Efaroxan is a selective α2-adrenergic receptor antagonist. It is used in research to study the role of α2-adrenergic receptors in various physiological processes, including blood pressure regulation, neurotransmission, and pain perception. Efaroxan has been shown to have antihypertensive effects and to increase sympathetic nerve activity. It is also being investigated as a potential treatment for depression and other mental health disorders.'
efaroxan: RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 72016 |
| CHEMBL ID | 57895 |
| CHEBI ID | 93806 |
| SCHEMBL ID | 127096 |
| MeSH ID | M0173169 |
| Synonym |
|---|
| efaroxano [inn-spanish] |
| (+-)-2-(2-ethyl-2,3-dihydro-2-benzofuranyl)-2-imidazoline |
| efaroxanum [inn-latin] |
| SPECTRUM_001997 |
| BSPBIO_003306 |
| LOPAC0_000521 |
| efaroxan |
| NCGC00024793-03 |
| KBIOSS_002570 |
| KBIO3_002808 |
| KBIO2_005129 |
| KBIO2_007697 |
| KBIO2_002561 |
| SPECTRUM3_001863 |
| NCGC00024793-02 |
| HMS2089D15 |
| NCGC00015410-05 |
| CHEMBL57895 |
| nsc-759562 |
| L001351 |
| 2-(2-ethyl-3h-1-benzofuran-2-yl)-4,5-dihydro-1h-imidazole |
| NCGC00015410-04 |
| 89197-32-0 |
| cas-89197-32-0 |
| dtxcid6025149 |
| tox21_110139 |
| dtxsid8045149 , |
| CCG-204611 |
| NCGC00015410-06 |
| NCGC00015410-03 |
| efaroxan [inn:ban] |
| g00490l21h , |
| efaroxano |
| unii-g00490l21h |
| nsc 759562 |
| efaroxanum |
| 1h-imidazole, 2-(2-ethyl-2,3-dihydro-2-benzofuranyl)-4,5-dihydro- |
| 2-(2-ethyl-2,3-dihydro-2-benzofuranyl)-4,5-dihydro-1h-imidazole |
| efaroxan [inn] |
| (+/-)-2-(2-ethyl-2,3-dihydro-2-benzofuranyl)-2-imidazoline |
| SCHEMBL127096 |
| tox21_110139_1 |
| NCGC00015410-08 |
| tox21 110139 |
| RATZLMXRALDSJW-UHFFFAOYSA-N |
| 2-(2-ethyl-2,3-dihydro-1-benzofuran-2-yl)-4,5-dihydro-1h-imidazole |
| AB00918533_03 |
| CHEBI:93806 |
| MRF-0000021 |
| SBI-0050504.P002 |
| bdbm50179393 |
| FT-0725797 |
| Q5347187 |
| efaroxan (hydrochloride) |
| rx 821037 |
| BRD-A10739734-003-05-6 |
| SDCCGSBI-0050504.P003 |
| NCGC00015410-13 |
| 2-(2-ethyl-2,3-dihydrobenzofuran-2-yl)-4,5-dihydro-1h-imidazole |
Pretreatment with efaroxan (30 mumol/kg, i.v.) abolished the suppressive effects of agmatine on the enhanced renal sympathetic nerve activity during renal ischemia. Pretreatment with rauwolscine (a selective alpha(2)-adrenoceptor antagonist) inhibited the moxonidine-induced increases in ANP secretion and decrease in pulse pressure.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Pretreatment with efaroxan (30 mumol/kg, i.v.), an alpha(2)/I(1)-receptor antagonist, abolished the suppressive effects of agmatine on the enhanced renal sympathetic nerve activity during renal ischemia and on the elevated norepinephrine overflow after reperfusion, and eliminated the preventing effects of agmatine on the ischemia/reperfusion-induced renal dysfunction and histological damage." | ( Preventive mechanisms of agmatine against ischemic acute kidney injury in rats. Fujii, T; Hayashi, K; Kobuchi, S; Matsumura, Y; Sugiura, T; Takaoka, M; Tsutsui, H, 2009) | 0.68 |
| "Pretreatment with efaroxan, at a dose sufficient to inhibit I₁R activation, attenuated the action of allantoin." | ( Stimulatory effect of allantoin on imidazoline I₁ receptors in animal and cell line. Cheng, JT; Chiu, NH; Chung, HH; Hsu, CT; Lee, WJ; Yang, TT, 2012) | 0.7 |
| "Pretreatment with efaroxan (a selective I(1)-imidazoline receptor antagonist) or rauwolscine (a selective alpha(2)-adrenoceptor antagonist) inhibited the moxonidine-induced increases in ANP secretion and interstitial ANP concentration and decrease in pulse pressure." | ( Augmentation of moxonidine-induced increase in ANP release by atrial hypertrophy. Cao, C; Kang, CW; Kim, SH; Kim, SZ, 2004) | 0.65 |
| "Pretreatment with efaroxan antagonized moxonidine-induced suppression of norepinephrine levels." | ( Potential mechanisms of moxonidine-induced ocular hypotension: role of norepinephrine. Chu, TC; Ogidigben, MJ; Potter, DE; Socci, RR, 1997) | 0.62 |
| "Pretreatment with efaroxan (250 micro g) elicited significantly greater antagonism of the ocular hypotensive response to naphazoline than did rauwolscine (250 micro g) suggesting an involvement of imidazoline (I(1)) receptors." | ( Naphazoline-induced suppression of aqueous humor pressure and flow: involvement of central and peripheral alpha(2)/I(1) receptors. Chu, TC; Ogidigben, MJ; Potter, DE, 2001) | 0.63 |
| 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 |
|---|---|---|
| "We determined the relative potency of these drugs with respect to their effects on mean arterial pressure and heart rate by performing cumulative intravenous dose-response relationship studies in six conscious rabbits." | ( Relative importance of central imidazoline receptors for the antihypertensive effects of moxonidine and rilmenidine. Chan, CK; Head, GA, 1996) | 0.29 |
| " Dose-response curves were obtained for each drug individually; for morphine:clonidine at 1:3, 1:1, and 1:0." | ( Interaction of morphine and clonidine on gastrointestinal transit in mice. Pol, O; Puig, MM; Warner, W, 1996) | 0.29 |
| Class | Description |
|---|---|
| 1-benzofurans | A member of the class of benzofurans consisting of a 1-benzofuran skeleton and its substituted derivatives thereof. |
| [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) |
|---|---|---|---|---|---|---|---|
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 14.5750 | 0.0041 | 10.8903 | 31.5287 | AID493107 |
| GLS protein | Homo sapiens (human) | Potency | 3.5481 | 0.3548 | 7.9355 | 39.8107 | AID624146 |
| TDP1 protein | Homo sapiens (human) | Potency | 4.7318 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| AR protein | Homo sapiens (human) | Potency | 20.6354 | 0.0002 | 21.2231 | 8,912.5098 | AID743035; AID743036; AID743063 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 1.6865 | 0.0006 | 57.9133 | 22,387.1992 | AID1259377; AID1259378; AID1259394 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 0.4228 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 3.3491 | 0.0002 | 29.3054 | 16,493.5996 | AID1259383 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 13.8029 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 0.7519 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| D(1A) dopamine receptor | Homo sapiens (human) | Potency | 2.3108 | 0.0224 | 5.9449 | 22.3872 | AID488982 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 32.5548 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| geminin | Homo sapiens (human) | Potency | 11.8856 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 15.8489 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 6.5170 | 0.0023 | 19.5956 | 74.0614 | AID651631; AID720552 |
| [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) |
|---|---|---|---|---|---|---|---|
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 0.0278 | 0.0001 | 0.8074 | 10.0000 | AID1306485; AID36517 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 0.0513 | 0.0002 | 0.7257 | 10.0000 | AID36517 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | Ki | 0.0513 | 0.0003 | 0.4834 | 10.0000 | AID36517 |
| Nischarin | Homo sapiens (human) | Ki | 0.0591 | 0.0042 | 0.2192 | 3.8019 | AID223238; AID342861 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| 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. |
| 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. |
| 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. |
| AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
| AID223238 | Displacement of [125I]p-iodoclonidine from imidazoline receptor I-1 in rat pheochromocytoma cells | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Imidazoline binding sites (IBS) profile modulation: key role of the bridge in determining I1-IBS or I2-IBS selectivity within a series of 2-phenoxymethylimidazoline analogues. |
| AID1306485 | Displacement of [3H]RS-79948-197 from recombinant human alpha2A adrenoreceptor expressed in CHOK1 cell membrane by scintillation counting method | 2016 | Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14 | A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin. |
| AID223239 | Relative binding to imidazoline I-1 and alpha-2 adrenergic receptors (ratio of pKi) | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Imidazoline binding sites (IBS) profile modulation: key role of the bridge in determining I1-IBS or I2-IBS selectivity within a series of 2-phenoxymethylimidazoline analogues. |
| AID35771 | Compound was evaluated for Alpha-2 adrenergic receptor antagonist activity;no data | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | Synthesis and biological evaluation of new 2-(4,5-dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine derivatives. |
| AID342860 | Displacement of [125I]PIC from human alpha2 adrenoceptors expressed in CHO cells | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | QSAR study of imidazoline antihypertensive drugs. |
| AID342861 | Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | QSAR study of imidazoline antihypertensive drugs. |
| AID1306490 | Induction of apoptosis in human K562 cells assessed as early apoptotic cells at 300 uM up to 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry | 2016 | Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14 | A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin. |
| AID1306487 | Intrinsic activity at recombinant human alpha2A adrenoreceptor expressed in CHOK1 cell membrane incubated for 30 mins by [35S]GTPgammaS binding assay relative to adrenaline | 2016 | Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14 | A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin. |
| AID1306484 | Antiproliferative activity against human K562 cells assessed as inhibition of cell survival after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14 | A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin. |
| AID342863 | Selectivity ratio of pKi for human imidazoline receptor 1 to pKi for human alpha2 adrenoceptors | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | QSAR study of imidazoline antihypertensive drugs. |
| AID36517 | Displacement of [3H]-RX 821002 from Alpha-2 adrenergic receptors of rabbit white fat cell membranes | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11 | Imidazoline binding sites (IBS) profile modulation: key role of the bridge in determining I1-IBS or I2-IBS selectivity within a series of 2-phenoxymethylimidazoline analogues. |
| AID1306486 | Agonist activity at recombinant human alpha2A adrenoreceptor expressed in CHOK1 cell membrane incubated for 30 mins by [35S]GTPgammaS binding assay | 2016 | Bioorganic & medicinal chemistry, 07-15, Volume: 24, Issue:14 | A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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 (0.61) | 18.7374 |
| 1990's | 54 (32.93) | 18.2507 |
| 2000's | 66 (40.24) | 29.6817 |
| 2010's | 35 (21.34) | 24.3611 |
| 2020's | 8 (4.88) | 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 (23.39) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 2 (1.17%) | 5.53% |
| Reviews | 3 (1.75%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 166 (97.08%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||