Bopindolol is a non-selective beta blocker that was initially developed for the treatment of hypertension. It has been shown to exhibit both beta-adrenergic blocking activity and partial agonist activity at serotonin 5-HT1A receptors. Bopindolol has been studied for its potential therapeutic effects in conditions such as hypertension, anxiety, and depression. Its unique pharmacological profile has led to interest in its potential use in treating various cardiovascular and neuropsychiatric disorders. However, bopindolol has not been widely used in clinical practice due to concerns about its side effects and the availability of other more effective medications.'
bopindolol: RN given refers to cpd without isomeric designation [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
bopindolol : A racemate comprising of equal amounts of (R)-bopindolol and (S)-bopindolol. It is a non-selective antagonist of beta1- and beta2-adrenoceptors and a prodrug in which the ester group is hydrolysed to form the corresponding hydroxy derivative. [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]
1-(tert-butylamino)-3-[(2-methyl-1H-indol-4-yl)oxy]propan-2-yl benzoate : A methylindole that is 2-methyl-1H-indol-4-ol in which the hydrogen of the hydroxy group is replaced by a 2-(benzoyloxy)-3-(tert-butylamino)propyl group. [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]
ID Source | ID |
---|---|
PubMed CID | 44112 |
CHEMBL ID | 357995 |
CHEBI ID | 143782 |
SCHEMBL ID | 49500 |
MeSH ID | M0109948 |
Synonym |
---|
AB01275452-01 |
lt-31200 |
bopindolol |
62658-63-3 |
2-[(1,1-dimethylethyl)amino]-1-{[(2-methyl-1h-indol-4-yl)oxy]methyl}ethyl benzoate |
(+-)-1-(tert-butylamino)-3-((2-methylindol-4-yl)oxy)-2-propanol benzoate (ester) |
(+-)-1-((1,1-dimethylethyl)amino)-3-((2-methyl-1h-indol-4-yl)oxy)-2-propanol benzoate (ester) |
(+-)-4-(2-benzoyloxy-3-tert-butylaminopropoxy)-2-methylindole |
(+-)-bopindolol |
bopindololum [inn-latin] |
D07537 |
bopindolol (inn) |
sandonorm (tn) |
NCGC00163155-01 |
c23h28n2o3 |
2-propanol, 1-((1,1-dimethylethyl)amino)-3-((2-methyl-1h-indol-4-yl)oxy)-, benzoate (ester), (+-)- |
L013383 |
HMS2089O20 |
CHEMBL357995 |
DB08807 |
[1-(tert-butylamino)-3-[(2-methyl-1h-indol-4-yl)oxy]propan-2-yl] benzoate |
FT-0663594 |
CHEBI:143782 |
1-(tert-butylamino)-3-[(2-methyl-1h-indol-4-yl)oxy]propan-2-yl benzoate |
NCGC00163155-02 |
dtxcid402684 |
dtxsid6022684 , |
cas-62658-63-3 |
tox21_112017 |
2-propanol, 1-[(1,1-dimethylethyl)amino]-3-[(2-methyl-1h-indol-4-yl)oxy]-, benzoate (ester) |
1-(tert-butylamino)-3-((2-methyl-1h-indol-4-yl)oxy)propan-2-yl benzoate |
AKOS016014321 |
bopindolol [inn] |
bopindololum |
unii-kt304vzo57 |
kt304vzo57 , |
smr001550598 |
bopindolol, bopindolol maleate |
MLS003882860 |
(+/-)-1-(tert-butylamino)-3-((2-methylindol-4-yl)oxy)-2-propanol benzoate (ester) |
bopindolol [mi] |
1-((1,1-dimethylethyl)amino)-3-((2-methyl-1h-indol-4-yl)oxy)-2-propanol benzoate ester |
bopindolol [who-dd] |
SCHEMBL49500 |
tox21_112017_1 |
NCGC00263654-01 |
4-(2-benzoyloxy-3-tert.butylaminopropoxy)-2-methyl-indole |
2-(tert-butylamino)-1-{[(2-methyl-1h-indol-4-yl)oxy]methyl}ethyl benzoate |
tox21 112017 |
sr-05000001453 |
SR-05000001453-1 |
4-(2-benzoyloxy-3-t-butylamino-propoxy) -2-methyl indole |
1-(tert-butylamino)-3-(2-methyl-1h-indol-4-yloxy)propan-2-yl benzoate |
rac bopindolol |
Q834660 |
(+/-)-bopindolol |
A922919 |
()-bopindolol |
CS-0013446 |
HY-B1562 |
racbopindolol-d9 |
Bopindolol is a nonselective beta-adrenoceptor antagonist [corrected] with partial agonist activity which is used in the treatment of hypertension. It has a long duration of action and antihypertensive properties at low dosage.
Excerpt | Reference | Relevance |
---|---|---|
"Bopindolol has beta-blocking effects for 96 hr despite a 4-hr t1/2. " | ( Simultaneous modeling of bopindolol kinetics and dynamics. Galeazzi, RL; Niederberger, W; Platzer, R; Rosenthaler, J, 1984) | 2.01 |
Excerpt | Reference | Relevance |
---|---|---|
" The side-effect score for edema was lower with ISR plus diuretics than with other combinations, whereas the ACE inhibitor was associated with a higher score for cough." | ( Efficacy and safety of various combination therapies based on a calcium antagonist in essential hypertension: results of a placebo-controlled randomized trial. Lüscher, TF; Waeber, B, 1993) | 0.29 |
Steady-state pharmacokinetic parameters of the new, long-acting beta-adrenoceptor blocker bopindolol have been measured in 17 young and 20 elderly men.
Excerpt | Reference | Relevance |
---|---|---|
" In two separate studies, each with 12 healthy male volunteers, the pharmacokinetic and dynamic properties of a transdermal delivery system for bopindolol were evaluated." | ( Pharmacokinetics and pharmacodynamics of a new transdermal delivery system for bopindolol. Drewe, J; Gyr, K; Kissel, T; Meier, R; Munzer, J; Thumshirn, M; Timonen, U, 1991) | 0.71 |
"Steady-state pharmacokinetic parameters of the new, long-acting beta-adrenoceptor blocker bopindolol have been measured in 17 young and 20 elderly healthy men." | ( Steady state pharmacokinetics of hydrolysed bopindolol in young and elderly men. Holmes, D; Houle, JM; Nuesch, E; Rosenthaler, J, 1991) | 0.76 |
" In pharmacokinetic terms, however, these drugs show no pronounced difference in their elimination half-life (ranging between 4 and 8 h)." | ( Pharmacodynamic models of various beta blockers: an explanation for the long duration of action of bopindolol. Grevel, J, 1986) | 0.49 |
Excerpt | Reference | Relevance |
---|---|---|
"The antihypertensive effect and safety of treatment of hypertension with isradipine, a Ca antagonist of dihydropyridine group in monotherapy and in combination with the betablocker bopindolol was assessed in a multicentre study joined by six Czechoslovak centres." | ( Isradipine in monotherapy and in combination with bopindolol: results of a 3-month multicentre study in hypertensives. Dvorák, I; Dzúrik, R; Fetkovská, N; Jonás, P; Kotlík, I; Markuljak, I; Petr, P; Widimský, J, 1990) | 0.72 |
Excerpt | Reference | Relevance |
---|---|---|
" Its bioavailability after oral administration amounts to about 70%." | ( Clinical pharmacological studies with the long-acting beta-adrenoceptor blocking drug bopindolol. Aellig, WH, 1986) | 0.49 |
" The absolute bioavailability of the active compound is about 70%." | ( Relationship between plasma concentrations and cardiac beta-adrenoceptor blockade--a study with oral and intravenous bopindolol. Aellig, WH; Engel, G; Grevel, J; Niederberger, W; Nüesch, E; Rosenthaler, J, 1986) | 0.48 |
"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 |
The clinical efficacy of bopindolol, a new, long-acting beta-adrenoceptor blocking drug, in a dosage of 1-2 mg daily was compared with that of atenolol (50-100 mg daily) in 33 patients with mild or moderate arterial hypertension. Blood pressure was reduced from 151 +/- 12/105 +/- 7 during placebo to 129 +/- 10/88 +/- 6 after bopinolol treatment.
Excerpt | Relevance | Reference |
---|---|---|
" If normalization of diastolic blood pressure (BP) had not been reached, the dosage was increased to 5 mg." | ( MIS (Multicentric Isradipine Study of antihypertensive therapy). Balazovjech, I; Dzúrik, R; Fetkovská, N; Kvasnicka, J; Lupínek, Z; Mayer, O; Pidrman, V; Widimský, J, 1992) | 0.28 |
" The patches showed a good local and systemic tolerability in both studies over a dosing interval of up to 7 days." | ( Pharmacokinetics and pharmacodynamics of a new transdermal delivery system for bopindolol. Drewe, J; Gyr, K; Kissel, T; Meier, R; Munzer, J; Thumshirn, M; Timonen, U, 1991) | 0.51 |
" The clinical relevance of the effects was not examined, but similar changes have been reported for other beta-blockers which did not appear to be clinically relevant and did not affect the dosage required to treat hypertension." | ( Steady state pharmacokinetics of hydrolysed bopindolol in young and elderly men. Holmes, D; Houle, JM; Nuesch, E; Rosenthaler, J, 1991) | 0.54 |
" The aim of this study was to define the optimal dosage of bopindolol in outpatients with mild to moderate hypertension and to compare it to atenolol in term of tolerance and efficacy, both administered once daily." | ( Dose-finding study with bopindolol in arterial hypertension. Peter, R; Siegenthaler, H; Willimann, P, 1986) | 0.82 |
"The clinical efficacy of bopindolol, a new, long-acting beta-adrenoceptor blocking drug, in a dosage of 1-2 mg daily was compared with that of atenolol (50-100 mg daily) in 33 patients with mild or moderate arterial hypertension who were treated for a total period of 12 months." | ( Evaluation of the antihypertensive effect of a beta-blocker with the aid of daily blood pressure profiles. Abetel, G; Genoud, G; Karly, M, 1986) | 0.57 |
" Within this dosage range, bopindolol itself had no significant effect on PRA." | ( Effect of bopindolol on renin secretion and renal excretory function in rats. Anderson, LA; Barrett, RJ; Proakis, AG; Taylor, DR; Wright, KF, 1989) | 0.98 |
" The dosage was increased every month up to 2 mg bopindolol and 200 mg atenolol." | ( Bopindolol and atenolol in patients with stable angina pectoris. Double-blind randomized comparative trial. Hertzeanu, H; Kellermann, JJ; Loidl, AF; Shemesh, J, 1989) | 1.97 |
" During a one-year treatment period following the comparative trial, the seven patients who had received bopindolol showed no evidence of tachyphylaxia, the blood-pressure remaining well controlled while the dosage was slightly reduced." | ( Bopindolol, a new long-acting beta-adrenoceptor antagonist--a randomized comparison against propranolol in hypertensive patients. Axthelm, T; Kirch, W, 1983) | 1.92 |
" In patients showing a decrease of the potassium plasma level, potassium sparing diuretic-amiloride should be added or the dosage of the drug should be halved." | ( [Treatment of hypertension with a fixed combination of bopindolol and chlorthalidone (Sandoretic)]. Balazovjech, I; Havlík, V; Havránek, P; Hulínský, V; Kroupa, E; Lánská, V; Nikodýmová, L; Pátek, F; Svihovcová, P; Svítil, F; Widimský, J, 1996) | 0.54 |
Class | Description |
---|---|
methylindole | Any member of the class of indoles carrying one or more methyl substituents. |
secondary amino compound | A compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups. |
aromatic ether | Any ether in which the oxygen is attached to at least one aryl substituent. |
benzoate ester | Esters of benzoic acid or substituted benzoic acids. |
[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] |
Pathway | Proteins | Compounds |
---|---|---|
Bopindolol Action Pathway | 47 | 8 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 13.3332 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521 |
TDP1 protein | Homo sapiens (human) | Potency | 22.7231 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
GLI family zinc finger 3 | Homo sapiens (human) | Potency | 8.4127 | 0.0007 | 14.5928 | 83.7951 | AID1259369 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 39.8107 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 21.1923 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 6.9178 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 27.2435 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159555 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 17.5424 | 0.0015 | 30.6073 | 15,848.9004 | AID1224848; AID1224849; AID1259403 |
G | Vesicular stomatitis virus | Potency | 3.4671 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 0.2455 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 15.8489 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 21.3784 | 0.0016 | 28.0151 | 77.1139 | AID1224843; AID1224895 |
potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 8.9125 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 26.6032 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 18.1056 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
Interferon beta | Homo sapiens (human) | Potency | 3.4671 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 3.4671 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 3.4671 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 3.4671 | 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) |
---|---|---|---|---|---|---|---|
Beta-2 adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 0.0200 | 0.0002 | 0.9326 | 7.2000 | AID625205 |
Beta-2 adrenergic receptor | Homo sapiens (human) | Ki | 0.0140 | 0.0000 | 0.6635 | 9.5499 | AID625205 |
Beta-1 adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 0.0470 | 0.0002 | 1.4681 | 9.0000 | AID625204 |
Beta-1 adrenergic receptor | Homo sapiens (human) | Ki | 0.0270 | 0.0001 | 1.3391 | 9.9840 | AID625204 |
Cytochrome P450 2D6 | Homo sapiens (human) | IC50 (µMol) | 5.4764 | 0.0000 | 2.0151 | 10.0000 | AID625249 |
Beta-3 adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 0.4580 | 0.0023 | 3.2415 | 8.0600 | AID625206 |
Beta-3 adrenergic receptor | Homo sapiens (human) | Ki | 0.3440 | 0.0030 | 2.3098 | 6.0450 | AID625206 |
5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.2670 | 0.0003 | 1.3833 | 8.4000 | AID625190 |
5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Ki | 0.1530 | 0.0001 | 0.7396 | 10.0000 | AID625190 |
5-hydroxytryptamine receptor 2A | Homo sapiens (human) | IC50 (µMol) | 1.5810 | 0.0001 | 0.8801 | 8.8500 | AID625192 |
5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 0.4520 | 0.0000 | 0.3855 | 10.0000 | AID625192 |
5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.2670 | 0.0005 | 1.4835 | 7.8000 | AID625190 |
5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | Ki | 0.1530 | 0.0003 | 1.2967 | 9.2440 | AID625190 |
5-hydroxytryptamine receptor 2B | Homo sapiens (human) | IC50 (µMol) | 1.5230 | 0.0001 | 1.1873 | 8.9125 | AID625217 |
5-hydroxytryptamine receptor 2B | Homo sapiens (human) | Ki | 0.9690 | 0.0003 | 0.7693 | 10.0000 | AID625217 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
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. |
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. |
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID547622 | Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease. |
AID547804 | Selectivity window, ratio of EC50 for BESM cells to EC50 for Trypanosoma cruzi amastigotes infected in BESM cells | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease. |
AID496765 | Modulation of neurological behavior in zebrafish assessed as prolongation of high intensity light-induced motor response at 10 to 100 uM by photomotor response assay | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Rapid behavior-based identification of neuroactive small molecules in the zebrafish. |
AID547621 | Cytotoxicity against BESM cells after 88 hrs by HTS assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease. |
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. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 56 (44.80) | 18.7374 |
1990's | 49 (39.20) | 18.2507 |
2000's | 6 (4.80) | 29.6817 |
2010's | 7 (5.60) | 24.3611 |
2020's | 7 (5.60) | 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 (25.08) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 49 (37.40%) | 5.53% |
Reviews | 6 (4.58%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 76 (58.02%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |