bretazenil: RN given for (S) isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 107926 |
| CHEMBL ID | 366947 |
| SCHEMBL ID | 124595 |
| MeSH ID | M0154150 |
| Synonym |
|---|
| PDSP1_000566 |
| bretazenil |
| ro-16-6028 |
| ro-16-6028/000 |
| bretazenil [usan:inn] |
| 9h-imidazo(1,5-a)pyrrolo(2,1-c)(1,4)benzodiazepine-1-carboxylic acid, 8-bromo-11,12,13,13a-tetrahydro-9-oxo-, 1,1-dimethylethyl ester, (s)- |
| bretazenilum [inn-latin] |
| ro 16-6028 |
| brn 4765855 |
| tert-butyl (s)-8-bromo-11,12,13,13a-tetrahydro-9-oxo-9h-imidazo(1,5-a)pyrrolo(2,1-c)(1,4)benzodiazepine-1-carboxylate |
| bretazenil (usan/inn) |
| D03155 |
| 84379-13-5 |
| PDSP2_000564 |
| NCGC00160640-01 |
| NCGC00160640-02 |
| bdbm50083908 |
| CHEMBL366947 , |
| ro-166028000 |
| ro 16-6028/000 |
| 8-bromo-7-oxo-3b,4,5,6-tetrahydro-7h-2,6a,11b-triaza-benzo[g]cyclopenta[e]azulene-3-carboxylic acid tert-butyl ester |
| dtxsid6046266 , |
| cas-84379-13-5 |
| tox21_111947 |
| dtxcid4026266 |
| bretazenilum |
| osz0e9dgoj , |
| unii-osz0e9dgoj |
| AKOS015896668 |
| gtpl4146 |
| bretazenil [usan] |
| ro-f61816-6028/000 |
| bretazenil [inn] |
| tert-butyl (s)-8-bromo-11,12,13,13a-tetrahydro-9-oxo-9h-imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylate |
| SCHEMBL124595 |
| tox21_111947_1 |
| NCGC00160640-03 |
| ES-0044 |
| tert.butyl (s)-8-bromo-11,12,13,13a-tetrahydro-9-oxo-9h-imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylate |
| LWUDDYHYYNNIQI-ZDUSSCGKSA-N |
| (13as)-8-bromo-11,12,13,13a-tetrahydro-9-oxo-9h-imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylic acid 1,1-dimethylethyl ester |
| 1-bretazenil |
| bretazenil, >=96% (hplc), solid |
| AC-8829 |
| sr-01000944937 |
| SR-01000944937-1 |
| Q4961977 |
| HMS3677P18 |
| BCP09629 |
| HMS3413P18 |
| ro 16-6028; ro 16-6028/000 |
| (13as)-tert-butyl 8-bromo-9-oxo-11,12,13,13a-tetrahydro-9h-benzo[e]imidazo[5,1-c]pyrrolo[1,2-a][1,4]diazepine-1-carboxylate |
| tert-butyl (s)-8-bromo-9-oxo-11,12,13,13a-tetrahydro-9h-benzo[e]imidazo[5,1-c]pyrrolo[1,2-a][1,4]diazepine-1-carboxylate |
| tert-butyl (7s)-14-bromo-12-oxo-2,4,11-triazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(17),3,5,13,15-pentaene-5-carboxylate |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Bretazenil has been well-characterized as a partial benzodiazepine agonist and zolpidem as benzodiazepine-receptor-subtype selective; the present results are consistent with their partial or selective agonist effects in those other paradigms." | ( Drug discrimination analysis of midazolam under a three-lever procedure. II: Differential effects of benzodiazepine receptor agonists. Ator, NA; Sannerud, CA, 1995) | 1.01 |
Bretazenil did not produce 25% potentiation even at receptor saturation. It did not suppress the response rates which is consistent with previous studies.
| Excerpt | Reference | Relevance |
|---|---|---|
| "That bretazenil did not produce acute physical dependence supports the findings of others (20,23) who report that chronic administration of bretazenil does not result in physical dependence." | ( Chlordiazepoxide, but not bretazenil, produces acute dependence, as evidenced by disruptions in schedule-controlled behavior. Bronson, ME, 1994) | 1.04 |
| "Bretazenil did not produce 25% potentiation even at receptor saturation." | ( Relationship between benzodiazepine receptor occupancy and potentiation of gamma-aminobutyric acid-stimulated chloride flux in vitro of four ligands of differing intrinsic efficacies. Facklam, M; Haefely, WE; Schoch, P, 1992) | 1 |
| "Bretazenil did not suppress the response rates which is consistent with previous studies reporting a lack of sedative and muscle-relaxant effects of bretazenil." | ( The pentylenetetrazole-cue antagonist actions of bretazenil (Ro 16-6028) as compared to midazolam. Järbe, TU; Rijnders, HJ; Slangen, JL, 1991) | 1.26 |
The pharmacokinetic and pharmacodynamic interactions of ethanol with the full benzodiazepine agonist midazolam, the partial agonist bretazenil and the selective agonist zolpidem have been determined in the rat in vivo. There were no consistent indications for synergistic, supra-additive pharmacodynamics interactions between alcohol and bretzenil or diazepam.
| Excerpt | Reference | Relevance |
|---|---|---|
| "The pharmacokinetic and pharmacodynamic interactions between the benzodiazepine agonist midazolam, on one hand, and the partial agonist bretazenil and inverse agonist Ro 19-4603, on the other, were characterized in vivo in rats using effect parameters derived from quantitative EEG analysis." | ( In vivo modeling of the pharmacodynamic interaction between benzodiazepines which differ in intrinsic efficacy. Danhof, M; Kuck, MT; Mandema, JW, 1992) | 0.49 |
| " There were no consistent indications for synergistic, supra-additive pharmacodynamic interactions between alcohol and bretazenil or diazepam." | ( Pharmacokinetic and pharmacodynamic interactions of bretazenil and diazepam with alcohol. Breimer, DD; Cohen, AF; Gieschke, R; Pieters, MS; Roncari, G; Schoemaker, RC; Tuk, B; van Steveninck, AL, 1996) | 0.75 |
| "The pharmacokinetic and pharmacodynamic interactions of ethanol with the full benzodiazepine agonist midazolam, the partial agonist bretazenil and the benzodiazepine BZ1 receptor subtype selective agonist zolpidem have been determined in the rat in vivo, using an integrated pharmacokinetic-pharmacodynamic approach." | ( Mechanism-based pharmacodynamic modeling of the interaction of midazolam, bretazenil, and zolpidem with ethanol. Danhof, M; Tuk, B; van Gool, T, 2002) | 0.75 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Drug discrimination was used to examine the behavioral effects of L-838,417 and bretazenil, two low efficacy positive GABAA modulators that act at benzodiazepine sites, alone and in combination with benzodiazepines and a neuroactive steroid (alfaxolone)." | ( Differential behavioral effects of low efficacy positive GABAA modulators in combination with benzodiazepines and a neuroactive steroid in rhesus monkeys. France, CP; McMahon, LR, 2006) | 0.56 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The effects of the CCKB receptor antagonists L-365,260, CI-988 and L-740,093, a new compound with improved bioavailability and CNS penetration, were assessed for anxiolytic-like effects in three rat anxiolytic screens sensitive to benzodiazepines, the elevated plus maze (EPM), conditioned suppression of drinking (CSD) and conditioned emotional response (CER) tests." | ( Lack of effect of CCKB receptor antagonists in ethological and conditioned animal screens for anxiolytic drugs. Curnow, R; Dawson, GR; Iversen, SD; Rupniak, NM; Stanhope, KJ; Tricklebank, MD; Tye, S, 1995) | 0.29 |
| "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 |
|---|---|---|
| " Two of these animals died prematurely following treatment at the initial dosing levels of 80 and 55 mg/kg/day; one of these two dogs was asymptomatic and in good general condition until death." | ( Vascular toxicity in dogs associated with overdoses of a novel benzodiazepine receptor partial agonist. Roncari, G; Schlaeppi, B; Zahm, P, 1991) | 0.28 |
| " The dose-response curve produced by Ro 16-6028 was flatter than that for Ro 17-1812, however." | ( Further investigation of the stimulus properties of chlordiazepoxide and zolpidem. Agonism and antagonism by two novel benzodiazepines. Sanger, DJ, 1987) | 0.27 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 0.1585 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 9.5205 | 0.1737 | 34.3047 | 61.8120 | AID1346859 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 9.5205 | 0.1737 | 34.3047 | 61.8120 | AID1346859 |
| TDP1 protein | Homo sapiens (human) | Potency | 33.4983 | 0.0008 | 11.3822 | 44.6684 | AID686978 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 3.1748 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224893 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 21.6843 | 0.0123 | 7.9835 | 43.2770 | AID1346984; AID1645841 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 0.0952 | 0.0002 | 14.3764 | 60.0339 | AID720692 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 17.2983 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID1159531 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 27.6227 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224848; AID1224849; AID1259401; AID1259403 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 14.5911 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982; AID1346985 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 9.5205 | 0.0002 | 29.3054 | 16,493.5996 | AID743069 |
| G | Vesicular stomatitis virus | Potency | 4.3649 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 13.3322 | 0.0237 | 23.2282 | 63.5986 | AID743222 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 21.1317 | 0.0007 | 23.0674 | 1,258.9301 | AID743085 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 1.2850 | 0.0391 | 47.5451 | 146.8240 | AID1224845; AID1224896 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 29.8470 | 0.0006 | 27.2152 | 1,122.0200 | AID743202 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 31.6228 | 0.2512 | 15.8432 | 39.8107 | AID504327 |
| Interferon beta | Homo sapiens (human) | Potency | 4.3649 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 4.3649 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 4.3649 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 4.3649 | 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) |
|---|---|---|---|---|---|---|---|
| Gamma-aminobutyric acid receptor subunit alpha-1 | Homo sapiens (human) | Ki | 0.0003 | 0.0000 | 0.2108 | 5.6234 | AID72927 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Homo sapiens (human) | Ki | 0.0029 | 0.0000 | 0.1881 | 9.0000 | AID71266; AID72927; AID73089; AID73244; AID73523 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Homo sapiens (human) | Ki | 0.0029 | 0.0001 | 0.2076 | 9.0000 | AID71266; AID72927; AID73089; AID73244; AID73523 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Homo sapiens (human) | Ki | 0.0005 | 0.0001 | 0.2442 | 5.6234 | AID73523 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Homo sapiens (human) | Ki | 0.0002 | 0.0001 | 0.2515 | 5.6234 | AID73244 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Homo sapiens (human) | Ki | 0.0006 | 0.0001 | 0.2401 | 5.6234 | AID73089 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Homo sapiens (human) | Ki | 0.0127 | 0.0002 | 0.4119 | 9.0000 | AID71266 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID73244 | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-3-beta-3-gamma-2 | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach. |
| AID73523 | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-5-beta-3-gamma-2 | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach. |
| AID721184 | Displacement of [3F]FMZ from Wistar rat cerebellum GABAA receptor by competitive radioligand assay | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | The development of potential new fluorine-18 labelled radiotracers for imaging the GABA(A) receptor. |
| AID73089 | Binding affinity to human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-2-beta-3-gamma-2 | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach. |
| AID71266 | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-6-beta-3-gamma-2 | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach. |
| AID72927 | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-1-beta-3-gamma-2 | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 11 (11.58) | 18.7374 |
| 1990's | 49 (51.58) | 18.2507 |
| 2000's | 20 (21.05) | 29.6817 |
| 2010's | 9 (9.47) | 24.3611 |
| 2020's | 6 (6.32) | 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 strong demand-to-supply ratio for research on this compound.
| This Compound (46.27) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 8 (7.92%) | 5.53% |
| Reviews | 3 (2.97%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 90 (89.11%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||