huperzine A: RN given refers to 5R-(5alpha,9beta,11E)-isomer; structure given in first source
huperzine A : A sesquiterpene alkaloid isolated from a club moss Huperzia serrata that has been shown to exhibit neuroprotective activity. It is also an effective inhibitor of acetylcholinesterase and has attracted interest as a therapeutic candidate for Alzheimer's disease.
Flora | Rank | Flora Definition | Family | Family Definition |
---|---|---|---|---|
Huperzia | genus | A plant genus of the family LYCOPODIACEAE. Members contain huperzine, one of the CHOLINESTERASE INHIBITORS.[MeSH] | Lycopodiaceae | The club-moss plant family of the order Lycopodiales, class Lycopodiopsida, division Lycopodiophyta, subkingdom TRACHEOPHYTA. The common name of clubmoss applies to several genera of this family. Despite the name this is not one of the true mosses (BRYOPSIDA ).[MeSH] |
Huperzia serrata | species | [no description available] | Lycopodiaceae | The club-moss plant family of the order Lycopodiales, class Lycopodiopsida, division Lycopodiophyta, subkingdom TRACHEOPHYTA. The common name of clubmoss applies to several genera of this family. Despite the name this is not one of the true mosses (BRYOPSIDA ).[MeSH] |
ID Source | ID |
---|---|
PubMed CID | 1253 |
CHEMBL ID | 3184073 |
MeSH ID | M0143991 |
PubMed CID | 854026 |
CHEMBL ID | 395280 |
CHEBI ID | 78330 |
CHEBI ID | 94624 |
SCHEMBL ID | 136368 |
MeSH ID | M0143991 |
Synonym |
---|
120786-18-7 |
CBIOL_001885 |
huperzine a |
fordine |
BIO2_000882 |
BIO2_000402 |
BIO1_001149 |
BIO1_000171 |
BIO1_000660 |
BSPBIO_001143 |
selagine |
(-)-huperzine a , |
bdbm10441 |
(+)-huperzine a |
(13e)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.0^{2,7}]trideca-2(7),3,10-trien-5-one |
(1r,13e)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.0^{2,7}]trideca-2(7),3,10-trien-5-one |
(5s,11e)-5-amino-11-ethylidene-7-methyl-5,6,9,10-tetrahydro-5,9-methanocycloocta[b]pyridin-2(1h)-one |
(1s,13e)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.0^{2,7}]trideca-2(7),3,10-trien-5-one |
(+/-)huperzine a |
IDI1_002157 |
(+/-)-huperzine a |
NCGC00163246-01 |
KBIO2_003051 |
KBIOSS_000483 |
KBIO2_000483 |
KBIO3_000885 |
KBIO2_005619 |
KBIOGR_000483 |
KBIO3_000886 |
102518-79-6 |
HMS1990I05 |
103735-86-0 |
huperzine-a |
FT-0642946 |
5,9-methanocycloocta(b)pyridin-2(1h)-one,5-amino-11-ethylidene-5,6,9,10-tetrah |
CHEMBL3184073 |
(-)-huperzine a-d5 (major) |
1290113-17-5 |
AKOS032962044 |
Q27163539 |
lsm-1581 |
BCP31534 |
fordine; (+/-)-huperzine a |
1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.02,7]trideca-2(7),3,10-trien-5-one |
(1r,9r)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.0^{2,7]trideca-2(7),3,10-trien-5-one |
(1r,9r,13e)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.0^{2,7]trideca-2(7),3,10-trien-5-one |
(13e)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.02,7]trideca-2(7),3,10-trien-5-one |
BRD-K62240499-001-02-6 |
SDCCGMLS-0066755.P001 |
hup a |
cerebra |
5,9-methanocycloocta(b)pyridin-2(1h)-one, 5-amino-11-ethylidene-5,6,9,10-tetrahydro-7-methyl-, (5r-(5-alpha,9-beta,11e))- |
5,9-methanocycloocta(b)pyridin-2(1h)-one, 5-amino-11-ethylidene-5,6,9,10-tetrahydro-7-methyl-, (5r,9r,11e)- |
HUP , |
huperaine a |
1VOT |
SPECTRUM1505255 |
1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.0~2,7~]trideca-2(7),3,10-trien-5-one |
1-amino-13-ethylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one((+/-)-huperzine a) |
(+-)-ha |
bdbm50199522 |
(huperazine a)(-)-1-amino-13-ethylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one |
(r)-1-amino-13-ethylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one |
1-amino-13-ethylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one((-)-huperzine a) |
(-)-huperazine a |
1-amino-13-eth-(e)-ylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one |
(-)1-amino-13-ethylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one( (-)-huperzine a) |
1-amino-13-ethylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one |
1-amino-13-eth-(z)-ylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one |
hyperazzine a |
(-)-1-amino-13-ethylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one(huperzine a) |
(r)-1-amino-13-eth-(e)-ylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one |
(1r,9r)-1-amino-13-eth-(e)-ylidene-11-methyl-6-aza-tricyclo[7.3.1.0*2,7*]trideca-2(7),3,10-trien-5-one |
chebi:78330 , |
CHEMBL395280 , |
l-huperzine a |
tox21_111603 |
dtxcid6026038 |
cas-102518-79-6 |
dtxsid8046038 , |
CCG-40292 |
kimpukan a |
0111871i23 , |
unii-0111871i23 |
huperzine a [who-dd] |
(5r,9r,11e)-5-amino-11-ethylidene-5,6,9,10-tetrahydro-7-methyl-5,9-methanocycloocta(b)pyridin-2(1h)-one |
huperzine a [vandf] |
huperzine a [mi] |
DB04864 |
SCHEMBL136368 |
NCGC00263655-01 |
tox21_111603_1 |
H1700 |
(5r,9r,11e)-5-amino-11-ethylidene-7-methyl-5,6,9,10-tetrahydro-5,9-methanocycloocta[b]pyridin-2(1h)-one |
(5r,9r,e)-5-amino-11-ethylidene-7-methyl-5,6,9,10-tetrahydro-5,9-methanocycloocta[b]pyridin-2(1h)-one |
Q-100029 |
5,9-methanocycloocta[b]pyridin-2(1h)-one, 5-amino-11-ethylidene-5,6,9,10-tetrahydro-7-methyl-, (5r,9r,11e)- |
CHEBI:94624 |
huperzin a |
1369-64-8 |
Q425198 |
AS-15723 |
AKOS016842839 |
(-)-huperazinea |
(1r,9r,13e)-1-amino-13-ethylidene-11-methyl-6-azatricyclo[7.3.1.0,2,7]trideca-2(7),3,10-trien-5-one |
EN300-33171546 |
Huperzine A (Hup A) is a purified alkaloid compound extracted from a club moss called Huperzia serrata. It is an effective inhibitor of acetylcholinesterase and has attracted great interest as a therapeutic candidate for Alzheimer's disease.
Huperzine A has been shown to be useful in the treatment of symptoms of dementia of the Alzheimer type.
Huperzine A can inhibit cholinesterase in the brain to improve the cognitive function of rats recovering from general anesthesia.
Excerpt | Reference | Relevance |
---|---|---|
"Huperzine A can inhibit cholinesterase to increase Ach, which has a positive effect on cerebral cholinergic system in elderly patients during recovery from general anesthesia." | ( [Effect of huperzine A on cerebral cholinesterase and acetylcholine in elderly patients during recovery from general anesthesia]. Wang, G; Zhan, H; Zhang, SQ, 2006) | 2.17 |
"Huperzine A can inhibit cholinesterase in the brain to improve the cognitive function of rats recovering from general anesthesia." | ( [Effects of huperzine A on cognitive function of rats recovering from general anesthesia]. Chen, HW; Luo, GJ; Wang, G; Zhan, H; Zhang, SQ, 2008) | 2.17 |
Huperzine A treatment (0.1 mg/kg) resulted in significant protection against both HI-induced brain tissue losses and spatial memory impairments. Treatment also reduced glutamate-induced calcium mobilization, but did not affect elevations in intraneuronal free Ca2+ caused by KCl or (-)Bay K 8644.
Excerpt | Reference | Relevance |
---|---|---|
"Huperzine A treatment was shown to significantly attenuate the neurotoxicity of oligomeric Aβ(42), as demonstrated by increased neuronal viability." | ( Involvement of Intracellular and Mitochondrial Aβ in the Ameliorative Effects of Huperzine A against Oligomeric Aβ42-Induced Injury in Primary Rat Neurons. Jiang, HL; Lei, Y; Qin, MY; Tang, XC; Yang, HY; Yang, L; Ye, CY; Zhang, HY, 2015) | 1.36 |
"Huperzine A treatment significantly ameliorated all these phenomena." | ( Huperzine a improves chronic inflammation and cognitive decline in rats with cerebral hypoperfusion. Tang, XC; Wang, J; Zhang, HY, 2010) | 2.52 |
"Huperzine A treatment (0.1 mg/kg) resulted in significant protection against both HI-induced brain tissue losses and spatial memory impairments (mean escape latency: 34 s vs 44 s, P < 0.05, probe time: 35 s vs 14 s,P < 0.01)." | ( [Huperzine A attenuates cognitive deficits and brain injury after hypoxia-ischemic brain damage in neonatal rats]. Shao, XM; Tang, XC; Wang, LS; Zhou, J, 2003) | 1.95 |
"Huperzine A pretreatment also reduced glutamate-induced calcium mobilization, but did not affect elevations in intraneuronal free Ca2+ ([Ca]i) caused by KCl or (-)Bay K 8644." | ( Huperzine A, a potential therapeutic agent for dementia, reduces neuronal cell death caused by glutamate. Dave, JR; Doctor, BP; Koenig, ML; Ved, HS, 1997) | 2.46 |
"Treatment with Huperzine A, a compound isolated from Chinese club moss with NMDA receptor blocking activity, anticholinesterase activity, and anticonvulsant properties, produced useful suppression of the abnormal behavior for more than months." | ( Clinical use of an herbal-derived compound (Huperzine A) to treat putative complex partial seizures in a dog. Dodman, NH; Faissler, D; Ogata, N; Schneider, BM, 2009) | 0.95 |
Huperzine A is toxic at higher doses due to potent AChE inhibition which limits the utilization of its neuroprotective properties. Mild and transient adverse events (edema of bilateral ankles and insomnia) were observed in 3% of huperzine Alpha treated patients.
Huperzine A, an acetylcholinesterase inhibitor used to treat Alzheimer's disease (AD) patients in China, exhibits different pharmacokinetic features in elderly and young healthy subjects. After single-dose administration of ZT-1, the mean tmax of Hup A was 0.
Huperzine A (hup A) is a reversible and highly selective second-generation acetylcholine esterase (AchE) inhibitor for treating Alzheimer's disease (AD) But it suffers from low bioavailability in the brain.
Huperzine A's permeability characteristics pave the way to the development of its oral extended release dosage form. The improving effects of huperZine A exhibited a bell-shaped dose-response curve. The effect of hSuperZine on memory impairments exhibited an inverted U-shapeddose-response pattern.
Product Category | Products |
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Active Lifestyle & Fitness | 22 |
Vitamins & Supplements | 2 |
Weight Management | 2 |
Role | Description |
---|---|
EC 3.1.1.7 (acetylcholinesterase) inhibitor | An EC 3.1.1.* (carboxylic ester hydrolase) inhibitor that interferes with the action of enzyme acetylcholinesterase (EC 3.1.1.7), which helps breaking down of acetylcholine into choline and acetic acid. |
neuroprotective agent | Any compound that can be used for the treatment of neurodegenerative disorders. |
plant metabolite | Any eukaryotic metabolite produced during a metabolic reaction in plants, the kingdom that include flowering plants, conifers and other gymnosperms. |
nootropic agent | Any compound that improves mental functions such as cognition, memory, intelligence, motivation, attention, and concentration. |
[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] |
Class | Description |
---|---|
quinolone | |
sesquiterpene alkaloid | |
pyridone | |
primary amino compound | A compound formally derived from ammonia by replacing one hydrogen atom by an organyl group. |
organic heterotricyclic compound | An organic tricyclic compound in which at least one of the rings of the tricyclic skeleton contains one or more heteroatoms. |
[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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
EWS/FLI fusion protein | Homo sapiens (human) | Potency | 15.0321 | 0.0013 | 10.1577 | 42.8575 | AID1259253; AID1259255; AID1259256 |
acetylcholinesterase | Homo sapiens (human) | Potency | 0.3647 | 0.0025 | 41.7960 | 15,848.9004 | AID1347395; AID1347397; AID1347398; AID1347399 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Acetylcholinesterase | Tetronarce californica (Pacific electric ray) | Ki | 1.1743 | 0.0000 | 0.7671 | 4.3000 | AID1796454; AID1796488 |
Cholinesterase | Homo sapiens (human) | IC50 (µMol) | 4.4288 | 0.0000 | 1.5599 | 10.0000 | AID1796478; AID1796482; AID1796572; AID1801945 |
Cholinesterase | Homo sapiens (human) | Ki | 0.5235 | 0.0000 | 1.5173 | 9.7300 | AID1796481 |
Acetylcholinesterase | Mus musculus (house mouse) | Ki | 0.0046 | 0.0000 | 1.4282 | 9.3000 | AID1800423 |
Acetylcholinesterase | Homo sapiens (human) | IC50 (µMol) | 4.4288 | 0.0000 | 0.9332 | 10.0000 | AID1796478; AID1796482; AID1796572; AID1801945 |
Acetylcholinesterase | Homo sapiens (human) | Ki | 0.3505 | 0.0000 | 1.2786 | 9.7300 | AID1796481; AID1800423 |
Acetylcholinesterase | Rattus norvegicus (Norway rat) | IC50 (µMol) | 35.1362 | 0.0002 | 0.5259 | 7.2000 | AID1796569 |
Acetylcholinesterase | Rattus norvegicus (Norway rat) | Ki | 0.1110 | 0.0002 | 1.6401 | 10.0000 | AID1796454 |
Chain A, Acetylcholinesterase | Tetronarce californica (Pacific electric ray) | Ki | 0.2500 | 0.2500 | 0.2500 | 0.2500 | AID977610 |
Acetylcholinesterase | Electrophorus electricus (electric eel) | IC50 (µMol) | 8.0850 | 0.0000 | 0.9453 | 9.9400 | AID1666849; AID1781505 |
Cholinesterase | Homo sapiens (human) | IC50 (µMol) | 5,050.0000 | 0.0000 | 1.5599 | 10.0000 | AID1537270; AID1862259 |
Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 0.1200 | 0.0001 | 1.7536 | 10.0000 | AID1495954 |
Acetylcholinesterase | Homo sapiens (human) | IC50 (µMol) | 2.1226 | 0.0000 | 0.9332 | 10.0000 | AID1273850; AID1386641; AID1537269; AID1639003; AID1862258 |
Acetylcholinesterase | Bos taurus (cattle) | IC50 (µMol) | 0.1000 | 0.0000 | 0.6106 | 8.7000 | AID1697408 |
Cholinesterase | Canis lupus familiaris (dog) | IC50 (µMol) | 10,000.0000 | 6.2700 | 6.2700 | 6.2700 | AID1666848 |
Acetylcholinesterase | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0955 | 0.0002 | 0.5259 | 7.2000 | AID1319286; AID1347958; AID1495954; AID1682335 |
Carboxylic ester hydrolase | Rattus norvegicus (Norway rat) | IC50 (µMol) | 49.0767 | 0.0004 | 1.4811 | 9.8700 | AID1347959; AID1495955; AID1682163 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Acetylcholinesterase | Homo sapiens (human) | Kd | 0.0170 | 0.0080 | 1.7750 | 5.3000 | AID1756683 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1796569 | Enzyme Inhibition Assay from Article 10.1021/jm0496178: \\Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.\\ | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3 | Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors. |
AID1796454 | Enzyme Inhibition Assay from Article 10.1021/ja021111w: \\Acetylcholinesterase complexed with bivalent ligands related to huperzine a: experimental evidence for species-dependent protein-ligand complementarity.\\ | 2003 | Journal of the American Chemical Society, Jan-15, Volume: 125, Issue:2 | Acetylcholinesterase complexed with bivalent ligands related to huperzine a: experimental evidence for species-dependent protein-ligand complementarity. |
AID1796482 | Cholinesterase Inhibition Assay from Article 10.1021/jm050578p: \\Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.\\ | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine. |
AID1800423 | Assay of Substrate Hydrolysis from Article 10.1021/bi401043w: \\The natural product dihydrotanshinone I provides a prototype for uncharged inhibitors that bind specifically to the acetylcholinesterase peripheral site with nanomolar affinity.\\ | 2013 | Biochemistry, Oct-22, Volume: 52, Issue:42 | The natural product dihydrotanshinone I provides a prototype for uncharged inhibitors that bind specifically to the acetylcholinesterase peripheral site with nanomolar affinity. |
AID1796478 | Enzyme Inhibition Assay from Article 10.1021/jm0496741: \\Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors.\\ | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors. |
AID1796488 | Enzyme Inhibition Assay from Article 10.1021/bi020151+: \\X-ray structures of Torpedo californica acetylcholinesterase complexed with (+)-huperzine A and (-)-huperzine B: structural evidence for an active site rearrangement.\\ | 2002 | Biochemistry, Sep-03, Volume: 41, Issue:35 | X-ray structures of Torpedo californica acetylcholinesterase complexed with (+)-huperzine A and (-)-huperzine B: structural evidence for an active site rearrangement. |
AID1796572 | Cholinesterase Inhibition Assay from Article 10.1021/jm010491d: \\Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.\\ | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17 | Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines. |
AID1796481 | Enzyme Inhibition Assay from Article 10.1021/jm060257t: \\Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites.\\ | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11 | Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites. |
AID1801945 | AChE and BuChE Inhibition Assay from Article 10.1016/j.bioorg.2016.07.013: \\Design, synthesis and biological evaluation of coumarin derivatives as novel acetylcholinesterase inhibitors that attenuate H2O2-induced apoptosis in SH-SY5Y cells.\\ | 2016 | Bioorganic chemistry, 10, Volume: 68 | Design, synthesis and biological evaluation of coumarin derivatives as novel acetylcholinesterase inhibitors that attenuate H2O2-induced apoptosis in SH-SY5Y cells. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
AID1537271 | Selectivity index, ratio of IC50 for human BuChE to IC50 for human AChE | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease. |
AID1682151 | Neuroprotective activity against Bay-K8644-induced calcium mobilization in rat forebrain derived neurons assessed as calcium elevation at 100 nM (Rvb = 521 nM) | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
AID1756684 | Binding affinity to CM5 sensor chip immobilized recombinant human AChE assessed as on rate constant at 298.15 K by surface plasmon resonance assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate. |
AID1682157 | In vivo inhibition of acetylcholinesterase in rat at 0.066 micromol/kg, icv relative to control | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
AID1537276 | Inhibition of GSK3B (unknown origin) at 10 uM relative to control | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease. |
AID1682152 | Neuroprotective activity against glutamate-induced calcium mobilization in rat forebrain derived neurons assessed as calcium elevation at 100 nM (Rvb = 811 nM) | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
AID1347960 | Selectivity index, ratio of IC50 for BuChE in rat serum to IC50 for AChE in rat cortex homogenate | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
AID1319289 | Selectivity index, ratio of IC50 for rat serum BuChE to IC50 for rat cortex AChE | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18 | Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents. |
AID1666848 | Inhibition of dog serum BChE using butrylthiocholine iodide as substrate by spectrophotometry based Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 30, Issue:6 | Design, synthesis and evaluation of new 4-arylthiazole-2-amine derivatives as acetylcholinesterase inhibitors. |
AID1682148 | Neuroprotective activity against NMDA-induced cell death in rat neurons assessed as cell survival pretreated for 45 mins followed by NMDA stimulation and measured after 30 mins by MTT assay (Rvb = 35%) | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
AID1682158 | Potency index, ratio of in vivo inhibition of acetylcholinesterase in Sprague-Dawley rat cortex by tacrine to in vivo inhibition of acetylcholinesterase in Sprague-Dawley rat cortex by compound | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
AID1862259 | Inhibition of BuChE (unknown origin) using butyrylthiocholine iodide as substrate by DTNB reagent based Ellman's method | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and evaluation of 2-(2-oxoethyl)pyrimidine-5-carboxamide derivatives as acetylcholinesterase inhibitors. |
AID1495953 | Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment. |
AID1386641 | Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by Ellman's method | 2018 | Journal of natural products, 09-28, Volume: 81, Issue:9 | Colocynthenins A-D, Ring-A seco-Cucurbitane Triterpenoids from the Fruits of Citrullus colocynthis. |
AID1682162 | In vivo inhibition of acetylcholinesterase in Sprague-Dawley rat cortex at 1 micromol/kg, IG administered once daily for 8 days and measured 30 mins post 8th dose by spectrophotometric method relative to control | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
AID1862258 | Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate by DTNB reagent based Ellman's method | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Design, synthesis and evaluation of 2-(2-oxoethyl)pyrimidine-5-carboxamide derivatives as acetylcholinesterase inhibitors. |
AID1273850 | Inhibition of human acetylcholinesterase after 30 mins by microplate reader-based Ellman's method | 2015 | Journal of natural products, Dec-24, Volume: 78, Issue:12 | Avertoxins A-D, Prenyl Asteltoxin Derivatives from Aspergillus versicolor Y10, an Endophytic Fungus of Huperzia serrata. |
AID1319304 | Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability at 100 uM measured after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18 | Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents. |
AID1682150 | Displacement of [3H]MK-801 from Guinea pig synaptosomal plasma membrane NMDA receptor | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
AID1682156 | Potency index, ratio of in vivo inhibition of acetylcholinesterase in rat by tacrine to in vivo inhibition of acetylcholinesterase in Sprague-Dawley rat cortex by compound | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
AID1756683 | Binding affinity to CM5 sensor chip immobilized recombinant human AChE assessed as dissociation constant at 298.15 K by surface plasmon resonance assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate. |
AID1756685 | Binding affinity to CM5 sensor chip immobilized recombinant human AChE assessed as off rate constant at 298.15 K by surface plasmon resonance assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4 | Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate. |
AID1666849 | Inhibition of Electric eel AChE using acetylcholine iodide as substrate by spectrophotometry based Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 30, Issue:6 | Design, synthesis and evaluation of new 4-arylthiazole-2-amine derivatives as acetylcholinesterase inhibitors. |
AID1682153 | Neuroprotective activity against glutamate-induced cell death in rat forebrain derived neurons assessed as neuron death at 100 nM incubated for 45 mins (Rvb = 55%) | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
AID1537269 | Inhibition of human AChE using acetylthiocholine iodide as substrate measured for 1 min by Ellman's method | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease. |
AID1319287 | Inhibition of rat serum BuChE using butyrylthiocholine as substrate measured after 20 mins by Ellman's method | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18 | Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents. |
AID1319286 | Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate measured after 20 mins by Ellman's method | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18 | Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents. |
AID1781504 | Inhibition of equine serum BuChE at 100 uM using butylthiocholine chloride as substrate incubated for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | 2021 | Journal of natural products, 08-27, Volume: 84, Issue:8 | Pd-Catalyzed Direct Diversification of Natural Anti-Alzheimer's Disease Drug: Synthesis and Biological Evaluation of |
AID1697408 | Inhibition of bovine erythrocytes AChE using acetylthiocholine iodide as substrate incubated for 15 to 20 mins by Ellman's methods | |||
AID1682146 | Toxicity in male rat | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
AID1537277 | Permeability of the compound after 2.45 hrs by PAMPA | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease. |
AID1682163 | Inhibition of rat cortex homogenate BuChE by spectrophotometric method | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
AID1347958 | Inhibition of AChE in rat cortex homogenate using acetylthiocholine iodide as substrate after 20 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
AID1639003 | Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate after 5 mins by spectrophotometric analysis | 2019 | Journal of natural products, 04-26, Volume: 82, Issue:4 | Bialternacins A-F, Aromatic Polyketide Dimers from an Endophytic Alternaria sp. |
AID1781505 | Inhibition of electric eel AChE using acetylthiocholine chloride as a substrate incubated for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method | 2021 | Journal of natural products, 08-27, Volume: 84, Issue:8 | Pd-Catalyzed Direct Diversification of Natural Anti-Alzheimer's Disease Drug: Synthesis and Biological Evaluation of |
AID1495955 | Inhibition of rat serum BChE using butyrylthiocholine iodide as substrate after 20 mins by by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment. |
AID1300690 | Inhibition of ACAT in human monocyte derived macrophages assessed as reduction in foam cell formation by measuring acetyl LDL-induced cholesterol ester accumulation at 30 uM after 24 hrs in presence of cholesteryl-[3H]oleate | 2016 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11 | Serralongamines B-D, three new Lycopodium alkaloids from Lycopodium serratum var. longipetiolatum, and their inhibitory effects on foam cell formation in macrophages. |
AID1682147 | Toxicity in female rat | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
AID1319290 | Antioxidant activity assessed as trolox equivalent of AAPH radical scavenging activity preincubated for 10 mins followed by AAPH challenge measured every min for 180 mins by ORAC-FL assay | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18 | Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents. |
AID1682149 | Displacement of [3H]TCP from NMDA receptor in Guinea pig synaptosomal plasma membrane | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
AID1682335 | Inhibition of rat cortex homogenate acetylcholinesterase by spectrophotometric method | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
AID1319303 | Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability at 10 and 30 uM measured after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18 | Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents. |
AID1495954 | Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate after 20 mins by by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment. |
AID1347959 | Inhibition of BuChE in rat serum using butyrylthiocholine iodide as substrate after 20 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
AID1537270 | Inhibition of human BuChE using butyrylthiocholine iodide as substrate measured for 1 min by Ellman's method | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease. |
AID1682159 | Potency index, ratio of in vivo inhibition of acetylcholinesterase in Sprague-Dawley rat cortex by donepezil to in vivo inhibition of acetylcholinesterase in Sprague-Dawley rat cortex by compound | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The 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. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS 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. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The 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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 1997 | Nature structural biology, Jan, Volume: 4, Issue:1 | Structure of acetylcholinesterase complexed with the nootropic alkaloid, (-)-huperzine A. |
AID1811 | Experimentally measured binding affinity data derived from PDB | 1997 | Nature structural biology, Jan, Volume: 4, Issue:1 | Structure of acetylcholinesterase complexed with the nootropic alkaloid, (-)-huperzine A. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 12 (2.54) | 18.7374 |
1990's | 57 (12.08) | 18.2507 |
2000's | 182 (38.56) | 29.6817 |
2010's | 160 (33.90) | 24.3611 |
2020's | 61 (12.92) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (50.20) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 15 (3.21%) | 5.53% |
Trials | 0 (0.00%) | 5.53% |
Reviews | 58 (12.39%) | 6.00% |
Reviews | 1 (4.17%) | 6.00% |
Case Studies | 2 (0.43%) | 4.05% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Observational | 0 (0.00%) | 0.25% |
Other | 393 (83.97%) | 84.16% |
Other | 23 (95.83%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
Evaluation of Three Potential CNS Pretreatments for Soman Exposure - Huperzine A, Donepezil, and Galantamine - on Human Performance [NCT01194336] | 84 participants (Actual) | Observational | 2012-02-29 | Completed | |||
Effects of Huperzine A on Presbycusis-related Subjective Tinnitus and Cognitive Impairment [NCT03101722] | 60 participants (Anticipated) | Interventional | 2017-05-15 | Enrolling by invitation | |||
An Open-label, Three-period, Crossover Study in Healthy Volunteers to Evaluate the Relative Bioavailability of Two Different Release Rate Controlled Release Formulations of Huperzine A (0.4mg)Compared to the Equivalent Dose of an Immediate Release Formula [NCT01136551] | 8 participants (Anticipated) | Interventional | 2010-09-30 | Not yet recruiting | |||
A Multi-Center, Randomized, Double-Blind, Double-Dummy, Placebo- and Active-Controlled, Study to Evaluate the Safety and Efficacy of Huperzine A Sustained-Release Tablets in Patients With Mild to Moderate Alzheimer's Disease [NCT01282619] | Phase 2/Phase 3 | 390 participants (Anticipated) | Interventional | 2010-05-31 | Recruiting | ||
Huperzine for Cognitive and Functional Impairment in Schizophrenia [NCT00963846] | Phase 2 | 56 participants (Actual) | Interventional | 2010-03-31 | Completed | ||
Huperzine-A for Cognitive Dysfunction and Functional Status in Schizophrenia [NCT01012830] | Phase 4 | 15 participants (Anticipated) | Interventional | 2009-12-31 | Not yet recruiting | ||
Rivastigmine and Huperzine A as Treatments for Cocaine Dependence [NCT01030692] | Phase 1 | 72 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
Early Diagnosis and Early Treatment of Alzheimer's Disease Based on Senile Plaque Imaging [NCT02931136] | Phase 4 | 300 participants (Anticipated) | Interventional | 2019-11-30 | Not yet recruiting | ||
A Multi-center, Randomized, Double-blinded, Placebo-controlled Study of Huperzine A Injection in Reducing Postoperative Delirium in Elderly Patients Undergoing Non-cardiac Surgery [NCT05242419] | 40 participants (Anticipated) | Interventional | 2022-06-10 | Recruiting | |||
Effect of Huperzine A on Cognitive Function and Perception of Effort During Exercise [NCT03445104] | Early Phase 1 | 15 participants (Actual) | Interventional | 2018-01-16 | Completed | ||
Brain Single Photon Emission Computed Tomography and Quantitative Electroencephalography In Former NFL Players: A Single-Site Exploratory Pilot Study [NCT01515839] | 100 participants (Actual) | Interventional | 2009-05-31 | Completed | |||
A Multi-Center, Double-Blind, Placebo-Controlled Therapeutic Trial to Determine Whether Natural Huperzine A Improves Cognitive Function [NCT00083590] | Phase 2 | 150 participants (Anticipated) | Interventional | 2004-04-30 | Completed | ||
The Effect of Huperzine A Injection on Postoperative Cognitive Dysfunction in Patients With Aneurysmal Subarachnoid Hemorrhage: a Pilot Study [NCT05560373] | Phase 4 | 60 participants (Anticipated) | Interventional | 2022-09-30 | Not yet recruiting | ||
Evaluation of Safety and Efficacy of BIS-001-ER for the Treatment of Adult Focal Impaired Awareness Seizures [NCT03474770] | Phase 1/Phase 2 | 16 participants (Anticipated) | Interventional | 2018-04-10 | Active, not recruiting | ||
RENAISSANCE Study: A Phase 2, Multicenter, Open Label Safety and Tolerability Study of SPN-817 in Adult Patients With Treatment Resistant Epilepsy [NCT05518578] | Phase 2 | 35 participants (Anticipated) | Interventional | 2023-02-07 | Recruiting | ||
Huperzine A for the Treatment of Cognitive, Mood, and Functional Deficits After Moderate and Severe TBI [NCT01676311] | Phase 2 | 14 participants (Actual) | Interventional | 2013-12-31 | Terminated(stopped due to Insufficient accrual rate: 14 participants enrolled (target of 30).) | ||
A Single-Center, Randomized, Open-label, Multiple-Dose, Single-Sequence Crossover Study, Evaluating the Safety and Relative Bioavailability of Three SPN-817 Treatments (A, B and C) in Healthy Adult Subjects [NCT05102552] | Early Phase 1 | 30 participants (Actual) | Interventional | 2021-10-19 | Completed | ||
Evaluation of the Bioavailability, Safety, and Tolerability of BIS-001 ER Following Multiple Dose Administration in Healthy Subjects [NCT03156439] | Phase 1 | 8 participants (Actual) | Interventional | 2017-05-22 | Completed | ||
A Randomized, Controlled, Single-center Clinical Study of Huperzine A in the Treatment of Brain Injury in Patients With Hypertensive Cerebral Hemorrhage [NCT04509323] | Phase 4 | 20 participants (Anticipated) | Interventional | 2020-08-03 | Not yet recruiting | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |