; activity expressed as the no. of survivors at 24 hr out of population of 10 mice exposed intramuscularly at the dose 1/4 of 2LD50 of the compound1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 5. Structure-activity relationships for side-chain nitro-, sulfone-, amino-, and aminosulfonyl-substituted analogues for therapy against anticholinesterase intoxication.
AID1144133Ratio of drug level in whole blood to plasma in beagle dog treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 5 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID646770Protection against Sp-GB-Am-induced toxicity in Swiss-Webster mouse assessed as animal survival at 146 umol/mg, ip administered for 5 mins after Sp-GB-Am challenge measured after 24 hrs2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Nonquaternary reactivators for organophosphate-inhibited cholinesterases.
AID276246Reactivation of tabun inhibited AChE from rat brain at 0.1 uM2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase.
AID1471808Reactivation of VX inhibited human erythrocyte AChE assessed as reactivation rate constant using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID134320Protective index was expressed as LD50 with oxime/LD50 without oxime1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID1140217Reactivation of sarin-inhibited hemoglobin free human erythrocyte ghost acetylcholinesterase using acetylthiocholineiodide as substrate assessed as second order rate constant measured up to 1 hr by Ellman method2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE).
AID1144140Plasma concentration in beagle dog at 5 mg/kg, iv measured after 120 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID136842Compound was tested for protection of mice against ethyl p-nitrophenyl methylphosphonate (EPMP) at 2700 ug/kg plus 20 mg/kg atropine sulfate of 25 mg/Kg (1/4 LD50); 5/101989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID1140214Reactivation of sarin-inhibited hemoglobin free human erythrocyte ghost acetylcholinesterase using acetylthiocholineiodide as substrate assessed as rate constant for displacement of phosphoryl residue from phosphorylated enzyme-compound complex measured u2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE).
AID1144148Plasma concentration in beagle dog treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 240 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID120771Antidotal activity measured against soman in mice, activity expressed as the no. of survivors noted at 24 hr out of population of 10 mice each exposed intramuscularly at the dose 1/16 of 2LD50 of the compound1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 4. Effect of various side-chain substituents on therapeutic activity against anticholinesterase intoxication.
AID451158Reactivation of diisopropylfluorophosphate-inhibited AChE activity in bovine red blood cell at 5 mM after 30 mins by Ellman's method2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Fluorinated pyridinium oximes as potential reactivators for acetylcholinesterases inhibited by paraoxon organophosphorus agent.
AID1140215Reactivation of VX-inhibited hemoglobin free human erythrocyte ghost acetylcholinesterase using acetylthiocholineiodide as substrate assessed as rate constant for displacement of phosphoryl residue from phosphorylated enzyme-compound complex measured up t2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE).
AID118252Antidotal activity measured in mice exposed to tabun; activity expressed as the no. of survivors at 24 hr out of population of 10 mice each exposed intramuscularly at the dose 1/16 of 2LD50 of the compound1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 5. Structure-activity relationships for side-chain nitro-, sulfone-, amino-, and aminosulfonyl-substituted analogues for therapy against anticholinesterase intoxication.
AID1732656Reactivation of sarin-inhibited human AChE assessed as increase in enzyme activity at 100 uM incubated for 30 mins by Ellman's method relative to control2021European journal of medicinal chemistry, Apr-05, Volume: 215Molecular modeling-guided optimization of acetylcholinesterase reactivators: A proof for reactivation of covalently inhibited targets.
AID1859591Reactivation of VX induced inhibition of BChE in human plasma assessed as maximal first-order reactivation rate constant using ATCh as substrate at 1 mM incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID263585Reactivation of TEPP inhibited mouse brain AChE2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Quaternary salts of 4,3' and 4,4' bis-pyridinium monooximes. Part 2: synthesis and biological activity.
AID135979Number of surviving mice was calculated after the administration of 11.2 mg/kg of atropine sulfate, 1/8 LD50 of drug with 2-PAMCl used as base line1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 3. Synthesis and evaluation of (alkenyloxy)-, (alkynyloxy)-, and (aralkyloxy)methyl quaternarized 2-[(hydroxyimino)methyl]-1-alkylimidazolium halides as reactivators and therapy for soman intoxication
AID30843Effective rate constant for reactivation of GD-inhibited AChE activity in eel1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID710213Reactivation of tabun-inhibited human AChE assessed as reactivation rate constant2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase.
AID1311976Reactivation of VX-inhibited hemoglobin free erythrocyte ghost human AChE assessed as second order rate constant using acetylcholine iodide as substrate measured for 1 hr by spectrophotometry based Ellman method2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE).
AID301222Reactivation of 0.1 uM paraoxon-inhibited rat brain AchE2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
Monooxime reactivators of acetylcholinesterase with (E)-but-2-ene linker: preparation and reactivation of tabun- and paraoxon-inhibited acetylcholinesterase.
AID18745Reactivation rate constant with respect to enzyme(AChE) inhibition1984Journal of medicinal chemistry, Nov, Volume: 27, Issue:11
Structure-activity relationships for reactivators of organophosphorus-inhibited acetylcholinesterase: quaternary salts of 2-[(hydroxyimino)methyl]imidazole.
AID1732662Reactivation of soman-inhibited human AChE assessed as increase in enzyme activity at 100 uM incubated for 30 mins by Ellman's method relative to control2021European journal of medicinal chemistry, Apr-05, Volume: 215Molecular modeling-guided optimization of acetylcholinesterase reactivators: A proof for reactivation of covalently inhibited targets.
AID141407Compound was tested for the binding affinity towards muscarinic receptor in mouse brain membrane1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID68457In vitro rate of EPMP-inhibited acetylcholinesterase reactivation by anionic (oximate) form.1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Nonquaternary cholinesterase reactivators. 3. 3(5)-Substituted 1,2,4-oxadiazol-5(3)-aldoximes and 1,2,4-oxadiazole-5(3)-thiocarbohydroximates as reactivators of organophosphonate-inhibited eel and human acetylcholinesterase in vitro.
AID1311973Reactivation of sarin-inhibited hemoglobin free erythrocyte ghost human AChE assessed as rate constant for cleavage of P-O bond of sarin-AChE conjugate using acetylcholine iodide as substrate measured for 1 hr by spectrophotometry based Ellman method2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE).
AID14119Distribution of rat erythrocytes for tube 5 on rate of aging in 2 mL of cell suspension; Minus (-)1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Synthesis of some quaternary ammonium alkylating agents and their effects on soman-inhibited acetylcholinesterase.
AID1471833In vivo reactivation of sarin inhibited AChE in Wistar rat brain at 2.8 mg/kg, iv at 1 min measured after 4 hrs by Ellman's method2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID1859599Reactivation of VX induced inhibition of BChE in human plasma assessed as time needed to achieve maximal re activation using ATCh as substrate at 1 mM incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1732658Inhibition of human AChE assessed as decrease in enzyme activity incubated for 30 mins by Ellman's method2021European journal of medicinal chemistry, Apr-05, Volume: 215Molecular modeling-guided optimization of acetylcholinesterase reactivators: A proof for reactivation of covalently inhibited targets.
AID31641Effective rate constant for reactivation of GD-inhibited AChE in human erythrocytes1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID615409Reactivation of VX-inhibited electric eel AChE activity at 0.0001 M and pH 8 after 10 mins by Ellman's method relative to control2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE).
AID31647Bimolecular reactivation rate constant1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID26067pKa Rate constant at 25 degree Centigrade1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Sulfur derivatives of 2-oxopropanal oxime as reactivators of organophosphate-inhibited acetylcholinesterase in vitro: synthesis and structure-reactivity relationships.
AID31034Reversible inhibition of acetylcholinesterase (AChE) by 50 % in human erythrocytes 1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 3. Synthesis and evaluation of (alkenyloxy)-, (alkynyloxy)-, and (aralkyloxy)methyl quaternarized 2-[(hydroxyimino)methyl]-1-alkylimidazolium halides as reactivators and therapy for soman intoxication
AID1859582Reactivation of cyclosarin induced inhibition of BChE in human plasma assessed as dissociation constant using ATCh as substrate incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1859588Reactivation of tabun induced inhibition of BChE in human plasma assessed as second-order rate constant using ATCh as substrate incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID392539Reactivation of paraoxon-inhibited house fly AChE at 5 mM after 1 hr2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
Reactivation potency of fluorinated pyridinium oximes for acetylcholinesterases inhibited by paraoxon organophosphorus agent.
AID120773antidotal activity was measured against soman in mice and activity expressed as the no. of survivors noted at 24 hr out of population of 10 mice each exposed intramuscularly at the dose 1/64 of 2LD50 of the compound1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 4. Effect of various side-chain substituents on therapeutic activity against anticholinesterase intoxication.
AID233922Dose producing no observable symptom, sign free dose was evaluated1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Sulfur derivatives of 2-oxopropanal oxime as reactivators of organophosphate-inhibited acetylcholinesterase in vitro: synthesis and structure-reactivity relationships.
AID91074In vitro rate of EPMP-inhibited acetylcholinesterase reactivation, by the protonated (oxime) form.1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Nonquaternary cholinesterase reactivators. 3. 3(5)-Substituted 1,2,4-oxadiazol-5(3)-aldoximes and 1,2,4-oxadiazole-5(3)-thiocarbohydroximates as reactivators of organophosphonate-inhibited eel and human acetylcholinesterase in vitro.
AID1471807Reactivation of tabun inhibited human erythrocyte AChE assessed as overall biomolecular reactivation rate constant using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID30683Inhibition of acetylcholinesterase (AChE) in bovine erythrocyte(RBC)1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID260332Reactivation potency against inhibited AChE from rat brain homogenate at 1 mM2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Synthesis of the novel series of bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against chlorpyrifos-inhibited acetylcholinesterase.
AID1865771Reactivation of POX-inhibited electric eel recombinant AChE assessed as reactivation rate constant using ATC as substrate at 1 mM followed by substrate addition by Ellman's method based spectrophotometry2021RSC medicinal chemistry, Sep-23, Volume: 12, Issue:9
Dual acting oximes designed for therapeutic decontamination of reactive organophosphates
AID302657Reactivation activity of tabun-inhibited AChE in rat brain at 1 mM after 30 mins2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Design of a potent reactivator of tabun-inhibited acetylcholinesterase--synthesis and evaluation of (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203).
AID710205Reactivation of paraoxon-inhibited human AChE assessed as bimolecular reactivation rate constant2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase.
AID1127118Reactivation of methylphosphonothioate VX-inhibited recombinant human AChE measured up to 10 mins by Ellman's method2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and biological evaluation of novel tetrahydroacridine pyridine- aldoxime and -amidoxime hybrids as efficient uncharged reactivators of nerve agent-inhibited human acetylcholinesterase.
AID1144171Drug excretion in human at 1 g, po1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1237002Reactivation of O-ethylsarin-inhibited human acetylcholinesterase assessed as dissociation constant incubated for 60 mins using ATChI substrate by DTNB dye based UV-visible spectrophotometry2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and in vitro kinetic evaluation of N-thiazolylacetamido monoquaternary pyridinium oximes as reactivators of sarin, O-ethylsarin and VX inhibited human acetylcholinesterase (hAChE).
AID1471831Anticholinergic activity in Wistar rat assessed as protection against sarin-induced convulsions at 2.8 mg/kg, iv after 4 hrs2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID364800Permeability across rat brain2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Monoquaternary pyridinium salts with modified side chain-synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase.
AID31645Bimolecular rate constant for reactivation of AchE in human erythrocytes 1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 3. Synthesis and evaluation of (alkenyloxy)-, (alkynyloxy)-, and (aralkyloxy)methyl quaternarized 2-[(hydroxyimino)methyl]-1-alkylimidazolium halides as reactivators and therapy for soman intoxication
AID1732661Reactivation of dichlorvos-inhibited human AChE assessed as increase in enzyme activity at 100 uM incubated for 30 mins by Ellman's method relative to control2021European journal of medicinal chemistry, Apr-05, Volume: 215Molecular modeling-guided optimization of acetylcholinesterase reactivators: A proof for reactivation of covalently inhibited targets.
AID1237001Reactivation of sarin-inhibited human acetylcholinesterase assessed as dissociation constant incubated for 60 mins using ATChI substrate by DTNB dye based UV-visible spectrophotometry2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and in vitro kinetic evaluation of N-thiazolylacetamido monoquaternary pyridinium oximes as reactivators of sarin, O-ethylsarin and VX inhibited human acetylcholinesterase (hAChE).
AID1859594Reactivation of cyclosarin induced inhibition of BChE in human plasma assessed as maximal achieved reactivation using ATCh as substrate at 1 mM incubated for 30 mins by Ellman's method relative to control2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1471803Reactivation of cyclosarin inhibited human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID1144159Drug level in beagle dog whole blood treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 360 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1144179Retardation factor of the compound1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1311977Inhibition of hemoglobin free erythrocyte ghost human AChE using acetylcholine iodide as substrate measured for 1 hr by spectrophotometry based Ellman method2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE).
AID301221Reactivation of 0.1 uM tabun-inhibited rat brain AchE2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
Monooxime reactivators of acetylcholinesterase with (E)-but-2-ene linker: preparation and reactivation of tabun- and paraoxon-inhibited acetylcholinesterase.
AID1311975Reactivation of sarin-inhibited hemoglobin free erythrocyte ghost human AChE assessed as second order rate constant using acetylcholine iodide as substrate measured for 1 hr by spectrophotometry based Ellman method2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE).
AID14118Distribution of rat erythrocytes for tube 4 on rate of aging in 2 mL of cell suspension; Plus (+)1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Synthesis of some quaternary ammonium alkylating agents and their effects on soman-inhibited acetylcholinesterase.
AID17066Second-order rate constant for attack on PNPA at 25 degree Centigrade1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Sulfur derivatives of 2-oxopropanal oxime as reactivators of organophosphate-inhibited acetylcholinesterase in vitro: synthesis and structure-reactivity relationships.
AID1144153Drug level in beagle dog whole blood treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 45 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID301220Reactivation of 1 mM paraoxon-inhibited rat brain AchE2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
Monooxime reactivators of acetylcholinesterase with (E)-but-2-ene linker: preparation and reactivation of tabun- and paraoxon-inhibited acetylcholinesterase.
AID1144184Ratio of drug level in whole blood to plasma in beagle dog treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 60 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1237004Reactivation of sarin-inhibited human acetylcholinesterase assessed as reactivity rate constant incubated for 60 mins using ATChI substrate by DTNB dye based UV-visible spectrophotometry2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and in vitro kinetic evaluation of N-thiazolylacetamido monoquaternary pyridinium oximes as reactivators of sarin, O-ethylsarin and VX inhibited human acetylcholinesterase (hAChE).
AID615412Reactivation of VX-inhibited electric eel AChE activity after 40 mins by Ellman's method relative to control2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE).
AID710208Binding affinity to paraoxon-human AChE complex2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase.
AID1237009Reactivation of VX-inhibited human acetylcholinesterase assessed as second order rate constant incubated for 60 mins using ATChI substrate by DTNB dye based UV-visible spectrophotometry2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and in vitro kinetic evaluation of N-thiazolylacetamido monoquaternary pyridinium oximes as reactivators of sarin, O-ethylsarin and VX inhibited human acetylcholinesterase (hAChE).
AID1144149Drug level in beagle dog whole blood treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 5 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID118251Antidotal activity was measured against soman in mice and activity expressed as the no. of survivors noted at 24 hr out of population of 10 mice (exposed intramuscularly at the dose 1/64 of 2LD50)1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 5. Structure-activity relationships for side-chain nitro-, sulfone-, amino-, and aminosulfonyl-substituted analogues for therapy against anticholinesterase intoxication.
AID14123Distribution of rat erythrocytes for tube 7 on rate of aging in 2 mL of cell suspension; Plus (+)1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Synthesis of some quaternary ammonium alkylating agents and their effects on soman-inhibited acetylcholinesterase.
AID1144167Drug excretion in beagle dog feces at 43.9 mg/kg, po1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID14121Distribution of rat erythrocytes for tube 6 on rate of aging in 2 mL of cell suspension; Minus (-)1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Synthesis of some quaternary ammonium alkylating agents and their effects on soman-inhibited acetylcholinesterase.
AID1859597Reactivation of sarin induced inhibition of BChE in human plasma assessed as time needed to achieve maximal reactivation using ATCh as substrate at 1 mM incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1144190Reactivation of AChE in ICR mouse brain at 30 mg/kg, iv administered 15 mins post DFP challenge measured after 90 mins by Ellman method relative to control1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 3. Delivery of N-methylpyridinium-2-carbaldoxime chloride through the blood-brain barrier in its dihydropyridine pro-drug form.
AID1859576Reactivation of tabun induced inhibition of recombinant human AChE assessed as time needed to achieve maximal reactivation using ATCh as substrate at 100 uM incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID30847In vitro reversible inhibition of eel acetylcholinesterase.1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Nonquaternary cholinesterase reactivators. 3. 3(5)-Substituted 1,2,4-oxadiazol-5(3)-aldoximes and 1,2,4-oxadiazole-5(3)-thiocarbohydroximates as reactivators of organophosphonate-inhibited eel and human acetylcholinesterase in vitro.
AID1859590Reactivation of cyclosarin induced inhibition of BChE in human plasma assessed as maximal first-order reactivation rate constant using ATCh as substrate at 1 mM incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID307195Reactivation of 10 uM paraoxon-induced inhibition of AChE in rat brain at pH 7.6 after 10 mins2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Novel series of bispyridinium compounds bearing a (Z)-but-2-ene linker--synthesis and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase.
AID615407Reactivation of diisopropyl phosphorofluoridate-inhibited electric eel AChE activity at 0.0001 M and pH 8 after 10 mins by Ellman's method relative to control2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE).
AID1471812Toxicity in Wistar rat assessed as labored breathing at 32 umol/kg, iv2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID1144162Drug excretion in beagle dog urine assessed as radioactivity at 7 mg/kg, iv by liquid scintillation counting1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1311971Binding affinity to sarin-inhibited hemoglobin free erythrocyte ghost human AChE using acetylcholine iodide as substrate measured for 1 hr by spectrophotometry based Ellman method2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE).
AID31032Concentration required to inhibit 50% of acetylcholinesterase (AChE) in human erythrocyte(RBC).1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID68459In vitro rate of EPMP-inhibited acetylcholinesterase reactivation, by the protonated (oxime) form.1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Nonquaternary cholinesterase reactivators. 3. 3(5)-Substituted 1,2,4-oxadiazol-5(3)-aldoximes and 1,2,4-oxadiazole-5(3)-thiocarbohydroximates as reactivators of organophosphonate-inhibited eel and human acetylcholinesterase in vitro.
AID615404Reactivation of sarin-inhibited electric eel AChE activity at 0.001 M and pH 8 after 10 mins by Ellman's method relative to control2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE).
AID1859595Reactivation of VX induced inhibition of BChE in human plasma assessed as maximal achieved reactivation using ATCh as substrate at 1 mM incubated for 30 mins by Ellman's method relative to control2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1237008Reactivation of O-ethylsarin-inhibited human acetylcholinesterase assessed as second order rate constant incubated for 60 mins using ATChI substrate by DTNB dye based UV-visible spectrophotometry2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and in vitro kinetic evaluation of N-thiazolylacetamido monoquaternary pyridinium oximes as reactivators of sarin, O-ethylsarin and VX inhibited human acetylcholinesterase (hAChE).
AID30242Compound was tested for the competitive inhibition of acetylcholinesterase (AChE)1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID1144173Drug excretion in iv dosed beagle dog urine treated with [14C]-labelled N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride by radiochromatography1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1144181Ratio of drug level in whole blood to plasma in beagle dog treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 15 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1859570Reactivation of cyclosarin induced inhibition of recombinant human AChE assessed as time needed to achieve maximal reactivation using ATCh as substrate at 100 uM incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1529749Reactivation of paraoxon-inhibited electric eel AChE assessed as residual activity at 1 uM using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured every 3 mins for 15 mins relative to control2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
Novel tacrine-pyridinium hybrid reactivators of organophosphorus-inhibited acetylcholinesterase: Synthesis, molecular docking, and in vitro reactivation study.
AID1144164Drug excretion in beagle dog urine at 43.9 mg/kg, po1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID226936Protective index was calculated as the ratio of LD50 (paraoxon +compound) /LD50 (paraoxon)1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Sulfur derivatives of 2-oxopropanal oxime as reactivators of organophosphate-inhibited acetylcholinesterase in vitro: synthesis and structure-reactivity relationships.
AID89919In vitro rate of EPMP-inhibited acetylcholinesterase reactivation, by anionic (oximate) form.1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Nonquaternary cholinesterase reactivators. 3. 3(5)-Substituted 1,2,4-oxadiazol-5(3)-aldoximes and 1,2,4-oxadiazole-5(3)-thiocarbohydroximates as reactivators of organophosphonate-inhibited eel and human acetylcholinesterase in vitro.
AID1144136Plasma concentration in beagle dog at 5 mg/kg, iv measured after 15 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1144157Drug level in beagle dog whole blood treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 240 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1859607Neuroprotective activity against cyclosarin-induced CD-1 mouse assessed as protective agent at 26.4 mg/kg, IM after 24 hrs2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1140212Binding affinity to sarin-inhibited hemoglobin free human erythrocyte ghost acetylcholinesterase using acetylthiocholineiodide as substrate measured up to 1 hr by Ellman method2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE).
AID1471799Reactivation of sarin inhibited human erythrocyte AChE assessed as reactivation rate constant using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID1471821Anticholinergic activity in Wistar rat assessed as protection against sarin-induced seizure by measuring total EEG power AUC in brain at 2.8 mg/kg, iv after 4 hrs2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID14116Distribution of rat erythrocytes for tube 3 on rate of aging in 2 mL of cell suspension; Plus (+)1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Synthesis of some quaternary ammonium alkylating agents and their effects on soman-inhibited acetylcholinesterase.
AID1471832Anticholinergic activity in Wistar rat assessed as protection against sarin-induced seizure at 2.8 mg/kg, iv after 4 hrs2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID1144186Ratio of drug level in whole blood to plasma in beagle dog treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 240 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID615414Dissociation constant, pKa of the compound by spectrophotometric analysis2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE).
AID1144182Ratio of drug level in whole blood to plasma in beagle dog treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 30 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1144150Drug level in beagle dog whole blood treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 10 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID120772Antidotal activity measured against soman in mice and activity expressed as the no. of survivors noted at 24 hr out of population of 10 mice each exposed intramuscularly at the dose 1/4 of 2LD50 of the compound1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 4. Effect of various side-chain substituents on therapeutic activity against anticholinesterase intoxication.
AID25773Effective biomolecular rate constant at the concentration 10 uM [HOX] in the conditions of 25degreeC,pH 7.61984Journal of medicinal chemistry, Nov, Volume: 27, Issue:11
Structure-activity relationships for reactivators of organophosphorus-inhibited acetylcholinesterase: quaternary salts of 2-[(hydroxyimino)methyl]imidazole.
AID14114Distribution of rat erythrocytes for tube 2 on rate of aging in 2 mL of cell suspension; Plus (+)1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Synthesis of some quaternary ammonium alkylating agents and their effects on soman-inhibited acetylcholinesterase.
AID31610Effective rate constant for reactivation of the Acetylcholinesterase by the compound at PH 7.6 was determined1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 4. Effect of various side-chain substituents on therapeutic activity against anticholinesterase intoxication.
AID30836Bimolecular reactivation rate constant1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID145513Compound was tested for the binding affinity towards Nicotinic acetylcholine receptor1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID26020Reactivation rate constant with respect to oxmiate concentration (1/OX (1/uM) =0.345)1984Journal of medicinal chemistry, Nov, Volume: 27, Issue:11
Structure-activity relationships for reactivators of organophosphorus-inhibited acetylcholinesterase: quaternary salts of 2-[(hydroxyimino)methyl]imidazole.
AID24443logP is the octanol/buffer partition coefficient for 0.1M, pH 7.8 phosphate buffer1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Sulfur derivatives of 2-oxopropanal oxime as reactivators of organophosphate-inhibited acetylcholinesterase in vitro: synthesis and structure-reactivity relationships.
AID17240K2, The intrinsic biomolecular reactivation rate constant on sarin at 25 degree Centigrade1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Sulfur derivatives of 2-oxopropanal oxime as reactivators of organophosphate-inhibited acetylcholinesterase in vitro: synthesis and structure-reactivity relationships.
AID710212Reactivation of VX-inhibited human AChE assessed as bimolecular reactivation rate constant2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase.
AID1144185Ratio of drug level in whole blood to plasma in beagle dog treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 180 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1144145Plasma concentration in beagle dog treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 45 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1144191Reactivation of AChE in ICR mouse brain at 40 mg/kg, iv administered 15 mins post DFP challenge measured after 90 mins by Ellman method relative to control1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 3. Delivery of N-methylpyridinium-2-carbaldoxime chloride through the blood-brain barrier in its dihydropyridine pro-drug form.
AID351912Reactivation of diisopropyl phosphorofluoridate-induced electric eel AChE inhibition at 0.1 mM by Ellman's method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and evaluation of novel bis-pyridinium oximes as reactivators of DFP-inhibited acetylcholinesterase.
AID1471809Reactivation of VX inhibited human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID364612Reactivation of 10 uM tabun inhibited AChE in rat brain homogenate2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Monoquaternary pyridinium salts with modified side chain-synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase.
AID30845Bimolecular reactivation rate constant1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID1140219Inhibition of hemoglobin free human erythrocyte ghost acetylcholinesterase using acetylthiocholineiodide as substrate measured up to 1 hr by Ellman method2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE).
AID1144152Drug level in beagle dog whole blood treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 30 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1859598Reactivation of cyclosarin induced inhibition of BChE in human plasma assessed as time needed to achieve maximal reactivation using ATCh as substrate at 1 mM incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1471805Reactivation of tabun inhibited human erythrocyte AChE assessed as reactivation rate constant using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID1859568Reactivation of cyclosarin induced inhibition of recombinant human AChE assessed as maximal first-order reactivation rate constant using ATCh as substrate at 100 uM incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1471796Reactivation of cyclosarin inhibited human erythrocyte AChE assessed as residual activity at 10 to 1000 uM using acetylthiocholine iodide as substrate preincubated for 2 to 120 mins followed by substrate addition measured for 3 mins by Ellman's method2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID1144142Plasma concentration in beagle dog treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 10 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1859581Reactivation of sarin induced inhibition of BChE in human plasma assessed as dissociation constant using ATCh as substrate incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID136839Compound was tested for protection of mice against ethyl p-nitrophenyl methylphosphonate (EPMP) at 2000 ug/kg plus 20 mg/kg atropine sulfate of 25 mg/kg (1/4 LD50); 5/101989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID451159Reactivation of paraoxon-inhibited AChE activity in bovine red blood cell at 5 mM after 1 hr by Ellman's method2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Fluorinated pyridinium oximes as potential reactivators for acetylcholinesterases inhibited by paraoxon organophosphorus agent.
AID1865766Effect on human recombinant AChE assessed as decrease in enzyme activity using ATC as substrate at 1 mM followed by substrate addition by Ellman's method based spectrophotometry2021RSC medicinal chemistry, Sep-23, Volume: 12, Issue:9
Dual acting oximes designed for therapeutic decontamination of reactive organophosphates
AID1144187Protection against phospholine iodide-induced toxicity in white mouse assessed as survival at 50 mg/kg administered 10 mins prior to phospholine iodide challenge1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 3. Delivery of N-methylpyridinium-2-carbaldoxime chloride through the blood-brain barrier in its dihydropyridine pro-drug form.
AID1859579Reactivation of VX induced inhibition of BChE in human plasma assessed as first-order reactivation rate constant using ATCh as substrate incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1144134Plasma concentration in beagle dog at 5 mg/kg, iv measured after 5 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID31634Percentage of maximum reactivation of GD-inhibited human erythrocyte acetylcholinesterase (AChE)1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
AID1144141Plasma concentration in beagle dog treated with N-Methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride at 5 mg/kg, iv measured after 5 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID710209Binding affinity to tabun-human AChE complex2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase.
AID260333Reactivation potency against inhibited AChE from rat brain homogenate at 0.01 mM2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Synthesis of the novel series of bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against chlorpyrifos-inhibited acetylcholinesterase.
AID364613Reactivation of 1000 uM paraoxon inhibited AChE in rat brain homogenate2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Monoquaternary pyridinium salts with modified side chain-synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase.
AID134554Significant protection against the lethal effects of soman, by administering compound intramuscularly in mouse1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 3. Synthesis and evaluation of (alkenyloxy)-, (alkynyloxy)-, and (aralkyloxy)methyl quaternarized 2-[(hydroxyimino)methyl]-1-alkylimidazolium halides as reactivators and therapy for soman intoxication
AID1859566Reactivation of sarin induced inhibition of recombinant human AChE assessed as maximal achieved reactivation using ATCh as substrate at 100 uM incubated for 30 mins by Ellman's method relative to control2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1471810Reactivation of VX inhibited human erythrocyte AChE assessed as overall biomolecular reactivation rate constant using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID615405Reactivation of sarin-inhibited electric eel AChE activity at 0.0001 M and pH 8 after 10 mins by Ellman's method relative to control2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE).
AID364614Reactivation of 10 uM paraoxon inhibited AChE in rat brain homogenate2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Monoquaternary pyridinium salts with modified side chain-synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase.
AID1865769Reactivation of POX-inhibited electric eel recombinant AChE assessed as reactivation rate constant using ATC as substrate at 0.1 mM followed by substrate addition by Ellman's method based spectrophotometry2021RSC medicinal chemistry, Sep-23, Volume: 12, Issue:9
Dual acting oximes designed for therapeutic decontamination of reactive organophosphates
AID68458The compound was tested for % of maximum reactivation for GD-inhibited Eel AChE (Acetylcholinesterase) by oximes1984Journal of medicinal chemistry, Nov, Volume: 27, Issue:11
Structure-activity relationships for reactivators of organophosphorus-inhibited acetylcholinesterase: quaternary salts of 2-[(hydroxyimino)methyl]imidazole.
AID302661Binding affinity to tabun-inhibited AChE2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Design of a potent reactivator of tabun-inhibited acetylcholinesterase--synthesis and evaluation of (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203).
AID25779Biomolecular rate constant for reactivation and measure of the inherent reactivity of the oximate form of the reactivator at the concentration 10 uM [HOX] in the conditions of 25degreeC,pH 7.61984Journal of medicinal chemistry, Nov, Volume: 27, Issue:11
Structure-activity relationships for reactivators of organophosphorus-inhibited acetylcholinesterase: quaternary salts of 2-[(hydroxyimino)methyl]imidazole.
AID1865764Reactivation of POX-inhibited human recombinant AChE assessed as reactivation rate constant using ATC as substrate at 0.5 mM followed by substrate addition by Ellman's method based spectrophotometry2021RSC medicinal chemistry, Sep-23, Volume: 12, Issue:9
Dual acting oximes designed for therapeutic decontamination of reactive organophosphates
AID1859587Reactivation of VX induced inhibition of BChE in human plasma assessed as second-order rate constant using ATCh as substrate incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1859578Reactivation of cyclosarin induced inhibition of BChE in human plasma assessed as first-order reactivation rate constant using ATCh as substrate incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID31028Compound was tested for the concentration required for reversible inhibition of human acetylcholinesterase. 1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Nonquaternary cholinesterase reactivators. 3. 3(5)-Substituted 1,2,4-oxadiazol-5(3)-aldoximes and 1,2,4-oxadiazole-5(3)-thiocarbohydroximates as reactivators of organophosphonate-inhibited eel and human acetylcholinesterase in vitro.
AID1237003Reactivation of VX-inhibited human acetylcholinesterase assessed as dissociation constant incubated for 60 mins using ATChI substrate by DTNB dye based UV-visible spectrophotometry2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Synthesis and in vitro kinetic evaluation of N-thiazolylacetamido monoquaternary pyridinium oximes as reactivators of sarin, O-ethylsarin and VX inhibited human acetylcholinesterase (hAChE).
AID1471802Reactivation of cyclosarin inhibited human erythrocyte AChE assessed as reactivation rate constant using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method2017Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22
Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase.
AID1144170Drug excretion in po dosed human1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID710207Reactivation of tabun-inhibited human AChE assessed as bimolecular reactivation rate constant2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase.
AID646771Protection against Sp-GB-Am-induced toxicity in Swiss-Webster mouse assessed as animal survival at 36.2 umol/mg, ip administered for 5 mins after Sp-GB-Am challenge measured after 24 hrs2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Nonquaternary reactivators for organophosphate-inhibited cholinesterases.
AID1144139Plasma concentration in beagle dog at 5 mg/kg, iv measured after 60 mins1976Journal of medicinal chemistry, Jan, Volume: 19, Issue:1
Improved delivery through biological membranes. 2. Distribution, excretion, and metabolism of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, a pro-drug of N-methylpyridinium-2-carbaldoxime chloride.
AID1311972Binding affinity to VX-inhibited hemoglobin free erythrocyte ghost human AChE using acetylcholine iodide as substrate measured for 1 hr by spectrophotometry based Ellman method2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE).
AID1859531Dissociation constant, pKa of the compound2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID1859584Reactivation of tabun induced inhibition of BChE in human plasma assessed as dissociation constant using ATCh as substrate incubated for 30 mins by Ellman's method2022European journal of medicinal chemistry, Aug-05, Volume: 238Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents.
AID307192Reactivation of 1000 uM tabun-induced inhibition of AChE in rat brain at pH 7.6 after 10 mins2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Novel series of bispyridinium compounds bearing a (Z)-but-2-ene linker--synthesis and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase.
AID615408Reactivation of VX-inhibited electric eel AChE activity at 0.001 M and pH 8 after 10 mins by Ellman's method relative to control2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE).
AID118254Antidotal activity against tabun in mice, activity expressed as the no. of survivors noted at 24 hr out of population of 10 mice each exposed intramuscularly at the dose 1/64 of 2LD50 of the compound1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 5. Structure-activity relationships for side-chain nitro-, sulfone-, amino-, and aminosulfonyl-substituted analogues for therapy against anticholinesterase intoxication.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (50)

TimeframeStudies, This Drug (%)All Drugs %
pre-19908 (16.00)18.7374
1990's2 (4.00)18.2507
2000's13 (26.00)29.6817
2010's18 (36.00)24.3611
2020's9 (18.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other50 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]