GYKI 52466: an AMPA (non-NMDA) receptor antagonist; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 3538 |
| CHEMBL ID | 275006 |
| CHEBI ID | 79560 |
| SCHEMBL ID | 194854 |
| MeSH ID | M0171631 |
| Synonym |
|---|
| bdbm50048389 |
| 4-(8-methyl-9h-1,3-dioxa-6,7-diaza-cyclohepta[f]inden-5-yl)-phenylamine (gyki 52466) |
| 4-(8-methyl-9h-1,3-dioxa-6,7-diaza-cyclohepta[f]inden-5-yl)-phenylamine |
| BRD-K24240364-003-02-1 |
| gyki-52466 |
| benzenamine, 4-(8-methyl-9h-1,3-dioxolo(4,5-h)(2,3)benzodiazepin-5-yl)- |
| 1-(p-aminophenyl)-4-methyl-7,8-methylenedioxy-5h-2,3-benzodiazepine hydrochloride |
| 4-(8-methyl-9h-1,3-dioxolo(4,5-h)(2,3)benzodiazepin-5-yl)benzenamine |
| tocris-1454 |
| NCGC00025169-01 |
| NCGC00015463-01 |
| lopac-g-119 |
| PDSP2_001826 |
| 102771-26-6 |
| gyki 52466 |
| 4-(8-methyl-9h-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-yl)benzenamine |
| gyki52466 |
| LOPAC0_000631 |
| PDSP1_001843 |
| NCGC00025169-02 |
| NCGC00015463-04 |
| CHEMBL275006 , |
| chebi:79560 , |
| 4-(8-methyl-9h-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-5-yl)aniline |
| CCG-204719 |
| NCGC00015463-03 |
| NCGC00015463-02 |
| BCP9000756 |
| 471v8nz5x3 , |
| unii-471v8nz5x3 |
| gtpl4210 |
| 4-{13-methyl-4,6-dioxa-11,12-diazatricyclo[7.5.0.0^{3,7}]tetradeca-1(9),2,7,10,12-pentaen-10-yl}aniline |
| gyki53784 |
| gyki-2466 |
| SCHEMBL194854 |
| gyki 52466 hcl |
| 1-(4-aminophenyl)-4-methyl-7,8 -methylenedioxy-5h-2,3-benzodiazepine |
| LFBZZHVSGAHQPP-UHFFFAOYSA-N , |
| 4-(8-methyl-9h-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-yl)-benzenamine hydrochloride |
| HB0311 |
| c17h15n3o2.hcl |
| 4-(8-methyl-9h-[1,3]dioxolo[4',5':4,5]benzo[1,2-d][1,2]diazepin-5-yl)aniline |
| DTXSID40145500 |
| HY-103234 |
| AKOS030582785 |
| FT-0729241 |
| Q5515088 |
| BCP02050 |
| SDCCGSBI-0050612.P002 |
| NCGC00015463-08 |
| benzenamine, 4-(8-methyl-9h-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-yl)- |
| CS-0025672 |
GYKI 52466 is a benzodiazepine derivative that has muscle relaxant and anticonvulsant properties thought to be mediated by highly selective, noncompetitive antagonism of non-NMDA receptors.
| Excerpt | Reference | Relevance |
|---|---|---|
| "1. GYKI 52466 is a benzodiazepine derivative that has muscle relaxant and anticonvulsant properties thought to be mediated by highly selective, noncompetitive antagonism of non-NMDA receptors. " | ( Effects of the non-NMDA antagonists NBQX and the 2,3-benzodiazepine GYKI 52466 on different seizure types in mice: comparison with diazepam and interactions with flumazenil. Hönack, D; Löscher, W, 1994) | 1.15 |
| "GYKI 52466 is a benzodiazepine molecule that has muscle relaxant and anticonvulsant properties not attributable to a gamma-aminobutyric acid receptor-mediated mechanism. " | ( A benzodiazepine recognition site associated with the non-NMDA glutamate receptor. Olney, JW; Price, MT; Yamada, KA; Zorumski, CF, 1993) | 1.73 |
| "GYKI 52466 is a specific antagonist of the neuronal excitation mediated by the non-NMDA type excitatory amino acid receptors, at several sites in the central nervous system. " | ( Inhibition of hippocampal field potentials by GYKI 52466 in vitro and in vivo. Andrási, F; Gaál, L; Molnár, P; Tarnawa, I, 1992) | 1.98 |
GYKI 52466 reduced the increase in escape latency and in swim distance induced by 4VO when given before ischemia but not when applied after.
| Excerpt | Reference | Relevance |
|---|---|---|
| "GYKI 52466 failed to inhibit this increase." | ( Effect of the non-NMDA receptor antagonist GYKI 52466 on the microdialysate and tissue concentrations of amino acids following transient forebrain ischaemia. Arvin, B; Chapman, AG; Graham, JL; Lekieffre, D; Meldrum, BS; Moncada, C, 1994) | 1.27 |
| "GYKI 52466 reduced the increase in escape latency and in swim distance induced by 4VO when given before ischemia but not when applied after ischemia." | ( Pretreatment but not posttreatment with GYKI 52466 reduces functional deficits and neuronal damage after global ischemia in rats. Block, F; Schmitt, W; Schwarz, M, 1996) | 1.28 |
The AMPA-receptors have little if any involvement in the in the mediation of neuropathological alterations in acute convulsions. In GYKI 52466-treated rats serotonin was reduced in the prefrontal cortex and nucleus accumbens while DA metabolism was not affected.
| Excerpt | Reference | Relevance |
|---|---|---|
| "The GYKI 52466-pretreatment did not prevent the astrocyte swelling in the investigated cortical areas; thus we conclude that the AMPA-receptors have little if any involvement in the in the mediation of neuropathological alterations in acute convulsions." | ( Blockade of AMPA-receptors attenuates 4-aminopyridine seizures, decreases the activation of inhibitory neurons but is ineffective against seizure-related astrocytic swelling. Krisztin-Péva, B; Mihály, A; Weiczner, R, 2008) | 0.83 |
| "In GYKI 52466-treated rats serotonin was reduced in the prefrontal cortex and nucleus accumbens while DA metabolism was not affected." | ( Behavioural and neurochemical interactions of the AMPA antagonist GYKI 52466 and the non-competitive NMDA antagonist dizocilpine in rats. Bubser, M; Hauber, W; Tzschentke, T, 1995) | 1.04 |
| "Pretreatment with GYKI 52466 protected rats against behavioural deficits and hippocampal neuronal damage induced by 4VO." | ( Pretreatment but not posttreatment with GYKI 52466 reduces functional deficits and neuronal damage after global ischemia in rats. Block, F; Schmitt, W; Schwarz, M, 1996) | 0.89 |
| "Treatment with GYKI 52466 or LY 231617 reduced the deficit in spatial learning by limiting the increase in swim distance due to ischemia." | ( Correlation between hippocampal neuronal damage and spatial learning deficit due to global ischemia. Block, F; Schwarz, M, 1997) | 0.64 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " In contrast, neither QA up to 5 mM nor trans-ACPD had a significant toxic effect in either KCl group." | ( NMDA and non-NMDA receptor-mediated excitotoxicity are potentiated in cultured striatal neurons by prior chronic depolarization. Chen, Q; Reiner, A; Surmeier, DJ, 1999) | 0.3 |
| " The toxic effect of kainate may be associated with calcium influx, because toxicity was reduced by polyamines that suppress calcium influx and by an inhibitor of calcium phosphatase." | ( A non-excitatory paradigm of glutamate toxicity. Shen, W; Slaughter, MM, 2002) | 0.31 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "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 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " Concomitant treatment with aniracetam (50 nmol/mouse) shifted to the right the dose-response curves and significantly increased the ED50 values for GYKI 52466, 2,3-BZ-2 and 2,3-BZ-2M." | ( GYKI 52466 and related 2,3-benzodiazepines as anticonvulsant agents in DBA/2 mice. Chapman, AG; Chimirri, A; De Sarro, A; de Sarro, G; Gitto, R; Giusti, P; Grasso, S, 1995) | 1.93 |
| " They were found fairly potent in rat tail flick and mouse phenylquinone writhing assays but the dose-response curves were rather shallow as compared to that of morphine." | ( Apparent antinociceptive and anti-inflammatory effects of GYKI 52466. Kedves, R; Máté, I; Székely, JI; Tarnawa, I; Török, K, 1997) | 0.54 |
| " injections at 1-h intervals, the first dosage was given shortly after the intrastriatal injection of (S)-alpha-amino-3-hydroxy-5,7-methylisoxazole-4-propionic acid (AMPA) (2." | ( Protective effect of the antiepileptic drug candidate talampanel against AMPA-induced striatal neurotoxicity in neonatal rats. Banczerowski-Pelyhe, I; Gulyás-Kovács, A; Takács, J; Tarnawa, I; Világi, I, 2002) | 0.31 |
| " The dose-response curve to glutamate was significantly broader in the presence of the desensitization inhibitor cyclothiazide." | ( Pharmacological characterization, localization, and regulation of ionotropic glutamate receptors in skate horizontal cells. Birnbaum, AD; Kreitzer, MA; Malchow, RP; Qian, H, ) | 0.13 |
| " The results show that a binge dosing regimen of METH to the rat increased plasma and brain ammonia concentrations that were paralleled by evidence of hepatotoxicity." | ( Peripheral ammonia as a mediator of methamphetamine neurotoxicity. Halpin, LE; Yamamoto, BK, 2012) | 0.38 |
| Class | Description |
|---|---|
| benzodiazepine | A group of heterocyclic compounds with a core structure containing a benzene ring fused to a diazepine ring. |
| [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) |
|---|---|---|---|---|---|---|---|
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 1.5849 | 0.0040 | 23.8416 | 100.0000 | AID485290 |
| Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 39.7164 | 0.1409 | 11.1940 | 39.8107 | AID2451 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 39.8107 | 0.0020 | 14.6779 | 39.8107 | AID1476 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 1.9953 | 0.0072 | 15.7588 | 89.3584 | AID411 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 28.1838 | 0.1000 | 20.8793 | 79.4328 | AID588453 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 4.2284 | 0.0316 | 37.5844 | 354.8130 | AID504865 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 5.0119 | 0.0282 | 7.0559 | 15.8489 | AID895; AID928 |
| GLS protein | Homo sapiens (human) | Potency | 12.5893 | 0.3548 | 7.9355 | 39.8107 | AID624146 |
| TDP1 protein | Homo sapiens (human) | Potency | 28.2320 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 31.6228 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 39.8107 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 12.5893 | 0.0013 | 7.7625 | 44.6684 | AID914; AID915 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 3.3786 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 7.5637 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 18.9991 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| arylsulfatase A | Homo sapiens (human) | Potency | 0.0338 | 1.0691 | 13.9551 | 37.9330 | AID720538 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 7.5193 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 28.3709 | 0.0020 | 7.5337 | 39.8107 | AID891 |
| hexokinase-4 isoform 1 | Homo sapiens (human) | Potency | 14.1254 | 2.5119 | 13.8003 | 28.1838 | AID743205 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 7.9433 | 0.0025 | 5.8400 | 31.6228 | AID899 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 1.2589 | 0.0063 | 6.9043 | 39.8107 | AID883 |
| glucokinase regulatory protein | Homo sapiens (human) | Potency | 14.1254 | 2.5119 | 13.8003 | 28.1838 | AID743205 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 8.8006 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 0.0224 | 0.0010 | 6.0009 | 35.4813 | AID943 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 8.8006 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Interferon beta | Homo sapiens (human) | Potency | 7.5637 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 7.5637 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 8.8006 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 8.8006 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 8.8006 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 8.8006 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 8.8006 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 8.8006 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 8.8006 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 8.8006 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 8.8006 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 8.8006 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 1.2589 | 0.0063 | 8.2350 | 39.8107 | AID883 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 8.8006 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 8.8006 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 8.8006 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 8.8006 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 7.5637 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 8.8006 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 7.5637 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 0.0379 | 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) |
|---|---|---|---|---|---|---|---|
| Glutamate receptor 1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 15.3200 | 0.0001 | 1.6179 | 10.0000 | AID258622; AID258623; AID31458; AID31580 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 15.3200 | 0.0001 | 1.7000 | 10.0000 | AID258622; AID258623; AID31458; AID31580 |
| Glutamate receptor 3 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 15.3200 | 0.0001 | 1.7000 | 10.0000 | AID258622; AID258623; AID31458; AID31580 |
| Glutamate receptor 4 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 15.3200 | 0.0001 | 1.7000 | 10.0000 | AID258622; AID258623; AID31458; AID31580 |
| Glutamate receptor 2 | Homo sapiens (human) | Ki | 4.5000 | 0.0168 | 1.2772 | 5.0000 | AID1486005; AID1486006 |
| [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) |
|---|---|---|---|---|---|---|---|
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| 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. |
| 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. |
| 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. |
| AID258623 | Displacement of [3H]CP-526427 from AMPA receptor in rat forebrain membranes | 2006 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 16, Issue:1 | New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists. |
| AID117880 | The compound was tested for percent reduction in KA-Evoked current against DBA/2 mice. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID132065 | Effective dose required for anticonvulsant activity against Clonic phase of seizure in DBA/2 mice 30 minutes after ip administration of the compound | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID212213 | Dose which induced 50% of mice to fall from the rotarod | 1998 | Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18 | 3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists. |
| AID114469 | Audiogenic seizures after concomitant treatment with Flumazenil (24.72 uM) in DBA / 2 mice clonic phase | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | 1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists. |
| AID112211 | The compound was tested for Anticonvulsant activity against Pentylenetetrazole (PTZ) induced seizures in Swiss mice | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID326372 | Antagonist activity at AMPA receptor in rat cerebral granule cells assessed as inhibition of kainate-induced calcium uptake after 30 mins | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5 | Structure-activity study of 2,3-benzodiazepin-4-ones noncompetitive AMPAR antagonists: identification of the 1-(4-amino-3-methylphenyl)-3,5-dihydro-7,8-ethylenedioxy-4H-2,3-benzodiazepin-4-one as neuroprotective agent. |
| AID113631 | Anticonvulsant activity against tonic phase of the audiogenic seizures in DBA / 2 mice 30 min after ip administration at a dose range 3.3-66 uM/kg | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | 1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists. |
| AID114475 | Audiogenic seizures after pretreatment with Aniracetam in DBA / 2 mice tonic phase at a dose range of 10-200 uM/kg | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | 1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists. |
| AID209497 | Anticonvulsant activity against KA induced seizures in swiss mice; Values ranges from: 18.8-40.9 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID53259 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice after pretreatment with Aniracetam expressed as ED50 values in clonic phase; Values ranges from: 88.8-203 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID129621 | Compound was evaluated for anticonvulsant activity against MES induced seizures(tonic phase) in swiss mice | 1998 | Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8 | 7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists. |
| AID20515 | Relative Lipophilicity measured by reversed-phase high performance thin-layer chromatography (RP-HPTLC) | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones. |
| AID132757 | In vivo anticonvulsant activity in mouse determined by maximum electroshock induced seizure (MES) assay | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14 | Synthesis of 7,8-(methylenedioxy)-1-phenyl-3,5-dihydro-4H-2, 3-benzodiazepin-4-ones as novel and potent noncompetitive AMPA receptor antagonists. |
| AID222986 | Anticonvulsant activity against MES induced seizures in swiss mice in tonic phase (95% confidence limits) | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID132062 | Effective dose required for anticonvulsant activity against Clonic phase of seizure in DBA/2 mice 120 minutes after ip administration of the compound | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID209500 | Anticonvulsant activity against PTZ induced seizures was observed in mice after intraperitoneal injection | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17 | Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives. |
| AID53435 | Evaluated for anticonvulsant property in DBA/2 mice against Audiogenic seizures during tonic phase (ip administration); value ranges from 16.0-40.0 | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones. |
| AID234046 | Therapeutic index (TD50/ED50) from the clonic phase of the audiogenic seizures | 1998 | Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18 | 3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists. |
| AID113450 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice (value required to prevent clonic phases of seizures). | 1998 | Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18 | 3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists. |
| AID20519 | Relative lipophilicity of the compound | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID1486006 | Antagonist activity at open state of GFP-tagged GluA2Qflip isoform (unknown origin) expressed in HEK293S cells assessed as reduction in glutamate-induced current response in presence of 3 mM glutamate by whole cell assay relative to control | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Development of novel N-3-bromoisoxazolin-5-yl substituted 2,3-benzodiazepines as noncompetitive AMPAR antagonists. |
| AID113453 | Anticonvulsant activity against audiogenic tonus seizure 30 min after intraperitoneal administration (3.3-200 umol/kg) in DBA/2 mice | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | 1-aryl-6,7-methylenedioxy-3H-quinazolin-4-ones as anticonvulsant agents. |
| AID112214 | The compound was tested for Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID209503 | Anticonvulsant activity against Pentylenetetrazole (PTZ) induced seizures in Swiss mice; Values ranges from: 56.2-83.1 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID20516 | Relative lipophilicity of compound | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | 1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists. |
| AID53416 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase at a time interval of 45 min after intraperitoneal administration; Values ranges from: 27.2-52.1 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID113459 | Anticonvulsant activity against clonic phase of the audiogenic seizures after concomitant with flumazenil at 8.24 umol dose in DBA/2 mice | 1998 | Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18 | 3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists. |
| AID112210 | The compound was tested for Anticonvulsant activity against KA induced seizures in DBA/2 mice. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID114070 | Pentylenetetrazole-induced seizures in Swiss mice after 45 min pretreatment at a dose range 10-100 uM/kg | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | 1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists. |
| AID113813 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice measured in tonic phase | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists. |
| AID51579 | Compound was examined in vitro for inhibition of AMPA (5 uM) evoked spreading depression in isolated retina prepared from young chicken | 2000 | Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9 | Structural analogues of some highly active non-competitive AMPA antagonists. |
| AID113024 | In vivo anticonvulsant activity was measured as median effective dose required to prevent tonic phase of seizure in DBA/2 mice | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 | QSAR study of anticonvulsant negative allosteric modulators of the AMPA receptor. |
| AID129633 | Compound was evaluated for anticonvulsant activity against audiogenic seizures in DBA/2 mice( clonic phase) | 1998 | Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8 | 7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists. |
| AID20517 | Relative lipophilicity | 1998 | Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18 | 3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists. |
| AID53251 | Anticonvulsant activity against Audiogenic seizures in DBA/2 mice was observed in clonic phase after pretreatment with Aniracetam | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17 | Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives. |
| AID112212 | The compound was tested for Anticonvulsant activity against audiogenic seizures in DBA/2 mice after pretreatment with Aniracetam in clonic phase | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID92629 | Percentage inhibition of [3H]AMPA binding to Ionotropic glutamate receptor AMPA of rat cortical membranes at 32 uM | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists. |
| AID132082 | Effective dose required for anticonvulsant activity against KA-induced (32 mg/kg s/c 15 minutes after intraperitoneal injection of compound) seizure in Swiss mice | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID53250 | Anticonvulsant activity against Audiogenic seizures in DBA/2 mice was observed in clonic phase after intraperitoneal injection | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17 | Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives. |
| AID113451 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice (value required to prevent tonic phases of seizures). | 1998 | Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18 | 3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists. |
| AID53261 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice after pretreatment with Aniracetam expressed as ED50 values in tonic phase; Values ranges from: 63.4-158 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID113599 | Anticonvulsant activity against clonic phase of the audiogenic seizures in DBA / 2 mice 30 min after ip administration at a dose range 3.3-66 uM/kg | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | 1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists. |
| AID114472 | Audiogenic seizures after concomitant treatment with Flumazenil (8.24 uM) in DBA / 2 mice tonic phase | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | 1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists. |
| AID132075 | Effective dose required for anticonvulsant activity against MES-induced Tonic seizure in Swiss mice 45 minutes after ip administration of the compound | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID113812 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice measured in clonic phase | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists. |
| AID129620 | Compound was evaluated for anticonvulsant activity against AMPA induced seizures in DBA/2 mice( tonic phase) | 1998 | Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8 | 7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists. |
| AID53421 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase at a time interval of 90 min after intraperitoneal administration | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID53131 | Anticonvulsant activity against ATPA induced seizures in DBA/2 mice. activity is expressed as ED50 values in clonus phase; Values ranges from: 45.4-89.7 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID352070 | Anticonvulsant activity against audiogenic clonus seizures in ip dosed DBA/2 mouse epilepsy model administered 30 mins before auditory simulation | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Solution-phase parallel synthesis and evaluation of anticonvulsant activity of N-substituted-3,4-dihydroisoquinoline-2(1H)-carboxamides. |
| AID31580 | Inhibitory activity against AMPA receptor currents in rat cortical cells stimulated with 50 uM kainic acid | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | Substituted 1,2-dihydrophthalazines: potent, selective, and noncompetitive inhibitors of the AMPA receptor. |
| AID231693 | Ratio between TD50 and ED50 from the clonic phase of the audiogenic seizures was determined | 1998 | Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8 | 7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists. |
| AID130095 | Loss of righting reflex was observed after the peroral administration of compound in mice | 2000 | Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9 | Structural analogues of some highly active non-competitive AMPA antagonists. |
| AID212215 | Motor toxicity in 50% of mice on locomotion assessed by Rotarod test following 30 min ip administration | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | 1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists. |
| AID92203 | Ability to displace [3H]CP-526427 from the AMPA receptor binding site in rat forebrain membranes | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists. |
| AID95169 | Percentage reduction of KA (kainate) evoked currents at a concentration of 100 uM in cerebellar neurons | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID129622 | Compound was evaluated for anticonvulsant activity against PTZ induced seizures (clonic phase) in swiss mice | 1998 | Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8 | 7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists. |
| AID136095 | Dose required to produce locomotor deficit assessed by rotarod test in DBA/2 mice. | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID112217 | The compound was tested for Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase. 30 min after ip administration. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID53249 | Anticonvulsant activity against ATPA induced seizures in DBA/2 mice. activity is expressed as ED50 values in tonus phase; Values ranges from: 32.4-57.3 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID212209 | Compound was evaluated for toxic dose on locomotor assessed by rotarod test in mice | 1998 | Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8 | 7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists. |
| AID132076 | Effective dose required for anticonvulsant activity against PTZ-induced Clonic seizure in Swiss mice 45 minutes after ip administration of the compound | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID258618 | Effect on clonic phase of audiogenic seizures in DBA/2 mice at 3.3-200 umol/kg, ip | 2006 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 16, Issue:1 | New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists. |
| AID129627 | Compound was evaluated for anticonvulsant activity against audiogenic induced seizures after pretreatment with aniracetam (clonic phase); p<0.01 | 1998 | Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8 | 7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists. |
| AID326374 | Inhibition of kainate-induced C57BL/6N mouse hippocampal neurons excitotoxicity after 48 hrs by MTT assay | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5 | Structure-activity study of 2,3-benzodiazepin-4-ones noncompetitive AMPAR antagonists: identification of the 1-(4-amino-3-methylphenyl)-3,5-dihydro-7,8-ethylenedioxy-4H-2,3-benzodiazepin-4-one as neuroprotective agent. |
| AID53581 | Toxic does was determined in DBA/2 mice; Values ranges from: 47.5-122 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID53267 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice expressed as ED50 values in clonic phase; Values ranges from: 24.4-52.4 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID258620 | Effect on locomotion in mice assessed by rotarod test at 3.3-200 umol/kg, ip | 2006 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 16, Issue:1 | New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists. |
| AID53125 | Anticonvulsant activity against AMPA-induced seizures in DBA/2 mice was observed in clonic phase after intraperitoneal injection | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17 | Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives. |
| AID51581 | Compound was examined in vitro for inhibition of kainate (5 uM) evoked spreading depression in isolated retina prepared from young chicken | 2000 | Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9 | Structural analogues of some highly active non-competitive AMPA antagonists. |
| AID112215 | The compound was tested for Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase. 120 min after ip administration. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID28646 | Relative lipophilicity expressed as Rm value | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID325520 | Anticonvulsant activity against audiogenic tonus seizures in DBA/2 mouse after 30 mins | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5 | Synthesis and anticonvulsant evaluation of N-substituted isoquinoline AMPA receptor antagonists. |
| AID179586 | In vitro inhibition of AMPA activated current in xenopus oocytes expressing rat cerebral cortex poly(A)+ RNA. | 1998 | Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14 | Synthesis of 7,8-(methylenedioxy)-1-phenyl-3,5-dihydro-4H-2, 3-benzodiazepin-4-ones as novel and potent noncompetitive AMPA receptor antagonists. |
| AID130094 | Loss of righting reflex was observed after the intraperitoneal administration of compound in mice | 2000 | Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9 | Structural analogues of some highly active non-competitive AMPA antagonists. |
| AID113447 | Anticonvulsant activity against audiogenic clonus seizure 30 min after intraperitoneal administration (3.3-200 umol/kg) in DBA/2 mice | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | 1-aryl-6,7-methylenedioxy-3H-quinazolin-4-ones as anticonvulsant agents. |
| AID114473 | Audiogenic seizures after pretreatment with Aniracetam in DBA / 2 mice clonic phase at a dose range of 10-200 uM/kg | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | 1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists. |
| AID270294 | Anticonvulsant activity against tonic phase of audiogenic seizures in ip dosed DBA/2 mouse | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Novel potent anticonvulsant agent containing a tetrahydroisoquinoline skeleton. |
| AID132060 | Effective dose required for anticonvulsant activity against AMPA-induced clonic seizure in Swiss mice 45 minutes after ip administration of the compound | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID223850 | Compound was tested for inhibition of whole cell current induced by 5 Purkinje cells | 2000 | Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9 | Structural analogues of some highly active non-competitive AMPA antagonists. |
| AID129619 | Compound was evaluated for anticonvulsant activity against AMPA induced seizures in DBA/2 mice( clonic phase) | 1998 | Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8 | 7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists. |
| AID129634 | Compound was evaluated for anticonvulsant activity against audiogenic seizures in DBA/2 mice( tonic phase) | 1998 | Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8 | 7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists. |
| AID129632 | Compound was evaluated for anticonvulsant activity against audiogenic induced seizures after pretreatment with aniracetam (tonic phase); p<0.01 | 1998 | Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8 | 7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists. |
| AID131376 | Effective dose (ip administration) required for anticonvulsant activity against clonic phase of audiogenic seizures in DBA/2 mice after pretreatment with aniracetam+ 2,3-benzodiazepine (p<0.01) | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID112216 | The compound was tested for Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase. 15 min after ip administration. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID132069 | Effective dose required for anticonvulsant activity against Clonic phase of seizure in DBA/2 mice 60 minutes after ip administration of the compound | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID222987 | Anticonvulsant activity against PTZ induced seizures in swiss mice in clonic phase (95% confidence limits) | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID1065307 | Anticonvulsant activity in ip dosed albino mouse assessed as protection against AMPA-induced tonic phase of seizures after 30 mins | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach. |
| AID113625 | Anticonvulsant activity against tonic phase of the audiogenic seizures after pretreatment with aniracetam in DBA/2 mice | 1998 | Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18 | 3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists. |
| AID113774 | Anticonvulsant activity against tonic seizures induced by icv injection of AMPA in DBA/2 mice | 1998 | Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18 | 3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists. |
| AID53283 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase at a time interval of 120 min after intraperitoneal administration | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID235208 | Therapeutic index is the ratio between TD50 and ED50 (from the clonic phase of the audiogenic seizures) | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones. |
| AID222990 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase after 15 min intraperitoneal administration (95% confidence limit in parentheses) | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID113607 | Anticonvulsant activity against pentylenetetrazole (PTZ)-induced seizures in swiss mice | 1998 | Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18 | 3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists. |
| AID53123 | Anticonvulsant activity against AMPA induced seizures in DBA/2 mice. activity is expressed as ED50 values in clonus phases; Values ranges from: 26.3-60.8 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID132063 | Effective dose required for anticonvulsant activity against Clonic phase of seizure in DBA/2 mice 15 minutes after ip administration of the compound | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID113612 | Anticonvulsant activity against the clonic seizures induced by icv injection of AMPA in DBA / 2 mice at a dose range of 10-100 uM/kg | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | 1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists. |
| AID222983 | Anticonvulsant activity against AMPA induced seizures in DBA/2 mice after intracerebro ventricular administration at the CD97 for clonus (9.7 nmol) (95% confidence limits) | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID326371 | Displacement of [3H]CP-526427 from AMPA receptor in Sprague-Dawley rat fore brain by radioligand binding assay | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5 | Structure-activity study of 2,3-benzodiazepin-4-ones noncompetitive AMPAR antagonists: identification of the 1-(4-amino-3-methylphenyl)-3,5-dihydro-7,8-ethylenedioxy-4H-2,3-benzodiazepin-4-one as neuroprotective agent. |
| AID222993 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase after 45 min intraperitoneal administration (95% confidence limit in parentheses) | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID129006 | Anticonvulsant activity of compound, administered perorally in mice was evaluated using maximal metrazole seizure model | 2000 | Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9 | Structural analogues of some highly active non-competitive AMPA antagonists. |
| AID113616 | Anticonvulsant activity against the maximal electroshock in Swiss mice after 45 minutes pretreatment at a dose range 10-100 uM/kg | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | 1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists. |
| AID112209 | The compound was tested for Anticonvulsant activity against AMPA induced seizures in DBA/2 mice in tonic phase | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID53255 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice 30 min after intraperitoneal administration (clonic phase) | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1 | Discovery of a novel and highly potent noncompetitive AMPA receptor antagonist. |
| AID113605 | Anticonvulsant activity against maximal electroshock (MES) seizures in swiss mice | 1998 | Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18 | 3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists. |
| AID113603 | Anticonvulsant activity against clonic seizures induced by icv injection of AMPA in DBA/2 mice | 1998 | Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18 | 3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists. |
| AID112213 | The compound was tested for Anticonvulsant activity against audiogenic seizures in DBA/2 mice after pretreatment with Aniracetam in tonic phase. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID222988 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase. | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID53440 | Evaluated for anticonvulsant property in DBA/2 mice against audiogenic Seizures after pretreatment with Aniracetam during tonic phase, *p<0.0 1; value ranges from 63.4-158 | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones. |
| AID53252 | Anticonvulsant activity against Audiogenic seizures in DBA/2 mice was observed in tonic phase after intraperitoneal injection | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17 | Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives. |
| AID131377 | Effective dose (ip administration) required for anticonvulsant activity against tonic phase of audiogenic seizures in DBA/2 mice after pretreatment with aniracetam+ 2,3-benzodiazepine (p<0.01) | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID223108 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice in tonic phase (95% confidence limit in parentheses) | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID221079 | Locomotion assessed by Rotarod test in mice | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID114471 | Audiogenic seizures after concomitant treatment with Flumazenil (8.24 uM) in DBA / 2 mice clonic phase | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | 1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists. |
| AID270293 | Anticonvulsant activity against clonic phase of audiogenic seizures in ip dosed DBA/2 mouse | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Novel potent anticonvulsant agent containing a tetrahydroisoquinoline skeleton. |
| AID53424 | Evaluated for anticonvulsant property in DBA/2 mice against AMPA induced seizures during tonic phase; value ranges from 26.3-60.8 | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones. |
| AID112218 | The compound was tested for Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase. 45 min after ip administration. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID113458 | Anticonvulsant activity against clonic phase of the audiogenic seizures after concomitant with flumazenil at 24.72 umol dose in DBA/2 mice | 1998 | Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18 | 3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists. |
| AID325521 | Reduction in AMPA-mediated current in CA1 pyramidal neurons of Wistar rat at 50 uM after 5 mins by patch clamp technique | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5 | Synthesis and anticonvulsant evaluation of N-substituted isoquinoline AMPA receptor antagonists. |
| AID258621 | Protective index [PI = TD50/ED50 (from clonic phase of the audiogenic seizures)] in mice at 3.3-200 umol/kg, ip | 2006 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 16, Issue:1 | New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists. |
| AID113620 | Anticonvulsant activity against the tonic seizures induced by icv injection of AMPA in DBA / 2 mice at a dose range of 10-100 uM/kg | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | 1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists. |
| AID242286 | In vitro inhibition of AMPA receptor mediated currents in primary cultured rat fetal hippocampal neurons | 2005 | Journal of medicinal chemistry, Jul-14, Volume: 48, Issue:14 | Novel alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptor antagonists of 2,3-benzodiazepine type: chemical synthesis, in vitro characterization, and in vivo prevention of acute neurodegeneration. |
| AID222984 | Anticonvulsant activity against AMPA induced seizures in DBA/2 mice after intracerebro ventricular administration at the CD97 for tonus (11.7 nmol) (95% confidence limits) | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID112219 | The compound was tested for Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase. 60 min after ip administration. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID31458 | Antagonist potency against functional AMPA receptor by kainate-induced Ca+2 in rat cerebellar granule neurons in primary culture | 2000 | Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11 | Methaqualone derivatives are potent noncompetitive AMPA receptor antagonists. |
| AID113023 | In vivo anticonvulsant activity was measured as median effective dose required to prevent clonic phase of seizure in DBA/2 mice | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 | QSAR study of anticonvulsant negative allosteric modulators of the AMPA receptor. |
| AID222985 | Anticonvulsant activity against KA induced seizures in DBA/2 mice at a dose of 32 mg/kg at CD97 after intraperitoneal administration (95% confidence limits) | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID113623 | Anticonvulsant activity against tonic phase of the audiogenic seizures after concomitant with flumazenil at 24.72 umol dose in DBA/2 mice | 1998 | Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18 | 3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists. |
| AID53419 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase at a time interval of 60 min after intraperitoneal administration; Values ranges from: 29.6-52.7 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID143626 | Percentage inhibition of [3H]glycine to NMDA receptors of rat cortical membranes at 32 uM | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists. |
| AID53413 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase at a time interval of 30 min after intraperitoneal administration; Values ranges from: 24.4-62.4 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID140253 | Percent reduction of KA-evoked current with the patch clamp technique in cerebellar granule neurons grown in primary culture after administration of 100 uM of KA and compound. | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID53124 | Anticonvulsant activity against AMPA induced seizures in DBA/2 mice. activity is expressed as ED50 values in tonus phases; Values ranges from: 43.5-76.0 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID179938 | Inhibition of KA-induced increase in [Ca2+]i in rat cerebellar granule neurons | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3 | Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists. |
| AID112220 | The compound was tested for Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase. 90 min after ip administration. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID258622 | Ability to inhibit kainate-induced increase of calcium in rat cerebellar granule cells expressing AMPA receptor | 2006 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 16, Issue:1 | New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists. |
| AID235218 | Therapeutic index it is the ratio between TD50 and ED50 (from the clonic phase of the audiogenic seizures) | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | 1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists. |
| AID53423 | Evaluated for anticonvulsant property in DBA/2 mice against AMPA induced seizures during clonic phase; value ranges from 43.5-76.0 | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones. |
| AID132079 | Anticonvulsant activity against audiogenic tonic seizures in DBA/2 mice, administered ip 30 minutes before auditory stimulation | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID132078 | Anticonvulsant activity against audiogenic Clonic seizures in DBA/2 mice, administered ip 30 minutes before auditory stimulation. | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID53446 | Evaluated for anticonvulsant property in DBA/2 mice against Locomotion assessed by Rotarod test (ip administration); value ranges from 47.5-122 | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones. |
| AID113460 | Anticonvulsant activity against clonic phase of the audiogenic seizures after pretreatment with aniracetam in DBA/2 mice | 1998 | Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18 | 3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists. |
| AID325519 | Anticonvulsant activity against audiogenic clonus seizures in DBA/2 mouse after 30 mins | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5 | Synthesis and anticonvulsant evaluation of N-substituted isoquinoline AMPA receptor antagonists. |
| AID222995 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase after 60 min intraperitoneal administration (95% confidence limit in parentheses) | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID209499 | Anticonvulsant activity against MES induced seizures was observed in mice after intraperitoneal injection | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17 | Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives. |
| AID209506 | Anticonvulsant activity against maximal electroshock (MES) induced seizures in Swiss mice; Values ranges from: 29.3-43.4 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID28727 | Partition coefficient (logP) | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID226938 | Ratio between TD50 and ED50 from the clonic phase of audiogenic seizures in mice | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID133525 | Ratio of TD50 to ED50, expressed as protective index | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID53256 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice 30 min after intraperitoneal administration (tonic phase) | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1 | Discovery of a novel and highly potent noncompetitive AMPA receptor antagonist. |
| AID132071 | Effective dose required for anticonvulsant activity against Clonic phase of seizure in DBA/2 mice 90 minutes after ip administration of the compound | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID226537 | Protective index as the ratio of TD50 to ED50 (from the clonic phase of the audiogenic seizures). | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID32523 | Percentage reduction of ATPA evoked currents at a concentration of 100 uM in cerebellar neurons | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID222991 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase after 30 min intraperitoneal administration (95% confidence limit in parentheses) | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID258619 | Effect on tonic phase of audiogenic seizures in DBA/2 mice at 3.3-200 umol/kg, ip | 2006 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 16, Issue:1 | New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists. |
| AID209517 | Evaluated for anticonvulsant property in Swiss mice against PTZ induced seizures; value ranges from 56.2-83.1 | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones. |
| AID53439 | Evaluated for anticonvulsant property in DBA/2 mice against audiogenic Seizures after pretreatment with Aniracetam during clonic phase, *p<0.01; value ranges from 88.8-203 | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones. |
| AID92202 | Ability to displace [3H]CP-526427 (3 nM) from binding site of the Ionotropic glutamate receptor AMPA in rat forebrain membrane | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24 | 1-aryl-6,7-methylenedioxy-3H-quinazolin-4-ones as anticonvulsant agents. |
| AID113624 | Anticonvulsant activity against tonic phase of the audiogenic seizures after concomitant with flumazenil at 8.24 umol dose in DBA/2 mice | 1998 | Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18 | 3,5-Dihydro-4H-2,3-benzodiazepine-4-thiones: a new class of AMPA receptor antagonists. |
| AID1486005 | Antagonist activity at closed state of GFP-tagged GluA2Qflip isoform (unknown origin) expressed in HEK293S cells assessed as reduction in glutamate-induced current response in presence of 0.1 mM glutamate by whole cell assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Development of novel N-3-bromoisoxazolin-5-yl substituted 2,3-benzodiazepines as noncompetitive AMPAR antagonists. |
| AID1065308 | Anticonvulsant activity in ip dosed albino mouse assessed as protection against AMPA-induced clonic phase of seizures after 30 mins | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach. |
| AID131234 | Muscle relaxant activity of compound, administered intraperitoneally in mice was evaluated using inclined screen test | 2000 | Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9 | Structural analogues of some highly active non-competitive AMPA antagonists. |
| AID132067 | Effective dose required for anticonvulsant activity against Clonic phase of seizure in DBA/2 mice 45 minutes after ip administration of the compound | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID53253 | Anticonvulsant activity against Audiogenic seizures in DBA/2 mice was observed in tonic phase after pretreatment with Aniracetam | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17 | Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives. |
| AID31590 | Inhibition of kainic acid induced AMPA receptor mediated current at 100 uM | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | Substituted 1,2-dihydrophthalazines: potent, selective, and noncompetitive inhibitors of the AMPA receptor. |
| AID112221 | The compound was tested for Anticonvulsant activity against audiogenic seizures in DBA/2 mice in tonic phase | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID222989 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase after 120 min intraperitoneal administration (95% confidence limit in parentheses) | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| AID53286 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase at a time interval of 15 min after intraperitoneal administration; Values ranges from: 7.11-16.4 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID53428 | Evaluated for anticonvulsant property in DBA/2 mice against Audiogenic seizures during clonic phase (ip administration); value ranges from 24.4-52.4 | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones. |
| AID132061 | Effective dose required for anticonvulsant activity against AMPA-induced tonic seizure in Swiss mice 45 minutes after ip administration of the compound | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones. |
| AID114470 | Audiogenic seizures after concomitant treatment with Flumazenil (24.72 uM) in DBA / 2 mice tonic phase | 1997 | Journal of medicinal chemistry, Apr-11, Volume: 40, Issue:8 | 1-Aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones: novel AMPA receptor antagonists. |
| AID53273 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice expressed as ED50 values in tonic phase; Values ranges from: 16.0-40.0 | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID122013 | The compound was tested for Anticonvulsant activity against audiogenic seizures in DBA/2 mice. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID352071 | Anticonvulsant activity against audiogenic tonus seizures in ip dosed DBA/2 mouse epilepsy model administered 30 mins before auditory simulation | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Solution-phase parallel synthesis and evaluation of anticonvulsant activity of N-substituted-3,4-dihydroisoquinoline-2(1H)-carboxamides. |
| AID27598 | Calculated partition coefficient (clogP) (PALLAS 2.0) | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | Synthesis and anticonvulsant activity of novel and potent 6,7-methylenedioxyphthalazin-1(2H)-ones. |
| AID112208 | The compound was tested for Anticonvulsant activity against AMPA induced seizures in DBA/2 mice clonic phase. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID209511 | Evaluated for anticonvulsant property in Swiss mice against MES induced seizures; value ranges from 29.3-43.4 | 2000 | Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25 | Synthesis and evaluation of pharmacological and pharmacokinetic properties of 11H-[1,2,4]triazolo[4,5-c][2,3]benzodiazepin-3(2H)-ones. |
| AID129004 | Anticonvulsant activity of compound, administered perorally in mice was evaluated using maximal electroshock seizure model | 2000 | Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9 | Structural analogues of some highly active non-competitive AMPA antagonists. |
| AID112222 | The compound was tested for Anticonvulsant activity against maximal electroshock (MES) induced seizures in Swiss mice. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists. |
| AID223105 | Anticonvulsant activity against audiogenic seizures in DBA/2 mice in clonic phase after 90 min intraperitoneal administration (95% confidence limit in parentheses) | 2002 | Journal of medicinal chemistry, Sep-26, Volume: 45, Issue:20 | Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 1 (0.33) | 18.7374 |
| 1990's | 141 (46.53) | 18.2507 |
| 2000's | 115 (37.95) | 29.6817 |
| 2010's | 39 (12.87) | 24.3611 |
| 2020's | 7 (2.31) | 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 (21.75) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 3 (0.96%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 309 (99.04%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||