Tepoxalin is a non-steroidal anti-inflammatory drug (NSAID) that has been studied for its potential to treat a variety of inflammatory conditions. Its synthesis involves a multi-step process that starts with the condensation of a ketone with an amine to form an imine, followed by a series of reactions to introduce the desired functional groups. Tepoxalin's mechanism of action is thought to involve the inhibition of cyclooxygenase (COX) enzymes, which are responsible for the production of prostaglandins, inflammatory mediators. It has shown promising results in preclinical studies for treating conditions like arthritis, inflammation associated with cancer, and osteoarthritis. Despite its potential, Tepoxalin has not yet been approved for clinical use due to concerns about its safety profile. Ongoing research is aimed at understanding the mechanism of action and optimizing its therapeutic window to improve its safety and efficacy.'
tepoxalin : A hydroxamic acid obtained by formal condensation of the carboxy group of 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)pyrazol-3-yl]propanoic acid with the amino group of N-methylhydroxylamine. It is used in veterinary medicine for the control of pain and inflammation caused by musculoskeletal disorders such as hip dysplasia and arthritis in dogs.
ID Source | ID |
---|---|
PubMed CID | 59757 |
CHEMBL ID | 316040 |
CHEBI ID | 76277 |
SCHEMBL ID | 75441 |
MeSH ID | M0197867 |
Synonym |
---|
chebi:76277 , |
CHEMBL316040 , |
zubrin |
rwj-20485 |
orf-20485 |
tepoxaline [french] |
tepoxalina [spanish] |
1h-pyrazole-3-propanamide, 5-(4-chlorophenyl)-n-hydroxy-1-(4-methoxyphenyl)-n-methyl- |
rwj 20485 |
3-(5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl)-n-hydroxy-n-methylpropanamide |
tepoxalin [usan:inn] |
tepoxalinum [latin] |
5-(p-chlorophenyl)-1-(p-methoxyphenyl)-n-methylpyrazole-3-propionohydroxamic acid |
tepoxalin |
103475-41-8 |
orf 20485 |
5-(4-chlorophenyl)-n-hydroxy-1-(4-methoxyphenyl)-n-methyl-1h-pyrazole-3-propanamide |
3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)pyrazol-3-yl]-n-hydroxy-n-methyl-propanamide |
tepoxalin (usan/inn) |
D06075 |
3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)pyrazol-3-yl]-n-hydroxy-n-methylpropanamide |
bdbm50001183 |
3-[5-(4-chloro-phenyl)-1-(4-methoxy-phenyl)-1h-pyrazol-3-yl]-n-hydroxy-n-methyl-propionamide |
C18362 |
tepoxalinum |
unii-tz4ox61974 |
tz4ox61974 , |
tepoxalina |
tepoxaline |
FT-0674859 |
BCP0726000210 |
CCG-213262 |
SCHEMBL75441 |
cas-103475-41-8 |
3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-1h-pyrazol-3-yl]-n-hydroxy-n-methylpropanamide |
dtxsid1057610 , |
NCGC00253573-01 |
tepoxaliume |
tox21_113717 |
dtxcid5031399 |
tepoxalin [mi] |
tepoxalin [mart.] |
tepoxalin [ema epar veterinary] |
tepoxalin [inn] |
tepoxalin [usan] |
tepoxalin [green book] |
XYKWNRUXCOIMFZ-UHFFFAOYSA-N |
3-(5-(4-chlorophenyl)-1-(4-methoxyphenyl)-1h-pyrazol-3-yl)-n-hydroxy-n-methylpropanamide |
AC-31487 |
AB01563016_01 |
J-000974 |
EX-A895 |
sr-01000944187 |
SR-01000944187-1 |
1h-pyrazole-3-propanamide, 5-(4-chlorophenyl)-n-hydroxy-1-(4-methoxyphenyl)-n-methyl-;1h-pyrazole-3-propanamide, 5-(4-chlorophenyl)-n-hydroxy-1-(4-methoxyphenyl)-n-methyl- |
AKOS032947222 |
orf-20485; orf20485; orf 20485; rwj-20485; rwj 20485; rwj20485 |
BCP23064 |
2-butyne-1,4-dioldiacetate |
F17424 |
DB11466 |
Q7701370 |
AMY23437 |
HY-13219 |
CS-0003182 |
tepoxalin (ema epar veterinary) |
zubrin rapidly-disintegrating tablets |
tepoxalinum (latin) |
tepoxalin (mart.) |
Tepoxalin is an NSAID approved for the treatment of arthritis in dogs in the United States. It is a potent inhibitor of both the cyclooxygenase and lipoxygen enzyme pathways of the arachidonic acid cascade.
Tepoxalin has an unique property as an NSAIDs that suppresses both cyclooxygenase and lipoxygen enzyme. Tepoxin has in vivo inhibitory activity against COX-1, COX -2, and 5-LOX in dogs at the current approved recommended dosage.
Excerpt | Reference | Relevance |
---|---|---|
"Tepoxalin has an unique property as an NSAIDs that suppresses both cyclooxygenase and lipoxygenase." | ( Pro-apoptotic effects of tepoxalin, a cyclooxygenase/lipoxygenase dual inhibitor, on canine synovial fibroblasts. Hosoya, K; Oh, N; Okumura, M; Sunaga, T; Takagi, S, 2012) | 1.4 |
"Tepoxalin has an unique property as an NSAIDs that suppresses both cyclooxygenase and lipoxygenase." | ( Pro-apoptotic effects of tepoxalin, a cyclooxygenase/lipoxygenase dual inhibitor, on canine synovial fibroblasts. Hosoya, K; Oh, N; Okumura, M; Sunaga, T; Takagi, S, 2012) | 1.4 |
"Tepoxalin has in vivo inhibitory activity against COX-1, COX-2, and 5-LOX in dogs at the current approved recommended dosage." | ( In vivo effects of tepoxalin, an inhibitor of cyclooxygenase and lipoxygenase, on prostanoid and leukotriene production in dogs with chronic osteoarthritis. Agnello, KA; Budsberg, SC; Reynolds, LR, 2005) | 2.1 |
Tepoxalin did not cause significant effects on renal function or cause hepatic injury in healthy dogs exposed to hypotension with isoflurane. N-acetyl-L-cysteine, which attenuated NF-kappaB activation, had no effect on leucocyte recruitment.
Excerpt | Reference | Relevance |
---|---|---|
"Tepoxalin did not cause significant effects on renal function or cause hepatic injury in healthy dogs exposed to hypotension with isoflurane, when administered pre- or postanesthetic and continued for five consecutive days." | ( Effect of tepoxalin on renal function and hepatic enzymes in dogs exposed to hypotension with isoflurane. Carregaro, AB; Freitas, GC; Lopes, C; Lopes, ST; Lukarsewski, R; Padilha, VS; Paim, FC, 2014) | 2.25 |
"Tepoxalin did not inhibit radiation-induced NF-kappaB activation or intercellular adhesion molecule-1 up-regulation, while N-acetyl-L-cysteine, which attenuated NF-kappaB activation, had no effect on leucocyte recruitment." | ( Tepoxalin inhibits inflammation and microvascular dysfunction induced by abdominal irradiation in rats. Anderson, DC; Casadevall, M; Conill, C; Granger, DN; Mollà, M; Panés, J; Piqué, JM; Roselló-Catafau, J; Salas, A; Sans, M, 2000) | 2.47 |
Excerpt | Reference | Relevance |
---|---|---|
"The pharmacodynamic properties of tepoxalin, Na-salicylate and ketoprofen were determined in an intravenous lipopolysaccharide (LPS) inflammation model in broiler chickens." | ( Pharmacodynamics of tepoxalin, sodium-salicylate and ketoprofen in an intravenous lipopolysaccharide inflammation model in broiler chickens. Beyaert, R; Croubels, S; de Backer, P; de Baere, S; de Boever, S; Meyer, E; Neirinckx, EA, 2010) | 0.96 |
Excerpt | Reference | Relevance |
---|---|---|
"A pharmacokinetic study was conducted to compare the oral bioavailability of tepoxalin and its pharmacologically active acid metabolite in fasted dogs and dogs fed either a low-fat or high-fat commercial diet." | ( Effect of dietary fat on oral bioavailability of tepoxalin in dogs. Clarke, CR; Homer, LM; Weingarten, AJ, 2005) | 0.81 |
No accumulation of tepoxalin or its carboxylic acid metabolite was detected in plasma following multiple dosing over a range of 5 to 50 mg/kg/day for rats. No significant change was obtained in GFR after a 28-day period of dosing with tEPoxalin and benazepril together.
Excerpt | Relevance | Reference |
---|---|---|
" In both rats and dogs, no accumulation of tepoxalin or its carboxylic acid metabolite was detected in plasma following multiple dosing over a range of 5 to 50 mg/kg/day for rats and 20 to 300 mg/kg/day for dogs." | ( Preclinical toxicity evaluation of tepoxalin, a dual inhibitor of cyclooxygenase and 5-lipoxygenase, in Sprague-Dawley rats and beagle dogs. Barrett, DS; Dempster, AM; Keenan, CM; Kimball, JP; Knight, EV; Lieuallen, WG; Panigrahi, D; Powers, WJ; Smith, IL; Szot, RJ; Wong, FA, 1996) | 0.83 |
" No significant change was obtained in GFR after a 28-day period of dosing with tepoxalin and benazepril together." | ( Effect of tepoxalin on renal function in healthy dogs receiving an angiotensin-converting enzyme inhibitor. Debailleul, M; Desfontis, JC; Fusellier, M; Gautier, F; Gogny, M; Madec, S; Marescaux, L, 2005) | 0.96 |
Role | Description |
---|---|
non-steroidal anti-inflammatory drug | An anti-inflammatory drug that is not a steroid. In addition to anti-inflammatory actions, non-steroidal anti-inflammatory drugs have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. |
non-narcotic analgesic | A drug that has principally analgesic, antipyretic and anti-inflammatory actions. Non-narcotic analgesics do not bind to opioid receptors. |
antipyretic | A drug that prevents or reduces fever by lowering the body temperature from a raised state. An antipyretic will not affect the normal body temperature if one does not have fever. Antipyretics cause the hypothalamus to override an interleukin-induced increase in temperature. The body will then work to lower the temperature and the result is a reduction in fever. |
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor | A compound or agent that combines with cyclooxygenases (EC 1.14.99.1) and thereby prevents its substrate-enzyme combination with arachidonic acid and the formation of icosanoids, prostaglandins, and thromboxanes. |
apoptosis inhibitor | Any substance that inhibits the process of apoptosis (programmed cell death) in multi-celled organisms. |
lipoxygenase inhibitor | A compound or agent that combines with lipoxygenase and thereby prevents its substrate-enzyme combination with arachidonic acid and the formation of the icosanoid products hydroxyicosatetraenoic acid and various leukotrienes. |
immunomodulator | Biologically active substance whose activity affects or plays a role in the functioning of the immune system. |
[role 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] |
Class | Description |
---|---|
pyrazoles | |
aromatic ether | Any ether in which the oxygen is attached to at least one aryl substituent. |
hydroxamic acid | A compound, RkE(=O)lNHOH, derived from an oxoacid RkE(=O)l(OH) (l =/= 0) by replacing -OH with -NHOH, and derivatives thereof. Specific examples of hydroxamic acids are preferably named as N-hydroxy amides. |
monochlorobenzenes | Any member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine. |
[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) |
---|---|---|---|---|---|---|---|
hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 22.6142 | 3.1890 | 29.8841 | 59.4836 | AID1224846; AID1224894 |
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 10.4155 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
GLI family zinc finger 3 | Homo sapiens (human) | Potency | 9.8156 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 7.4978 | 0.0006 | 57.9133 | 22,387.1992 | AID1259378 |
nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 27.6009 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224839; AID1224893 |
progesterone receptor | Homo sapiens (human) | Potency | 23.8675 | 0.0004 | 17.9460 | 75.1148 | AID1346784; AID1346795 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 1.0964 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 2.6818 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159555 |
retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 1.8681 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID1159531 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 19.3344 | 0.0015 | 30.6073 | 15,848.9004 | AID1224848; AID1224849; AID1259403 |
farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 19.3328 | 0.3758 | 27.4851 | 61.6524 | AID743217; AID743220; AID743239 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 29.8493 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 26.1024 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248 |
G | Vesicular stomatitis virus | Potency | 2.7540 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 4.8975 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 23.7083 | 0.0010 | 24.5048 | 61.6448 | AID743215 |
peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 3.7575 | 0.0010 | 19.4141 | 70.9645 | AID743191 |
vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 19.0490 | 0.0237 | 23.2282 | 63.5986 | AID743223; AID743241 |
activating transcription factor 6 | Homo sapiens (human) | Potency | 4.2527 | 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 | 9.5205 | 19.7391 | 45.9784 | 64.9432 | AID1159509 |
v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 25.3735 | 0.0578 | 21.1097 | 61.2679 | AID1159526; AID1159528 |
Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 55.1965 | 0.0391 | 47.5451 | 146.8240 | AID1224845; AID1224896 |
heat shock protein beta-1 | Homo sapiens (human) | Potency | 23.7083 | 0.0420 | 27.3789 | 61.6448 | AID743210 |
nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 1.4959 | 0.0006 | 27.2152 | 1,122.0200 | AID743202 |
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 | 2.7540 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 2.7540 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 26.6032 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 2.7540 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 2.7540 | 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) |
---|---|---|---|---|---|---|---|
Prostaglandin G/H synthase 1 | Ovis aries (sheep) | IC50 (µMol) | 2.8500 | 0.0003 | 2.1774 | 10.0000 | AID1810791 |
Polyunsaturated fatty acid 5-lipoxygenase | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.6667 | 0.0046 | 2.0182 | 10.0000 | AID3637; AID6868; AID6869 |
Prostaglandin G/H synthase 2 | Homo sapiens (human) | IC50 (µMol) | 2.8500 | 0.0001 | 0.9950 | 10.0000 | AID1810792 |
Prostaglandin G/H synthase 2 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 3.5250 | 0.0029 | 1.7868 | 10.0000 | AID54353; AID54355 |
Prostaglandin G/H synthase 1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 3.5250 | 0.0029 | 1.8232 | 10.0000 | AID54353; AID54355 |
[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) |
---|---|---|---|---|---|---|---|
Polyunsaturated fatty acid 5-lipoxygenase | Homo sapiens (human) | EC50 (µMol) | 0.0700 | 0.0700 | 2.8600 | 6.8000 | AID101298 |
Leukotriene B4 receptor 1 | Homo sapiens (human) | EC50 (µMol) | 0.0700 | 0.0700 | 2.4467 | 6.8000 | AID101298 |
Leukotriene B4 receptor 2 | Homo sapiens (human) | EC50 (µMol) | 0.0700 | 0.0700 | 1.9375 | 6.8000 | AID101298 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
AID3637 | The compound was tested for inhibitory activity against 5-Lipoxygenase in rat RBL-1 | 1992 | Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14 | 5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors. |
AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
AID1810791 | Inhibition of ovine COX-1 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents |
AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
AID54523 | Inhibitory activity against Cyclooxygenase using sheep seminal vesicle (SSV) enzyme (COX-1) | 1999 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7 | N-hydroxyurea and hydroxamic acid inhibitors of cyclooxygenase and 5-lipoxygenase. |
AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
AID1810790 | Inhibition of soybean LOX using arachidonic acid as substrate incubated for 5 mins | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents |
AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
AID54355 | Inhibitory activity against cyclooxygenase (COX) in intact rat barophilic leukemia cells (RBL-1) | 1999 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7 | N-hydroxyurea and hydroxamic acid inhibitors of cyclooxygenase and 5-lipoxygenase. |
AID6868 | Inhibitory activity against 5-lipoxygenase (5-LO) in intact rat barophilic leukemia cells (RBL-1) | 1999 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7 | N-hydroxyurea and hydroxamic acid inhibitors of cyclooxygenase and 5-lipoxygenase. |
AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
AID101298 | In vitro inhibition of ionophore stimulated LTB4 release from human peripheral blood leukocytes. | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Benzothiazole hydroxy ureas as inhibitors of 5-lipoxygenase: use of the hydroxyurea moiety as a replacement for hydroxamic acid. |
AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
AID54353 | Inhibitory activity against Cyclooxygenase (COX) using broken rat barophilic leukemia cells (RBL-1) | 1999 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7 | N-hydroxyurea and hydroxamic acid inhibitors of cyclooxygenase and 5-lipoxygenase. |
AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
AID1810792 | Inhibition of human COX-2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13 | Design, Synthesis, and Activity Evaluation of Stereoconfigured Tartarate Derivatives as Potential Anti-inflammatory Agents |
AID127801 | In vivo 5-Lipoxygenase inhibitory activity by using mouse zymosan peritonitis model | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Benzothiazole hydroxy ureas as inhibitors of 5-lipoxygenase: use of the hydroxyurea moiety as a replacement for hydroxamic acid. |
AID6869 | Inhibitory activity against 5-lipoxygenase (5-LO) using broken rat barophilic leukemia cells (RBL-1) | 1999 | Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7 | N-hydroxyurea and hydroxamic acid inhibitors of cyclooxygenase and 5-lipoxygenase. |
AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
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. |
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. |
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. |
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. |
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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. |
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. |
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. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 24 (35.82) | 18.2507 |
2000's | 18 (26.87) | 29.6817 |
2010's | 18 (26.87) | 24.3611 |
2020's | 7 (10.45) | 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 (32.33) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 14 (19.72%) | 5.53% |
Reviews | 6 (8.45%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 51 (71.83%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |