Azelnidipine is a dihydropyridine calcium channel blocker that is used to treat hypertension. It is a potent and selective inhibitor of the L-type calcium channel. Azelnidipine is well absorbed after oral administration and has a long half-life. It is metabolized in the liver and excreted in the urine. Azelnidipine has been shown to be effective in lowering blood pressure and improving symptoms of hypertension. It is generally well tolerated, although it can cause side effects such as dizziness, headache, and flushing. Azelnidipine is studied due to its potential to provide better blood pressure control and reduce the risk of cardiovascular events. It has shown promise in treating patients with resistant hypertension. Researchers are also exploring its potential therapeutic benefits in conditions such as heart failure and stroke. '
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azelnidipine: structure given in first source
ID Source | ID |
---|---|
PubMed CID | 65948 |
CHEMBL ID | 1275868 |
CHEBI ID | 31247 |
SCHEMBL ID | 49021 |
MeSH ID | M0170975 |
Synonym |
---|
AC-2151 |
AKOS015841674 |
rs-9054 |
cs-905 |
azelnidipine |
calblock |
3-[1-(diphenylmethyl)azetidin-3-yl] 5-(1-methylethyl) 2-amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
3,5-pyridinedicarboxylic acid, 1,4-dihydro-2-amino-6-methyl-4-(3-nitrophenyl)-, 3-(1-(diphenylmethyl)-3-azetidinyl) 5-(1-methylethyl) ester, (+-)- |
3,5-pyridinedicarboxylic acid, 1,4-dihydro-2-amino-6-methyl-4-(3-nitrophenyl)-, 3-(1-(diphenylmethyl)-3-azetidinyl)-5-(1-methylethyl) esster, (+-)- |
cs 905 |
azelnidipine [inn] |
3,5-pyridinedicarboxylic acid, 2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-, 3-(1-(diphenylmethyl)-3-azetidinyl) 5-(1-methylethyl) ester, (+-)- |
c33h34n4o6 |
3-(1-(diphenylmethyl)-3-azetidinyl) 5-isopropyl (+-)-2-amino-1,4-dihydro-6-methyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate |
D01145 |
123524-52-7 |
azelnidipine (jp17/inn) |
calblock (tn) |
NCGC00167436-01 |
3-o-(1-benzhydrylazetidin-3-yl) 5-o-propan-2-yl 2-amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
FT-0655294 |
o3-(1-benzhydrylazetidin-3-yl) o5-isopropyl 2-amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate;azelnidipine |
A805113 |
unii-pv23p19yug |
ccris 8650 |
pv23p19yug , |
CHEMBL1275868 |
cas-123524-52-7 |
dtxcid50120 |
tox21_112440 |
dtxsid3020120 , |
BCP9000370 |
3-(1-benzhydrylazetidin-3-yl) 5-isopropyl 2-amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
HY-B0023 |
BCPP000357 |
2-amino-1,4-dihydro-6-methyl-4-(3 nitrophenyl)-3,5-pyridinedicarboxylic acid 3-[1-(diphenylmethyl)-3-azetidinyl] 5-(1-methylethyl) ester |
PB24693 |
CS-0949 |
S3053 |
SCHEMBL49021 |
tox21_112440_1 |
NCGC00167436-02 |
KS-1248 |
azelnidipine [jan] |
azelnidipine [mart.] |
azelnidipine [who-dd] |
azelnidipine [mi] |
3-(1-(diphenylmethyl)-3-azetidinyl) 5-isopropyl (+/-)-2-amino-1,4-dihydro-6-methyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate |
2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 3-(1-diphenylmethylazetidin-3-yl)ester 5-isopropyl ester |
ZKFQEACEUNWPMT-UHFFFAOYSA-N |
(+/-)-2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 3-(1-diphenylmethylazetidin-3-yl) ester 5-isopropyl ester |
Q-200664 |
2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 3-[1-(diphenylmethyl)-3-azetidinyl] 5-isopropyl ester |
3-[1-(diphenylmethyl)-3-azetidinyl] 5-isopropyl 2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate |
AB01565841_02 |
DB09230 |
mfcd00865803 |
azelnidipine, >=98% (hplc), powder |
SR-01000944916-1 |
sr-01000944916 |
CHEBI:31247 |
HMS3651D18 |
SW219236-1 |
Q4832365 |
3,5-pyridinedicarboxylic acid, 2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-, 3-[1-(diphenylmethyl)-3-azetidinyl] 5-(1-methylethyl) ester |
AMY22122 |
HMS3885M05 |
CCG-270140 |
Azelnidipine (ALP) is a dihydropyridine calcium channel blocker and has been approved for use as an antihypertensive drug. It is a unique calcium blocker which does not increase heart rate.
Azelnidipine has been recognized in vascular remodeling. It has greater beneficial effects on the autonomic functions than benidipines. Azelnidipsine appears to have been responsible for the chyloperitoneum.
Azelnidipine may inhibit nitrotyrosine expression and cell damage caused by overproduction of nitric oxide.
Excerpt | Reference | Relevance |
---|---|---|
"Azelnidipine may increase PTC blood flow and improve renal hypoxia and tubulointerstitial injury induced by AII infusion." | ( Azelnidipine exerts renoprotective effects by improvement of renal microcirculation in angiotensin II infusion rats. Fujimoto, S; Horike, H; Kashihara, N; Nagasu, H; Sasaki, T; Satoh, M, 2009) | 3.24 |
"Azelnidipine may inhibit nitrotyrosine expression and cell damage caused by overproduction of nitric oxide, suggesting a mechanism for its cardiovascular protective effect." | ( Comparative effects of azelnidipine and other Ca2+-channel blockers on the induction of inducible nitric oxide synthase in vascular smooth muscle cells. Iida, H; Imuta, H; Jo, T; Kishida, S; Ma, J; Meguro, K; Morita, T; Nagai, R; Nakajima, T; Oonuma, H; Takano, H; Wang, GQ, 2006) | 1.37 |
Azelnidipine treatment in drug-naïve (DN) cases significantly decreased systolic blood pressure (SBP), diastolicBlood pressure (DBP) and heart rate (HR) Treatment with azelnodipine (5 microg/kg/min i.v., 10 min) had no effect on basal MAP, RBF, RVR, or PTC erythrocyte velocity.
Excerpt | Reference | Relevance |
---|---|---|
" The incidence of adverse events was similar in the O/A combination groups and the monotherapy groups." | ( A randomized, double-blind, four-arm parallel-group study of the efficacy and safety of azelnidipine and olmesartan medoxomil combination therapy compared with each monotherapy in Japanese patients with essential hypertension: the REZALT study. Kuramoto, K; Ogihara, T; Saruta, T; Shimada, K, 2009) | 0.58 |
The effects of olmesartan medoxomil and azelnidipine were modestly correlated with pharmacokinetic profiles. The pre-treatment PRA level could be a useful determinant of responsiveness in selecting the drugs.
Azelnidipine, dihydropyridine based calcium channel blocker has been used for treating ischemic heart disease and cardiac remodeling after myocardial infarction. The main challenge was the poor bioavailability due to its poor aqueous solubility and first-pass effect.
We analyzed the self-measured home BP data (measured in the morning and at bedtime) from this 16-week prospective observational study. Azelnidipine was photosensitive and its photodegradation in Calblock® tablets was promoted by the change of the dosage form.
Class | Description |
---|---|
isopropyl ester | Any carboxylic ester resulting from the formal condensation of a carboxylic acid with the hydroxy group of propan-2-ol. |
[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) |
---|---|---|---|---|---|---|---|
phosphopantetheinyl transferase | Bacillus subtilis | Potency | 89.1251 | 0.1413 | 37.9142 | 100.0000 | AID1490 |
hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 14.2685 | 3.1890 | 29.8841 | 59.4836 | AID1224846; AID1224894 |
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 22.8847 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
Fumarate hydratase | Homo sapiens (human) | Potency | 31.6228 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
USP1 protein, partial | Homo sapiens (human) | Potency | 44.6684 | 0.0316 | 37.5844 | 354.8130 | AID504865 |
TDP1 protein | Homo sapiens (human) | Potency | 24.3464 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
GLI family zinc finger 3 | Homo sapiens (human) | Potency | 30.7337 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
AR protein | Homo sapiens (human) | Potency | 23.8289 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID743035; AID743036; AID743053; AID743054; AID743063 |
caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 33.4915 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 23.3174 | 0.0006 | 57.9133 | 22,387.1992 | AID1259377; AID1259378 |
nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 32.2774 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224839; AID1224893 |
progesterone receptor | Homo sapiens (human) | Potency | 25.1567 | 0.0004 | 17.9460 | 75.1148 | AID1346784; AID1346795 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 0.6918 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 9.1777 | 0.0002 | 14.3764 | 60.0339 | AID720691; AID720692; AID720719 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 23.8150 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 12.5015 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID1159531 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 26.1087 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403 |
farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 28.7650 | 0.3758 | 27.4851 | 61.6524 | AID743217; AID743220; AID743239 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 8.2594 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982; AID1346985 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 23.6973 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID743069; AID743075; AID743077; AID743078; AID743079; AID743080; AID743091 |
G | Vesicular stomatitis virus | Potency | 1.9497 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 9.7717 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
polyprotein | Zika virus | Potency | 31.6228 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 20.0854 | 0.0010 | 24.5048 | 61.6448 | AID743212; AID743227 |
peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 19.2064 | 0.0010 | 19.4141 | 70.9645 | AID743094; AID743140; AID743191 |
vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 23.9145 | 0.0237 | 23.2282 | 63.5986 | AID743223 |
caspase-3 | Homo sapiens (human) | Potency | 33.4915 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 3.3491 | 0.0007 | 23.0674 | 1,258.9301 | AID743085 |
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 29.8493 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 21.5913 | 0.0016 | 28.0151 | 77.1139 | AID1224843; AID1224895 |
activating transcription factor 6 | Homo sapiens (human) | Potency | 30.1065 | 0.1434 | 27.6121 | 59.8106 | AID1159516 |
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 15.0890 | 19.7391 | 45.9784 | 64.9432 | AID1159509 |
v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 15.0890 | 0.0578 | 21.1097 | 61.2679 | AID1159526 |
Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 55.1965 | 0.0391 | 47.5451 | 146.8240 | AID1224845; AID1224896 |
Caspase-7 | Cricetulus griseus (Chinese hamster) | Potency | 33.4915 | 0.0067 | 23.4960 | 68.5896 | AID1346980 |
caspase-3 | Cricetulus griseus (Chinese hamster) | Potency | 33.4915 | 0.0067 | 23.4960 | 68.5896 | AID1346980 |
thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 4.4703 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
heat shock protein beta-1 | Homo sapiens (human) | Potency | 16.0822 | 0.0420 | 27.3789 | 61.6448 | AID743210; AID743228 |
nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 14.5357 | 0.0006 | 27.2152 | 1,122.0200 | AID743202; AID743219 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 35.4813 | 0.0079 | 8.2332 | 1,122.0200 | AID2546; AID2551 |
geminin | Homo sapiens (human) | Potency | 27.3171 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 25.5748 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 26.6032 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
Interferon beta | Homo sapiens (human) | Potency | 8.4108 | 0.0033 | 9.1582 | 39.8107 | AID1347407; AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 1.9497 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 12.7755 | 0.0023 | 19.5956 | 74.0614 | AID651631; AID720552 |
Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 26.6032 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 1.9497 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 13.3332 | 0.0119 | 17.9420 | 71.5630 | AID651632; AID720516 |
Ataxin-2 | Homo sapiens (human) | Potency | 13.3332 | 0.0119 | 12.2221 | 68.7989 | AID651632 |
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] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
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. |
AID1508629 | Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
AID1508628 | Confirmatory 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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1508627 | Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
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. |
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. |
AID537133 | Antileishmanial activity against promastigotes of Leishmania major MHOM/1L/80/Fredlin after 18 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID537132 | Antileishmanial activity against promastigotes of Leishmania amazonensis WHO/BR/00/LT0016 after 18 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID537131 | Antileishmanial activity against amastigotes of Leishmania chagasi MHOM/BR/1972/LD after 24 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID537138 | Selectivity index, ratio of IC50 for rhesus monkey LLC-MK2 cells to IC50 for trypomastigotes of Trypanosoma cruzi | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID640615 | Clearance in human liver microsomes at 1 uM measured after 60 mins by HPLC analysis | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Capture hydrolysis signals in the microsomal stability assay: molecular mechanisms of the alkyl ester drug and prodrug metabolism. |
AID537136 | Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID537137 | Selectivity index, ratio of IC50 for rhesus monkey LLC-MK2 cells to IC50 for amastigotes of Leishmania chagasi MHOM/BR/1972/LD | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID537139 | Cytotoxicity in BALB/c mouse erythrocytes assessed as hemolysis at 50 uM after 3 hrs | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID537135 | Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID537134 | Antileishmanial activity against promastigotes of Leishmania braziliensis MHO/BR/75/M2903 after 18 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
AID537130 | Antileishmanial activity against promastigotes of Leishmania chagasi MHOM/BR/1972/LD after 18 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 2 (1.03) | 18.7374 |
1990's | 7 (3.61) | 18.2507 |
2000's | 77 (39.69) | 29.6817 |
2010's | 94 (48.45) | 24.3611 |
2020's | 14 (7.22) | 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 very strong demand-to-supply ratio for research on this compound.
| This Compound (57.09) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 49 (24.75%) | 5.53% |
Reviews | 8 (4.04%) | 6.00% |
Case Studies | 2 (1.01%) | 4.05% |
Observational | 2 (1.01%) | 0.25% |
Other | 137 (69.19%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |