Velnacrine is a centrally acting, highly selective, and reversible inhibitor of acetylcholinesterase (AChE) that was investigated as a potential treatment for Alzheimer's disease. It is a synthetic compound that differs structurally from other known cholinesterase inhibitors and has a high affinity for AChE. Studies have shown that velnacrine improves cognitive function in patients with Alzheimer's disease. However, velnacrine was ultimately withdrawn from clinical trials due to hepatotoxicity concerns. Despite this, the compound remains of interest for research into the treatment of neurodegenerative diseases, as it provides insights into the role of AChE in cognitive function and the potential of AChE inhibitors as therapeutic agents.'
velnacrine: RN given refers to (+-)-isomer; RN for cpd without isomeric designation not available 8/88; structure in first source; potential Alzheimer's disease drug but trial halted due to abnormal liver tests [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 3655 |
| CHEMBL ID | 51934 |
| CHEBI ID | 91990 |
| SCHEMBL ID | 194467 |
| MeSH ID | M0158246 |
| Synonym |
|---|
| BRD-A98299281-050-04-7 |
| DIVK1C_000577 |
| KBIO1_000577 |
| SPECTRUM_000073 |
| OPREA1_439874 |
| IDI1_000577 |
| SPECTRUM5_001267 |
| AB00053578 |
| (2z)-but-2-enedioic acid; 9-amino-1,2,3,4-tetrahydroacridin-1-ol |
| 9-amino-1 ,2,3,4-tetrahydroacridin-1-ol deriv. 1a |
| chembl51934 , |
| bdbm9347 |
| BSPBIO_003296 |
| NCGC00162194-02 |
| 1-hydroxytacrine |
| velnacrine |
| 9-amino-1,2,3,4-tetrahydroacridin-1-ol |
| 1-acridinol, 9-amino-1,2,3,4-tetrahydro- |
| velnacrine [inn:ban] |
| KBIO3_002516 |
| KBIO2_005609 |
| KBIO2_003041 |
| KBIOSS_000473 |
| KBIO2_000473 |
| KBIOGR_001329 |
| SPECTRUM2_001215 |
| SPBIO_001030 |
| SPECTRUM4_000815 |
| NINDS_000577 |
| SPECTRUM3_001708 |
| BSPBIO_000496 |
| BPBIO1_000546 |
| LOPAC0_000584 |
| PRESTWICK3_000448 |
| NCGC00162194-01 |
| 104675-29-8 |
| HMS2089F15 |
| NCGC00015506-04 |
| 1-oh-tha |
| 124027-47-0 |
| AKOS001642124 |
| (+-)-9-amino-1,2,3,4-tetrahydroacridin-1-ol |
| unii-y2p6nv151k |
| y2p6nv151k , |
| CCG-204673 |
| NCGC00015506-05 |
| NCGC00015506-02 |
| SCHEMBL194467 |
| velnacrine [who-dd] |
| (+/-)-9-amino-1,2,3,4-tetrahydro-1-acridinol |
| velnacrine [inn] |
| 1-acridinol, 9-amino-1,2,3,4-tetrahydro-, (+/-)- |
| velnacrine [mi] |
| 9-amino-1,2,3,4-tetrahydroacridin-1ol |
| 9-amino-1,2,3,4-tetrahydroacridine-1-ol |
| AB00053578-05 |
| DTXSID4046945 |
| 1-hydroxy-tacrine |
| OQL6V4U301 , |
| 1-acridinol, 9-amino-1,2,3,4-tetrahydro-, (-)- |
| 121445-24-7 |
| velnacrine, (-)- |
| velnacrine, (+)- |
| 121445-26-9 |
| JFN3Z63E2C , |
| 1-acridinol, 9-amino-1,2,3,4-tetrahydro-, (+)- |
| unii-oql6v4u301 |
| unii-jfn3z63e2c |
| 9-imino-1,2,3,4,9,10-hexahydroacridin-1-ol |
| CHEBI:91990 |
| 9-amino-1,2,3,4-tetrahydro-1-acridinol, aldrichcpr |
| DS-9716 |
| Q27163788 |
| BRD-A98299281-050-09-6 |
| SDCCGSBI-0050566.P003 |
| I11848 |
| ZEA02747 |
| 1-acridinol, 9-amino-1,2,3,4-tetrahydro-, (a+/-)- |
Velnacrine maleate is a novel, orally active acetylcholinesterase inhibitor of the acridine class with a longer duration of action than physostigmine. Velnacrine has been considered for use in the treatment of Alzheimer's disease.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Velnacrine maleate is a well-known AChE inhibitor which plays a competitive role by decreasing NO-mediated erythrocyte responses." | ( Non-neuronal cholinergic system and signal transduction pathways mediated by band 3 in red blood cells. Almeida, JP; Carvalho, FA; Fernandes, IO; Freitas-Santos, T; Saldanha, C, 2008) | 1.07 |
| "Velnacrine is a derivative of tacrine." | ( Velnacrine for Alzheimer's disease. Birks, J; Wilcock, GG, 2004) | 2.49 |
| "Velnacrine maleate is a novel, orally active acetylcholinesterase inhibitor of the acridine class with a longer duration of action than physostigmine. " | ( Velnacrine maleate improves delayed matching performance by aged monkeys. Buccafusco, JJ; Jackson, WJ; Rush, DK; Terry, AV; Turk, DJ, 1995) | 3.18 |
| "Velnacrine is a centrally acting anticholinesterase which has been considered for use in the treatment of Alzheimer's disease. " | ( The effect of velnacrine on the mixed function oxidase system. Danbury, TC; Eccles, MJ; Ford, JM; Roberts, CJ, ) | 1.93 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Velnacrine has shown efficacy in the treatment of Alzheimer's disease and in improving both normal and experimentally impaired mnemonic function in animals and humans." | ( Velnacrine maleate improves delayed matching performance by aged monkeys. Buccafusco, JJ; Jackson, WJ; Rush, DK; Terry, AV; Turk, DJ, 1995) | 2.46 |
Clinical trials with tacrine (THA) and its principal (1-OH) metabolite (velnacrine) for the treatment of Alzheimer's disease have been hampered by adverse hepatic events that were undetected in preclinical studies.
| Excerpt | Reference | Relevance |
|---|---|---|
| " To assess adverse events in relation to dosage and plasma drug levels, 24 hospitalized AD subjects were randomly assigned to receive placebo or HP 029 for 10 days in a double-blind, sequential escalation study." | ( Clinical safety, tolerance, and plasma levels of the oral anticholinesterase 1,2,3,4-tetrahydro-9-aminoacridin-1-oL-maleate (HP 029) in Alzheimer's disease: preliminary findings. Cutler, NR; De Luna, DM; Murphy, MF; Nash, RJ; Prior, PL, 1990) | 0.28 |
| " Treatment-related adverse clinical events occurred in 36%, 28%, and 30% of patients in the groups that received placebo, velnacrine maleate (150 mg), and velnacrine maleate (225 mg), respectively." | ( Effectiveness and safety of velnacrine for the treatment of Alzheimer's disease. A double-blind, placebo-controlled study. Mentane Study Group. Antuono, PG, 1995) | 0.79 |
| " Direct liver injury, possibly associated with the production of a toxic metabolite, would be consistent with reports of aberrant xenobiotic metabolism in Alzheimer's disease patients." | ( Clinical trials with velnacrine: (PROPP) the physician reference of predicted probabilities--a statistical model for the estimation of hepatotoxicity risk with velnacrine maleate. Hardiman, S; Miller, K; Murphy, M, 1993) | 0.6 |
| "Clinical trials with tacrine (THA) and its principal (1-OH) metabolite (velnacrine) for the treatment of Alzheimer's disease have been hampered by adverse hepatic events that were undetected in preclinical studies." | ( Cytotoxicity of tacrine and velnacrine metabolites in cultured rat, dog and human hepatocytes. Curren, RD; Viau, CJ; Wallace, K, 1993) | 0.81 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Blood and urine samples were collected for the pharmacokinetic assessment." | ( Multiple dose pharmacokinetics, safety, and tolerance of velnacrine (HP 029) in healthy elderly subjects: a potential therapeutic agent for Alzheimer's disease. Ho, I; Hsu, R; Lassman, HB; Puri, SK, 1990) | 0.52 |
| " Pharmacokinetic study demonstrated that tacrine could be quickly absorbed and extensively metabolized to its monohydroxylated metabolites in vivo." | ( Pharmacokinetics and brain dispositions of tacrine and its major bioactive monohydroxylated metabolites in rats. Qian, S; Wo, SK; Zuo, Z, 2012) | 0.38 |
24 healthy, elderly men were given 100 mg of velnacrine on two different study days. Drug-related material was well absorbed in all three species. The majority of the dose recovered in the urine.
| Excerpt | Reference | Relevance |
|---|---|---|
| " In this open, randomized, crossover study, 24 healthy, elderly men were given 100 mg of velnacrine on two different study days to assess the influence of food on the bioavailability of velnacrine." | ( The effect of food on the bioavailability of velnacrine (HP 029) in healthy elderly men: a potential Alzheimer agent. Ho, I; Hsu, RS; Lassman, HB; Puri, SK, 1989) | 0.76 |
| " Following oral administration of [14C]velnacrine maleate, drug-related material was well absorbed in all three species, with the majority of the dose recovered in the urine." | ( Disposition of [14C]velnacrine maleate in rats, dogs, and humans. Coe, RA; Gilbert, PJ; Hartley, TE; Hillbeck, D; Troke, JA; Turcan, RG; Vose, CW, ) | 0.72 |
| "The mechanism associated with the increased bioavailability of tacrine as a result of a 24-h period of fasting was examined in rats." | ( Mechanism for increased bioavailability of tacrine in fasted rats. Ahn, SH; Chung, SJ; Hong, SS; Li, H; Park, BS; Park, CH; Seo, SY; Sung, JH, 2006) | 0.33 |
A velnacrine dosage of 300 mg/d that was tolerated in healthy elderly subjects was not tolerated by AD patients.
| Class | Description |
|---|---|
| acridines | |
| [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) |
|---|---|---|---|---|---|---|---|
| GLS protein | Homo sapiens (human) | Potency | 3.1623 | 0.3548 | 7.9355 | 39.8107 | AID624146 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 35.4813 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 31.6228 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 0.5012 | 1.0000 | 10.4756 | 28.1838 | AID1457 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 42.5615 | 0.0601 | 10.7453 | 37.9330 | AID485368 |
| [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 | Mus musculus (house mouse) | IC50 (µMol) | 1.0000 | 0.0007 | 1.1181 | 8.4000 | AID31783 |
| Acetylcholinesterase | Homo sapiens (human) | IC50 (µMol) | 0.8280 | 0.0000 | 0.9332 | 10.0000 | AID30659; AID31495 |
| Sodium-dependent dopamine transporter | Rattus norvegicus (Norway rat) | IC50 (µMol) | 20.0000 | 0.0007 | 0.9774 | 9.7000 | AID181678 |
| Sodium-dependent serotonin transporter | Rattus norvegicus (Norway rat) | IC50 (µMol) | 20.0000 | 0.0003 | 0.8197 | 8.4900 | AID181681 |
| Acetylcholinesterase | Rattus norvegicus (Norway rat) | IC50 (µMol) | 2.7870 | 0.0002 | 0.5259 | 7.2000 | AID1796315; AID31962; AID31965 |
| Transporter | Rattus norvegicus (Norway rat) | IC50 (µMol) | 20.0000 | 0.0008 | 1.9562 | 8.8000 | AID181678; AID181680 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| amyloid-beta binding | Acetylcholinesterase | Homo sapiens (human) |
| acetylcholinesterase activity | Acetylcholinesterase | Homo sapiens (human) |
| cholinesterase activity | Acetylcholinesterase | Homo sapiens (human) |
| protein binding | Acetylcholinesterase | Homo sapiens (human) |
| collagen binding | Acetylcholinesterase | Homo sapiens (human) |
| hydrolase activity | Acetylcholinesterase | Homo sapiens (human) |
| serine hydrolase activity | Acetylcholinesterase | Homo sapiens (human) |
| acetylcholine binding | Acetylcholinesterase | Homo sapiens (human) |
| protein homodimerization activity | Acetylcholinesterase | Homo sapiens (human) |
| laminin binding | Acetylcholinesterase | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| extracellular region | Acetylcholinesterase | Homo sapiens (human) |
| basement membrane | Acetylcholinesterase | Homo sapiens (human) |
| extracellular space | Acetylcholinesterase | Homo sapiens (human) |
| nucleus | Acetylcholinesterase | Homo sapiens (human) |
| Golgi apparatus | Acetylcholinesterase | Homo sapiens (human) |
| plasma membrane | Acetylcholinesterase | Homo sapiens (human) |
| cell surface | Acetylcholinesterase | Homo sapiens (human) |
| membrane | Acetylcholinesterase | Homo sapiens (human) |
| neuromuscular junction | Acetylcholinesterase | Homo sapiens (human) |
| synaptic cleft | Acetylcholinesterase | Homo sapiens (human) |
| synapse | Acetylcholinesterase | Homo sapiens (human) |
| perinuclear region of cytoplasm | Acetylcholinesterase | Homo sapiens (human) |
| side of membrane | Acetylcholinesterase | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1796315 | Enzyme Inhibition Assay from Article 10.1021/jm00128a024: \\9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics.\\ | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID111986 | Reversal of scopolamine-induced memory impairment in mice at 2.5 mg/Kg administered subcutaneously. | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
| AID184799 | Toxicity was evaluated in rats, after intraperitoneal administration;Value ranges from (40-80). | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID30659 | Inhibition of Acetylcholinesterase in monkey red blood cell | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | Identification of a 3-hydroxylated tacrine metabolite in rat and man: metabolic profiling implications and pharmacology. |
| AID111985 | Reversal of scopolamine-induced memory impairment in mice at 1.25 mg/Kg administered subcutaneously. | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
| AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
| AID31783 | Inhibition of Acetylcholinesterase in mouse red blood cell | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | Identification of a 3-hydroxylated tacrine metabolite in rat and man: metabolic profiling implications and pharmacology. |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID31962 | In vitro inhibition against acetylcholinesterase in rat striata. | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID111982 | Reversal of scopolamine-induced memory impairment in mice at 0.16 mg/Kg administered subcutaneously. | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID111987 | Reversal of scopolamine-induced memory impairment in mice at 5 mg/Kg administered subcutaneously. | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID181680 | Inhibition of norepinephrine reuptake in rat whole brains minus cerebellar | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID31965 | Inhibition of Acetylcholinesterase in rat red blood cell | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | Identification of a 3-hydroxylated tacrine metabolite in rat and man: metabolic profiling implications and pharmacology. |
| AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
| AID117242 | Toxicity was evaluated in mice, after intraperitoneal administration | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID111983 | Reversal of scopolamine-induced memory impairment in mice at 0.31 mg/Kg administered subcutaneously. | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID31495 | Inhibition of Acetylcholinesterase in human red blood cell | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | Identification of a 3-hydroxylated tacrine metabolite in rat and man: metabolic profiling implications and pharmacology. |
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
| AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
| AID181678 | Inhibition of the reuptake of dopamine in rat corpora striata. | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID181681 | Inhibition of serotonin reuptake in rat whole brains without cerebellum | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID111984 | Reversal of scopolamine-induced memory impairment in mice at 0.63 mg/Kg administered subcutaneously. | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
| AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
| AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| 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. |
| AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 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. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| 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. |
| AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC 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. |
| AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| 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. |
| AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| 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. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| AID493017 | Wombat Data for BeliefDocking | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | Identification of a 3-hydroxylated tacrine metabolite in rat and man: metabolic profiling implications and pharmacology. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 7 (10.61) | 18.7374 |
| 1990's | 35 (53.03) | 18.2507 |
| 2000's | 11 (16.67) | 29.6817 |
| 2010's | 8 (12.12) | 24.3611 |
| 2020's | 5 (7.58) | 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 moderate demand-to-supply ratio for research on this compound.
| This Compound (18.06) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 20 (27.40%) | 5.53% |
| Reviews | 3 (4.11%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 50 (68.49%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||