| ID Source | ID |
|---|---|
| PubMed CID | 53555 |
| CHEMBL ID | 283656 |
| SCHEMBL ID | 154037 |
| MeSH ID | M0117612 |
| Synonym |
|---|
| dazmegrel |
| uk-38485 |
| D03661 |
| dazmegrel (usan/inn) |
| 76894-77-4 |
| CBDIVE_000516 |
| OPREA1_040141 |
| 3-[3-(1h-imidazol-1-ylmethyl)-2-methyl-1h-indol-1-yl]propanoic acid |
| STK094650 |
| EU-0045204 |
| NCGC00160660-01 |
| uk-38,485 |
| 3-(imidazol-1-ylmethyl)-2-methylindole-1-propionic acid |
| 1h-indole-1-propanoic acid, 3-(1h-imidazol-1-ylmethyl)-2-methyl- |
| dazmegrelum [latin] |
| uk 38,485 |
| CHEMBL283656 , |
| bdbm50000317 |
| 3-(3-imidazol-1-ylmethyl-2-methyl-indol-1-yl)-propionic acid |
| 3-[3-(imidazol-1-ylmethyl)-2-methylindol-1-yl]propanoic acid |
| dazmegrelum |
| unii-31340r8pvu |
| dazmegrel [usan:inn:ban] |
| 31340r8pvu , |
| dtxsid9046281 , |
| dtxcid7026281 |
| cas-76894-77-4 |
| tox21_111966 |
| CCG-20521 |
| 1h-indole-1-propanoicacid, 3-(1h-imidazol-1-ylmethyl)-2-methyl- |
| AKOS005395464 |
| SCHEMBL154037 |
| NCGC00160660-02 |
| tox21_111966_1 |
| dazmegrel [usan] |
| dazmegrel [inn] |
| dazmegrel [mart.] |
| SR-01000082437-1 |
| sr-01000082437 |
| FT-0746556 |
| Q27256003 |
Dazmegrel is a selective thromboxane A2 synthetase inhibitor. Flunarizine (a calcium entry blocker) also inhibits the effects of elevated thromboxes A2 levels.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Dazmegrel is a selective thromboxane A2 synthetase inhibitor and flunarizine (a calcium entry blocker) also inhibits the effects of elevated thromboxane A2 levels." | ( Significance of thromboxane A2 and prostaglandin I2 in acute necrotizing pancreatitis in rats. Kort, WJ; Tinga, CJ; van Ooijen, B; Wilson, JH, 1990) | 1 |
| "Dazmegrel is a selective thromboxane A2 synthetase inhibitor and prevents the formation of thromboxane A2." | ( Significance of prostaglandin E2 in acute necrotising pancreatitis in rats. Kort, WJ; Tinga, CJ; van Ooijen, B; Westbroek, DL; Wilson, JH, 1989) | 1 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Dazmegrel did not inhibit proteinuria or glomerular hypercellularity." | ( Effect of a thromboxane synthetase inhibitor on eicosanoid synthesis and glomerular injury during acute unilateral glomerulonephritis in the rat. Cattell, V; Cook, HT; Moncada, S; Salmon, JA; Smith, J, 1986) | 0.99 |
Dazmegrel pretreatment prevented increased thromboxane A2, but resulted in a significant increase in plasma prostacyclin, measured as 6-keto-PGF1 alpha. Pretreatment with daz megrel 5 min before PAF abolished the PAF potentiation of the digitalis-induced arrhythmias.
| Excerpt | Reference | Relevance |
|---|---|---|
| "In Dazmegrel-treated animals in whom pulmonary vasoconstriction was established by epinephrine infusion, low doses of substance P produced vasodilation." | ( Opposing hemodynamic effects of substance P on pulmonary vasculature in rabbits. Grunstein, MM; Gumbay, RS; Tanaka, DT; Worthen, GS, 1985) | 0.78 |
| "Dazmegrel pretreatment prevented increased thromboxane A2, measured as thromboxane B2, but resulted in a significant increase in plasma prostacyclin, measured as 6-keto-PGF1 alpha." | ( Inhibition of thromboxane synthetase accentuates hemodynamic instability and burn edema in the anesthetized sheep model. Demling, RH; LaLonde, C, 1989) | 1 |
| "Pretreatment with dazmegrel 5 min before PAF, 0.05 nmol/animal i.v., abolished the PAF potentiation of the digitalis-induced arrhythmias." | ( Protective effects of dazmegrel on the PAF potential of ouabain-induced cardiac arrhythmias. Barrigón, S; Salinas, P, 1991) | 0.92 |
| "Pretreatment with dazmegrel totally prevented the pulmonary vascular response to bacterial infusion." | ( Cardiopulmonary function as related to thromboxane A2 synthesis in experimental septic shock. Falk, A; Haglund, U; Lindholm, E; Schützer, KM, 1988) | 0.6 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "4 microM) inhibitory activities, was found to be orally bioavailable with a long duration of action and offered effective protection against mortality in a collagen-epinephrine-induced pulmonary thromboembolism model in mice." | ( 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. Bruno, JJ; Hirschfeld, DR; Maloney, PJ; Martinez, GR; Walker, KA; Yang, DS, 1992) | 0.28 |
| "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 |
Pulmonary hypertension was not observed in the pretreatment group. Dazmegrel had a beneficial effect on wound healing when given systemically at a dosage of 3.
| Excerpt | Relevance | Reference |
|---|---|---|
| " 7e, 9e, 13a, 13d, 18, 20, 21, and 23, when dosed orally in conscious spontaneously hypertensive rats." | ( 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. Bruno, JJ; Hirschfeld, DR; Maloney, PJ; Martinez, GR; Walker, KA; Yang, DS, 1992) | 0.28 |
| " In separate groups of rats, the log dose-response curve for bolus intravenous injection of AII was shifted to the right by SQ-29,548 while that for PE was unaffected." | ( Thromboxane mediation of the pressor response to infused angiotensin II. Welch, WJ; Wilcox, CS, 1990) | 0.28 |
| "We have previously demonstrated more rapid wound healing in deep partial thickness burn guinea-pigs treated with intramuscular injection of the lower dosage of the thromboxane synthetase inhibitor Dazmegrel." | ( [Effect of the thromboxane synthetase inhibitor dazmegrel (UK 38,485) on skin blood flow in deep partial thickness burns]. Wang, SL, 1989) | 0.72 |
| " That is, the dose-response curves shifted to lower concentrations with increasing incubation times with UK-38485 prior to addition of aggregation agents." | ( Pharmacology of UK-38485 (dazmegrel), a specific inhibitor of thromboxane A2 synthetase. Rebec, MV; Skrinska, VA, 1989) | 0.58 |
| " Finally, the Tx receptor antagonist L-640,035 was tested using a dosing regimen that reduced the increase in right ventricular pressure caused by a stable endoperoxide analogue in MCTP-treated rats." | ( Thromboxane does not mediate pulmonary vascular response to monocrotaline pyrrole. Ganey, PE; Roth, RA, 1987) | 0.27 |
| " Rabbits were fed a diet supplemented with 2% cholesterol and 8% peanut oil for 12 weeks with or without UK-38485 at a dosage that maintained 80% to 90% inhibition of TXA2 formation in serum." | ( Suppression of foam cell lesions in hypercholesterolemic rabbits by inhibition of thromboxane A2 synthesis. Galang, CF; Gerrity, RG; Konieczkowski, M; Rebec, MV; Skrinska, VA, ) | 0.13 |
| " After establishing a dose-response relationship, we chose a control dose that produced intermediate hypertensive responses." | ( Hemodynamic responses of chronically instrumented piglets to bolus injections of group B streptococci. Barefield, E; Godoy, G; Gray, BM; Graybar, G; Lyrene, RK; Philips, JB; Sams, JE, 1988) | 0.27 |
| " Consistent with a mechanistic link between migration and apoptosis, the dose-response for stimulation of migration on laminin was inversely proportional to apoptosis induction." | ( Migrating glioma cells activate the PI3-K pathway and display decreased susceptibility to apoptosis. Beaudry, CE; Berens, ME; Demuth, T; Holz, DR; Joy, AM; Ponce, FA; Tran, NL, 2003) | 0.32 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 21.8761 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 1.9497 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 27.5404 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 40.5334 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
| Interferon beta | Homo sapiens (human) | Potency | 1.9497 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 1.9497 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 1.9497 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 1.9497 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [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) |
|---|---|---|---|---|---|---|---|
| Thromboxane-A synthase | Homo sapiens (human) | IC50 (µMol) | 0.0280 | 0.0009 | 1.2304 | 10.0000 | AID210470; AID215773 |
| Thromboxane-A synthase | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0280 | 0.0040 | 0.3923 | 1.5000 | AID210470 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| 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. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| 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. |
| AID89307 | Relative potency to inhibit ADP-induced aggregation of human platelet rich plasma compared to that of dazoxiben, in vitro using pig aortal microsomes. | 1989 | Journal of medicinal chemistry, Apr, Volume: 32, Issue:4 | [(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors. |
| AID179761 | In vitro inhibition of thromboxane A2 production in rat platelet-rich plasma. | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives. |
| AID117592 | Activity at 10 mg/kg given intravenously against mortality in a pulmonary thromboembolism model in mice (10 animals) at -7h following oral administration | 1989 | Journal of medicinal chemistry, Apr, Volume: 32, Issue:4 | [(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors. |
| AID117584 | Time course of protection against mortality in a pulmonary thromboembolism model in mice after -1h | 1992 | Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4 | 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. |
| AID203339 | Inhibition of serum TXB2 production after 15 minutes at 1.0 mg/kg intravenous dose | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Selective thromboxane synthetase inhibitors. 2. 3-(1H-imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogues. |
| AID197381 | Enhancement of prostaglandin E2 levels in serum of incubated whole blood at 1 hr after an oral dose of 1 mg/kg | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives. |
| AID203465 | Inhibition of serum TXB2 production after 2 minutes at 1.0 mg/kg intravenous dose | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Selective thromboxane synthetase inhibitors. 2. 3-(1H-imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogues. |
| AID120757 | Protection against mortality in pulmonary thromboembolism model in mice at 3 mg/kg | 1992 | Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4 | 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. |
| AID117590 | Activity at 10 mg/kg given intravenously against mortality in a pulmonary thromboembolism model in mice (10 animals) at -1h following oral administration | 1989 | Journal of medicinal chemistry, Apr, Volume: 32, Issue:4 | [(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors. |
| AID89303 | In vitro inhibition of ADP-induced aggregation of human platelet rich plasma in the presence of pig aortal microsomes. | 1989 | Journal of medicinal chemistry, Apr, Volume: 32, Issue:4 | [(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors. |
| AID183565 | Inhibition of thromboxane B2 production in whole blood of rats 1 hr following 1 mg/kg p.o. | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives. |
| AID197384 | Increase in serum prostaglandin I2 levels in incubated whole blood from rats, 1 hr following 1 mg/kg p.o. | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives. |
| AID203467 | Inhibition of serum TXB2 production after 45 minutes at 1.0 mg/kg intravenous dose | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Selective thromboxane synthetase inhibitors. 2. 3-(1H-imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogues. |
| AID183570 | Inhibition of thromboxane B2 production in whole blood of rats, 6 hr after a peroral dose of 1.0 mg/kg | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives. |
| AID221955 | Inhibition of ADP-induced platelet aggregation of human PRP in the presence of pig aortal microsomes (PAM) | 1992 | Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4 | 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. |
| AID215773 | Inhibition of TXA2 synthetase from human platelets | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Selective thromboxane synthetase inhibitors. 2. 3-(1H-imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogues. |
| AID183551 | Inhibition of thromboxane B2 production in whole blood of rat 15 min after intravenous injection of compound at 0.1 mg/kg | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives. |
| AID120751 | Protection against mortality in pulmonary thromboembolism model in mice at 12 mg/kg | 1992 | Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4 | 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. |
| AID221954 | Inhibition of ADP-induced platelet aggregation of human PRP without pig aortal microsomes (PAM) | 1992 | Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4 | 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. |
| AID117588 | Activity at 10 mg/kg given intravenously against mortality in a pulmonary thromboembolism model in mice (10 animals) at -18h following oral administration | 1989 | Journal of medicinal chemistry, Apr, Volume: 32, Issue:4 | [(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors. |
| AID183555 | Inhibition of thromboxane B2 production in whole blood of rat 45 min after intravenous injection of compound at 0.1 mg/kg | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives. |
| AID3093 | Inhibition of 11 beta-hydroxylase from rat adrenal gland | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Selective thromboxane synthetase inhibitors. 2. 3-(1H-imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogues. |
| AID183563 | Inhibition of thromboxane B2 production in whole blood of rat 75 min after intravenous injection of compound at 0.1 mg/kg | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives. |
| AID117591 | Activity at 10 mg/kg given intravenously against mortality in a pulmonary thromboembolism model in mice (10 animals) at -5h following oral administration | 1989 | Journal of medicinal chemistry, Apr, Volume: 32, Issue:4 | [(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors. |
| AID117586 | Time course of protection against mortality in a pulmonary thromboembolism model in mice after -5h | 1992 | Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4 | 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. |
| AID120753 | Protection against mortality in pulmonary thromboembolism model in mice at 1 mg/kg | 1992 | Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4 | 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. |
| AID117585 | Time course of protection against mortality in a pulmonary thromboembolism model in mice after -3h | 1992 | Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4 | 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. |
| AID120760 | Protection against mortality in pulmonary thromboembolism model in mice at 9 mg/kg | 1992 | Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4 | 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. |
| AID183566 | Inhibition of thromboxane B2 production in whole blood of rats, 3h after a peroral dose of 1.0 mg/kg | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives. |
| AID155523 | Inhibition of PGI-2 synthetase from porcine aorta | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Selective thromboxane synthetase inhibitors. 2. 3-(1H-imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogues. |
| AID117587 | Time course of protection against mortality in a pulmonary thromboembolism model in mice after -7h | 1992 | Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4 | 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. |
| AID203466 | Inhibition of serum TXB2 production after 45 minutes at 0.3 mg/kg intravenous dose | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Selective thromboxane synthetase inhibitors. 2. 3-(1H-imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogues. |
| AID161164 | Inhibition of Prostaglandin G/H synthase from ram seminal vesicle microsomes | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Selective thromboxane synthetase inhibitors. 2. 3-(1H-imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogues. |
| AID120755 | Protection against mortality in pulmonary thromboembolism model in mice at 30 mg/kg | 1992 | Journal of medicinal chemistry, Feb-21, Volume: 35, Issue:4 | 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. |
| AID117593 | Activity at 10 mg/kg given intravenously against mortality in a pulmonary thromboembolism model in mice (9 animals) at -3h following oral administration | 1989 | Journal of medicinal chemistry, Apr, Volume: 32, Issue:4 | [(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors. |
| AID210470 | Activity against human platelet microsome Thromboxane synthase | 1997 | Journal of medicinal chemistry, Oct-10, Volume: 40, Issue:21 | Thromboxane modulating agents. 3. 1H-imidazol-1-ylalkyl- and 3-pyridinylalkyl-substituted 3-[2-[(arylsulfonyl)amino]ethyl]benzenepropanoic acid derivatives as dual thromboxane synthase inhibitor/thromboxane receptor antagonists. |
| AID203338 | Inhibition of serum TXB2 production after 15 minutes at 0.3 mg/kg intravenous dose | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Selective thromboxane synthetase inhibitors. 2. 3-(1H-imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogues. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 117 (60.31) | 18.7374 |
| 1990's | 62 (31.96) | 18.2507 |
| 2000's | 5 (2.58) | 29.6817 |
| 2010's | 4 (2.06) | 24.3611 |
| 2020's | 6 (3.09) | 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 weak demand-to-supply ratio for research on this compound.
| This Compound (9.09) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 9 (4.35%) | 5.53% |
| Reviews | 2 (0.97%) | 6.00% |
| Case Studies | 1 (0.48%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 195 (94.20%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||