tolfenamic acid: structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
tolfenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 3-chloro-2-methylphenyl group. Tolfenamic acid is used specifically for relieving the pain of migraine. It also shows anticancer activity. [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 | 610479 |
| CHEMBL ID | 121626 |
| CHEBI ID | 32243 |
| SCHEMBL ID | 25190 |
| MeSH ID | M0054268 |
| Synonym |
|---|
| tolfenamic |
| BIDD:GT0343 |
| n-(3-chloro-o-tolyl)anthranilic acid |
| 2-((3-chloro-2-methylphenyl)amino)benzoic acid |
| brn 0657821 |
| acidum tolfenamicum [inn-latin] |
| acido tolfenamico [inn-spanish] |
| n-(3-chloro-o-tolyl)-anthranilic acid |
| einecs 237-264-3 |
| gea 6414 |
| n-(3-chloro-2-methylphenyl)anthranilic acid |
| benzoic acid, 2-((3-chloro-2-methylphenyl)amino)- |
| n-(2-methyl-3-chlorophenyl)anthranilic acid |
| acide tolfenamique [inn-french] |
| tolfenamic acid [inn:ban:jan] |
| anthranilic acid, n-(3-chloro-o-tolyl)- |
| AB00052244-15 |
| BRD-K50133271-001-05-4 |
| smr000058289 |
| MLS000028531 |
| SPECTRUM_001263 |
| tolfenamic acid |
| PRESTWICK_579 |
| 13710-19-5 |
| NCGC00016705-01 |
| cas-13710-19-5 |
| UNM000001237003 |
| PRESTWICK2_000205 |
| OPREA1_692996 |
| BSPBIO_003223 |
| SPECTRUM5_001143 |
| BSPBIO_000189 |
| PRESTWICK3_000205 |
| AB00052244 |
| tolfenamic acid, nsaid |
| tolfenamic acid (jan/inn) |
| D01183 |
| clotam (tn) |
| NCGC00022587-04 |
| NCGC00022587-03 |
| KBIO2_006879 |
| KBIOSS_001743 |
| KBIO3_002723 |
| KBIO2_004311 |
| KBIO2_001743 |
| KBIOGR_000935 |
| PRESTWICK0_000205 |
| SPECTRUM4_000238 |
| PRESTWICK1_000205 |
| SPECTRUM2_001446 |
| SPECTRUM3_001762 |
| SPBIO_002110 |
| SPBIO_001311 |
| SPECTRUM1501198 |
| NCGC00016705-02 |
| NCGC00022587-05 |
| clotam |
| bifenac |
| BPBIO1_000209 |
| HMS2090D04 |
| 2-(3-chloro-o-toluidino)benzoic acid |
| 2-[(3-chloro-2-methylphenyl)amino]benzoic acid |
| C2064 |
| cid_610479 |
| bdbm35905 |
| chebi:32243 , |
| nsc-757873 |
| n-(3-chloro-o-tolyl)anthranilic |
| CHEMBL121626 |
| 2-(3-chloro-2-methylanilino)benzoic acid |
| FT-0652603 |
| inchi=1/c14h12clno2/c1-9-11(15)6-4-8-12(9)16-13-7-3-2-5-10(13)14(17)18/h2-8,16h,1h3,(h,17,18) |
| yeznlouzaiomlt-uhfffaoysa- |
| HMS1568J11 |
| HMS1921P13 |
| NCGC00016705-05 |
| A807198 |
| 2-[(3-chloranyl-2-methyl-phenyl)amino]benzoic acid |
| HMS2095J11 |
| n-(3-chloro-ortho-tolyl) anthranilic acid |
| pharmakon1600-01501198 |
| nsc757873 |
| dtxsid1045409 , |
| tox21_110570 |
| dtxcid9025409 |
| AKOS012836098 |
| HMS2230J13 |
| CCG-39189 |
| NCGC00016705-06 |
| NCGC00016705-04 |
| NCGC00016705-07 |
| NCGC00016705-03 |
| acido tolfenamico |
| unii-3g943u18km |
| acide tolfenamique |
| nsc 757873 |
| 3g943u18km , |
| acidum tolfenamicum |
| S1959 |
| HMS3370A02 |
| tolfenamic acid [inn] |
| tolfenamic acid [ep monograph] |
| tolfenamic acid [who-dd] |
| tolfenamic acid [mart.] |
| tolfenamic acid [ep impurity] |
| tolfenamic acid [mi] |
| tolfenamic acid [jan] |
| gtpl8769 |
| HY-B0335 |
| SCHEMBL25190 |
| tox21_110570_1 |
| NCGC00016705-10 |
| mfcd00133865 |
| tolfedine |
| benzoic acid, 2-(3-chloro-2-methylphenylamino)- |
| YEZNLOUZAIOMLT-UHFFFAOYSA-N |
| tolfine |
| 2-(3-chloro-2-methylanilino)benzoic acid # |
| benzoic acid, 2-[(3-chloro-2-methylphenyl)amino]- |
| AB00052244_16 |
| AB00052244_17 |
| DB09216 |
| SR-01000000102-3 |
| sr-01000000102 |
| tolfenamic acid, vetranal(tm), analytical standard |
| HMS3651E06 |
| tolfenamic acid, european pharmacopoeia (ep) reference standard |
| tolfenamic acid, pharmaceutical secondary standard; certified reference material |
| tolfenamic acid; 2-[(3-chloro-2-methylphenyl)amino]benzoic acid; n-(3-chlor-o-tolyl)-anthranilsaure |
| J-006962 |
| SR-01000000102-2 |
| SBI-0051687.P002 |
| HMS3712J11 |
| SW196753-3 |
| n-(3-chloro-ortho-tolyl)anthranilic acid |
| 2(3-chloro-2-methylanilino)benzoic acid |
| 2-(3-chloro-2-methylphenylamino)benzoic acid |
| AS-13748 |
| 2-([3-chloro-2-methylphenyl]amino)benzoic acid |
| Q59412 |
| BRD-K50133271-001-10-4 |
| HMS3884M16 |
| tolfenamic-acid |
| D78227 |
| tolfenamicacid |
| 2-((3-chloro-2-methylphenyl)amino)benzoicacid |
| SY052546 |
| tolfenamic acid 1000 microg/ml in acetonitrile |
| EN300-7416304 |
| clotam, tolfedine,2-[(3-chloro-2-methylphenyl)amino]benzoic acid |
Tolfenamic acid (TA) is an anti-inflammatory drug used as an analgesic and antipyretic in humans and animals. It alleviates learning and memory deficits in the APP transgenic mouse model of Alzheimer's disease. Tolfenamid inhibits lung, esophageal, breast and pancreatic cancer cell and tumor growth.
Tolfenamic acid (Clotam) has been used in the therapy of rheumatic diseases for some years. It has been shown to alter the expression of several genes that represent cancer hallmarks including apoptosis, growth arrest, angiogenesis and metastasis.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Tolfenamic acid has been shown to alter the expression of several genes that represent cancer hallmarks including apoptosis, growth arrest, angiogenesis and metastasis." | ( Chemopreventive Properties of Tolfenamic Acid: A Mechanistic Review. Feldman, D; Leahy, E; Lee, SH, 2018) | 1.49 |
| "Tolfenamic acid (TA) has been transformed from crystalline to amorphous state through freeze-drying by using varying ratios of polyacrylic acid (PA) at various pH values. " | ( Effect of pH, polymer concentration and molecular weight on the physical state properties of tolfenamic acid. Ahmed, S; Sheraz, MA; Ur Rehman, I, 2015) | 2.08 |
| "Tolfenamic acid and tenidap have been reported to be dual inhibitors of cyclo-oxygenase and 5-lipoxygenase. " | ( Are tolfenamic acid and tenidap dual inhibitors of 5-lipoxygenase and cyclo-oxygenase? McMillan, RM; Proudman, KE, 1991) | 2.28 |
| "Tolfenamic acid (Clotam) has been used in the therapy of rheumatic diseases for some years. " | ( Effect of tolfenamic acid on the metabolism of the main connective tissue components in rats. Adam, M; Krajícková, J; Pesáková, V; Senius, KE, 1987) | 2.12 |
Tolfenamic acid promotes the degradation of Sp1. It did not inhibit the release of Ca2+ from intracellular stores induced by fMLP or A23187.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Tolfenamic acid promotes the degradation of Sp1, our previous studies demonstrated its ability to down-regulate transcriptional targets of Sp1 like amyloid precursor protein and reduce amyloid beta (Aβ), the main component of AD plaques." | ( Tolfenamic acid reduces tau and CDK5 levels: implications for dementia and tauopathies. Adwan, L; Basha, R; Subaiea, GM; Zawia, NH, 2015) | 2.58 |
| "Tolfenamic acid did not inhibit the release of Ca2+ from intracellular stores induced either by fMLP or A23187." | ( Inhibition of human neutrophil function by tolfenamic acid involves inhibition of Ca2+ influx. Kankaanranta, H; Moilanen, E; Siltaloppi, E; Vapaatalo, H; Vuorinen, P; Wuorela, H, 1995) | 1.28 |
Treatment with tolfenamic acid led to inhibition of cell growth and down-regulation of β-catenin expression in human colon cancer cell lines.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Tolfenamic acid treatment inhibited cell growth and induced apoptosis as measured by caspase activity and bioelectric impedance." | ( ESE-1/EGR-1 pathway plays a role in tolfenamic acid-induced apoptosis in colorectal cancer cells. Baek, SJ; Bahn, JH; Choi, CK; English, AE; Lee, SH; Safe, S; Whitlock, NC, 2008) | 1.34 |
| "Treatment with tolfenamic acid led to inhibition of cell growth and down-regulation of β-catenin expression in a dose- and time-dependent manner in human colon cancer cell lines." | ( Tolfenamic acid downregulates β-catenin in colon cancer. Baek, SJ; Ha, T; Lee, SH; Lou, Z, 2016) | 2.22 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Subsequently, a number of other NSAIDs have been identified as toxic to vultures, while one, meloxicam, is safe at concentrations likely to be encountered by vultures in the wild." | ( Experimental safety testing shows that the NSAID tolfenamic acid is not toxic to Gyps vultures in India at concentrations likely to be encountered in cattle carcasses. Chandramohan, S; Chutia, K; Galligan, TH; Green, RE; Gupta, R; Kesavan, M; Mahendran, K; Mallord, JW; Mathesh, K; Pawde, A; Prakash, NV; Prakash, VM; Ravichandran, P; Saikia, D; Sharma, AK; Shringarpure, R; Timung, A, 2022) | 0.98 |
Pharmacokinetic and pharmacodynamic properties in goats of the non-steroidal anti-inflammatory drug tolfenamic acid (TA), administered both alone and in combination with the fluoroquinolone marbofloxacin (MB) Tolfenamic Acid pharmacokinetics were characterized by a relatively short tmax (0.5) The long half-life was caused by the slow el
| Excerpt | Reference | Relevance |
|---|---|---|
| " The long half-life was caused by the slow elimination of tolfenamic acid metabolites." | ( Pharmacokinetics of tolfenamic acid: disposition in bile, blood and urine after intravenous administration to man. Alhava, E; Pentikäinen, PJ; Penttilä, A; Tokola, O, 1984) | 0.84 |
| " Tolfenamic acid pharmacokinetics were characterized by a relatively short tmax (0." | ( Pharmacodynamics and pharmacokinetics of tolfenamic acid in ruminating calves: evaluation in models of acute inflammation. Foot, R; Gettinby, G; Lees, P; McKellar, QA, 1998) | 1.48 |
| "Pharmacokinetic and pharmacodynamic properties of tolfenamic acid (TA) in calves were determined in serum and fluids of inflamed (carrageenan administered) and non-inflamed subcutaneously implanted tissue cages after intramuscular administration both alone and in combination with marbofloxacin (MB)." | ( Influence of marbofloxacin on the pharmacokinetics and pharmacodynamics of tolfenamic acid in calves. Landoni, MF; Lees, P; Sidhu, PK, 2005) | 0.81 |
| "Pharmacokinetic and pharmacodynamic properties in goats of the non-steroidal anti-inflammatory drug tolfenamic acid (TA), administered both alone and in combination with the fluoroquinolone marbofloxacin (MB), were established in a tissue cage model of acute inflammation." | ( Pharmacokinetic and pharmacodynamic interactions of tolfenamic acid and marbofloxacin in goats. Landoni, MF; Lees, P; Sidhu, PK, 2006) | 0.8 |
| " Plasma concentrations of tolfenamic acid were determined by HPLC-UV, and the pharmacokinetic parameters were estimated using a non-compartmental method." | ( Pharmacokinetics of tolfenamic acid in goats after different administration routes. Altinok Yipel, F; Corum, O; Durna Corum, D; Emiroglu, SB; Ilhan, A; Tekeli, IO; Turk, E; Uguz, H; Uney, K, 2021) | 1.24 |
In a four-period cross-over study, the fluoroquinolone antibacterial drug marbofloxacin (MB) was administered to goats intramuscularly (IM) Both alone and in combination with the non-steroidal anti-inflammatory drug tolfenamic acid (TA), also administered IM at a dose rate of 2 mg/kg.
| Excerpt | Reference | Relevance |
|---|---|---|
| " The extent of absorption following oral administration of tolfenamic acid is decreased during migraine attacks, irrespectively if the volunteers received caffeine or placebo in combination with the drug." | ( Tolfenamic acid in combination with caffeine: absorption during acute migraine. Tokola, RA, 1985) | 1.96 |
| " Nonsteroidal anti-inflammatory drugs (NSAID) such as tolfenamic acid and naproxen sodium combined with sumatriptan have demonstrated efficacy in reducing recurrence observed with the single use of this drug." | ( Dexamethasone decreases migraine recurrence observed after treatment with a triptan combined with a nonsteroidal anti-inflammatory drug. Barbosa, JS; Krymchantowski, AV, 2001) | 0.56 |
| "In a four-period cross-over study, the fluoroquinolone antibacterial drug marbofloxacin (MB) was administered to goats intramuscularly (IM) at a dose rate of 2 mg/kg, both alone and in combination with the non-steroidal anti-inflammatory drug tolfenamic acid (TA), also administered IM at a dose rate of 2 mg/kg." | ( Pharmacokinetic and pharmacodynamic modelling of marbofloxacin administered alone and in combination with tolfenamic acid in goats. Aliabadi, FS; Landoni, MF; Lees, P; Sidhu, PK, 2010) | 0.76 |
| "In a four-period, cross-over study, the fluoroquinolone antibacterial drug marbofloxacin (MB) was administered to calves, alone and in combination with the nonsteroidal anti-inflammatory drug tolfenamic acid (TA)." | ( Pharmacokinetic and pharmacodynamic modelling of marbofloxacin administered alone and in combination with tolfenamic acid in calves. Aliabadi, MH; Landoni, MF; Lees, P; Sidhu, PK; Toutain, PL, 2011) | 0.77 |
The aim of this study was to determine the pharmacokinetics and bioavailability of tolfenamic acid in goats after intravenous (IV), intramuscular (IM), subcutaneous (SC), and oral (PO) administrations at 2mg/kg dose.
Tolfenamic acid shows linear pharmacokinetics and during multiple dosage regimen. Levofloxacin, with an alteration in the dosage regimen, can be used effectively for the therapy of infections and inflammatory conditions in sheep.
| Excerpt | Relevance | Reference |
|---|---|---|
| " Dosage was repeated after 2 h if the attack had not abated." | ( Randomized double-blind comparison of tolfenamic acid and paracetamol in migraine. Andersen, B; Christiansen, LV; Larsen, BH; Olesen, J, 1990) | 0.55 |
| " The actions of tolfenamic acid in inhibiting PGE2 synthesis and in attenuating two of the cardinal signs of inflammation (heat and swelling) suggest that a dosage of 2 mgkg-1 administered intramuscularly should be effective clinically as an anti-inflammatory agent." | ( Pharmacodynamics and pharmacokinetics of tolfenamic acid in ruminating calves: evaluation in models of acute inflammation. Foot, R; Gettinby, G; Lees, P; McKellar, QA, 1998) | 0.91 |
| " The COX selectivity of each drug was evaluated from dose-response curves by calculating a ratio (COX-1:COX-2) of inhibitory concentration values on the basis of concentrations that reduced PGE2 by 50% in each COX model." | ( In vitro effects of nonsteroidal anti-inflammatory drugs on cyclooxygenase activity in dogs. Benn, SJ; Conlon, P; Kay-Mugford, P; LaMarre, J, 2000) | 0.31 |
| " From the pharmacokinetic and eicosanoid inhibition data for TA, pharmacodynamic parameters after dosing with TA alone for serum TxB2 and exudate PGE2 expressing efficacy (Emax=69." | ( Pharmacokinetic and pharmacodynamic interactions of tolfenamic acid and marbofloxacin in goats. Landoni, MF; Lees, P; Sidhu, PK, 2006) | 0.58 |
| " These data were used to predict once daily dosage schedules of MB for subsequent clinical evaluation." | ( Pharmacokinetic and pharmacodynamic modelling of marbofloxacin administered alone and in combination with tolfenamic acid in goats. Aliabadi, FS; Landoni, MF; Lees, P; Sidhu, PK, 2010) | 0.57 |
| " Along with the analytical profile, the stability and degradation of TA, its pharmacology and pharmacokinetics, dosage forms and dose, adverse effects and toxicity, and interactions have been discussed." | ( Tolfenamic Acid. Ahmad, I; Ahmed, S; Sheraz, MA, ) | 1.57 |
| " Levofloxacin, with an alteration in the dosage regimen, can be used effectively with tolfenamic acid and flunixin meglumine for the therapy of infections and inflammatory conditions in sheep." | ( Influences of tolfenamic acid and flunixin meglumine on the disposition kinetics of levofloxacin in sheep. Cetin, G; Corum, O; Durna Corum, D; Eser Faki, H; Ider, M; Uney, K; Yildiz, R, 2020) | 1.14 |
| " Therefore, the present study aimed to develop and validate a simple, accurate, rapid, economical, and precise spectrofluorimetric method to assay TA in its pure and dosage forms, and also in degraded solutions." | ( Development and validation of a spectrofluorimetric method for the analysis of tolfenamic acid in pure and tablet dosage form. Ahmad, I; Ahmed, S; Andleeb, S; Anwar, Z; Sheraz, MA, 2020) | 0.79 |
| " himalayensis by oral gavage, with 15 control birds dosed with benzyl alcohol (the carrier solution for tolfenamic acid)." | ( Experimental safety testing shows that the NSAID tolfenamic acid is not toxic to Gyps vultures in India at concentrations likely to be encountered in cattle carcasses. Chandramohan, S; Chutia, K; Galligan, TH; Green, RE; Gupta, R; Kesavan, M; Mahendran, K; Mallord, JW; Mathesh, K; Pawde, A; Prakash, NV; Prakash, VM; Ravichandran, P; Saikia, D; Sharma, AK; Shringarpure, R; Timung, A, 2022) | 1.19 |
| 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. |
| 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. |
| EC 2.7.1.33 (pantothenate kinase) inhibitor | An EC 2.7.1.* (phosphotransferases with an alcohol group as acceptor) inhibitor that interferes with the action of pantothenate kinase (EC 2.7.1.33). |
| [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 |
|---|---|
| aminobenzoic acid | |
| organochlorine compound | An organochlorine compound is a compound containing at least one carbon-chlorine bond. |
| secondary amino compound | A compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups. |
| [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) |
|---|---|---|---|---|---|---|---|
| Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 15.8114 | 0.1409 | 11.1940 | 39.8107 | AID2451 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 28.1838 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 24.5704 | 0.0072 | 15.7588 | 89.3584 | AID588342; AID624030 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 17.9500 | 0.1737 | 34.3047 | 61.8120 | AID1346859; AID1346924 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 79.4328 | 0.0316 | 37.5844 | 354.8130 | AID504865 |
| GLS protein | Homo sapiens (human) | Potency | 5.6234 | 0.3548 | 7.9355 | 39.8107 | AID624170 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 17.9500 | 0.1737 | 34.3047 | 61.8120 | AID1346859; AID1346924 |
| TDP1 protein | Homo sapiens (human) | Potency | 15.6758 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 35.4813 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
| AR protein | Homo sapiens (human) | Potency | 6.4493 | 0.0002 | 21.2231 | 8,912.5098 | AID743036; AID743053 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 10.0000 | 0.0013 | 7.7625 | 44.6684 | AID914; AID915 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 7.0850 | 0.0006 | 57.9133 | 22,387.1992 | AID1259377; AID1259378 |
| progesterone receptor | Homo sapiens (human) | Potency | 13.3332 | 0.0004 | 17.9460 | 75.1148 | AID1346795 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 14.4875 | 0.0002 | 14.3764 | 60.0339 | AID720691; AID720692; AID720719 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 11.9856 | 0.0008 | 17.5051 | 59.3239 | AID1159527 |
| 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 | 11.0166 | 0.0002 | 29.3054 | 16,493.5996 | AID743069; AID743075; AID743078 |
| G | Vesicular stomatitis virus | Potency | 38.9018 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 4.7304 | 0.0010 | 19.4141 | 70.9645 | AID743191 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 26.8807 | 0.0237 | 23.2282 | 63.5986 | AID743222; AID743223 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 44.6684 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa) | Homo sapiens (human) | Potency | 50.1187 | 0.0165 | 25.3078 | 41.3999 | AID602332 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 15.8489 | 0.0025 | 5.8400 | 31.6228 | AID899 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 3.1623 | 0.0063 | 6.9043 | 39.8107 | AID883 |
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 14.1254 | 0.0018 | 15.6638 | 39.8107 | AID894 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 34.8937 | 0.3548 | 28.0659 | 89.1251 | AID504847 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 12.6082 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| ubiquitin carboxyl-terminal hydrolase 2 isoform a | Homo sapiens (human) | Potency | 10.0000 | 0.6561 | 9.4520 | 25.1189 | AID927 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 25.1547 | 0.0006 | 27.2152 | 1,122.0200 | AID743202; AID743219 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 15.8489 | 0.0079 | 8.2332 | 1,122.0200 | AID2551 |
| geminin | Homo sapiens (human) | Potency | 25.9290 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
| Vpr | Human immunodeficiency virus 1 | Potency | 12.5893 | 1.5849 | 19.6264 | 63.0957 | AID651644 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 14.2191 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 7.0795 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Interferon beta | Homo sapiens (human) | Potency | 38.9018 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 38.9018 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 23.1234 | 0.0023 | 19.5956 | 74.0614 | AID651631; AID720552 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 3.1623 | 0.0063 | 8.2350 | 39.8107 | AID883 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Disintegrin and metalloproteinase domain-containing protein 17 | Homo sapiens (human) | Potency | 10.0000 | 1.5849 | 13.0043 | 25.1189 | AID927 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 38.9018 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 14.2191 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 38.9018 | 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) |
|---|---|---|---|---|---|---|---|
| phospholipase A2 precursor | Homo sapiens (human) | IC50 (µMol) | 7.7400 | 1.0200 | 9.0025 | 15.2000 | AID588400 |
| cysteine protease ATG4B isoform a | Homo sapiens (human) | IC50 (µMol) | 8.1700 | 1.2500 | 10.6632 | 19.1000 | AID504756 |
| Cytochrome c oxidase subunit 2 | Homo sapiens (human) | IC50 (µMol) | 1.2900 | 0.0200 | 0.8493 | 3.0000 | AID1862082; AID1885558 |
| Androgen receptor | Homo sapiens (human) | IC50 (µMol) | 52.4500 | 0.0000 | 0.8753 | 10.0000 | AID1799354; AID329526 |
| Cytochrome P450 2C9 | Homo sapiens (human) | Ki | 537,650,003,968.0000 | 0.0003 | 1.6842 | 10.0000 | AID313084 |
| Fatty acid-binding protein, intestinal | Homo sapiens (human) | Ki | 6.1000 | 0.3000 | 5.4814 | 9.4000 | AID1801103 |
| Prostaglandin G/H synthase 2 | Homo sapiens (human) | IC50 (µMol) | 0.8800 | 0.0001 | 0.9950 | 10.0000 | AID1811234 |
| Aldo-keto reductase family 1 member C3 | Homo sapiens (human) | Ki | 0.0080 | 0.0059 | 0.7091 | 3.1000 | AID664572 |
| [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) |
|---|---|---|---|---|---|---|---|
| glycogen synthase kinase-3 beta isoform 1 | Homo sapiens (human) | EC50 (µMol) | 300.0000 | 0.2125 | 22.1562 | 83.9400 | AID434954 |
| Transthyretin | Homo sapiens (human) | Kd | 0.1500 | 0.0030 | 1.3482 | 10.0000 | AID1239060 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| 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. |
| 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. |
| 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. |
| AID651635 | Viability Counterscreen for 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. |
| 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1755691 | Inhibition of Salmonella typhimurium LsrK expressed in Escherichia coli MET1158 in presence of DPD by kinase-glo max luminescent assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Tackling Antimicrobial Resistance with Small Molecules Targeting LsrK: Challenges and Opportunities. |
| AID169240 | Incidence of melena defecation was recorded 24 hrs of last treatment given once daily for 4 days; Positive | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L-cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity. |
| AID329525 | Activity at androgen receptor ligand binding domain assessed as inhibition of SRC2-3 interaction at 50 uM after 2 hrs by fluorescence polarization assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Oct-09, Volume: 104, Issue:41 | A surface on the androgen receptor that allosterically regulates coactivator binding. |
| 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] | |||
| AID1811235 | Inhibition of human topoisomerase I using DNA pBR322 as substrate assessed as DNA relaxation incubated for 45 mins by ethidium bromide staining based agarose gel electrophoresis | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | N-2-(phenylamino) benzamide derivatives as novel anti-glioblastoma agents: Synthesis and biological evaluation. |
| AID1862082 | Inhibition of COX-2 (unknown origin) | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Discovery of dual inhibitors of topoisomerase I and Cyclooxygenase-2 for colon cancer therapy. |
| AID1885614 | Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced COX-2 expression at 6.6 uM incubated for 1 hrs followed by LPS stimulation and measured after 24 hrs by western blot analysis | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| AID1846047 | Antitumor activity against human Daoy cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiter-Glo luminescent assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Medulloblastoma drugs in development: Current leads, trials and drawbacks. |
| AID664572 | Inhibition of human AKR1C3 using S-(+)-1,2,3,4-tetrahydro-1-naphthol as substrate | 2012 | Journal of natural products, Apr-27, Volume: 75, Issue:4 | Selective inhibition of human type-5 17β-hydroxysteroid dehydrogenase (AKR1C3) by baccharin, a component of Brazilian propolis. |
| AID1811233 | Antiproliferative activity against rat C6 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | N-2-(phenylamino) benzamide derivatives as novel anti-glioblastoma agents: Synthesis and biological evaluation. |
| AID1885555 | Antiproliferative activity against human HT-29 cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| AID558036 | Therapeutic index, ratio of TC50 for JC polyomavirus M1/SVEdelta infected human SVG-A cells to EC50 for JC polyomavirus M1/SVEdelta | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Identification and characterization of mefloquine efficacy against JC virus in vitro. |
| AID190508 | Ulcerogenic activity administered once daily at 760 uM/kg for 4 days was determined as no of animals showing perforating ulcers | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L-cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity. |
| AID118143 | Antiinflammatory activity, administered ip at 150 uM/kg dose was determined against carrageenan-induced mice paw edema model | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L-cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity. |
| AID1885556 | Antiproliferative activity against human HGC-27 cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID977599 | Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID1811231 | Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | N-2-(phenylamino) benzamide derivatives as novel anti-glioblastoma agents: Synthesis and biological evaluation. |
| AID1885582 | Induction of mitochondrial membrane loss in in human HGC-27 at 10 uM and measured after 36 hrs by TMRE dye based flow cytometry | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
| AID329526 | Activity at androgen receptor ligand binding domain assessed as inhibition of SRC2-3 interaction after 2 hrs by fluorescence polarization assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Oct-09, Volume: 104, Issue:41 | A surface on the androgen receptor that allosterically regulates coactivator binding. |
| AID1220259 | Oral absorption in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1576546 | Antiinflammatory activity against TPA-induced ear edema in BALB/c mouse assessed as inhibition of ear edema at 100 mg/kg, po administered 6 mins prior to TPA challenge and treated twice in 4 hrs and measured after 6 hrs post administration relative to con | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Synergistic effect of tolfenamic acid and glycyrrhizic acid on TPA-induced skin inflammation in mice. |
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
| AID1862081 | Inhibition of COX-2 (unknown origin) at 3 uM | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Discovery of dual inhibitors of topoisomerase I and Cyclooxygenase-2 for colon cancer therapy. |
| AID24265 | Ability to undergo in vitro ester hydrolysis in 80% human plasma ( pH of 7.4) at 37 degree Celsius expressed as half life of methyl ester hydrolysis | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Esters of N,N-disubstituted 2-hydroxyacetamides as a novel highly biolabile prodrug type for carboxylic acid agents. |
| AID1811234 | Inhibition of human recombinant COX-2 using arachidonic acid as substrate preincubated 10 mins followed by substrate addition and measured after 2 mins by ELISA | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | N-2-(phenylamino) benzamide derivatives as novel anti-glioblastoma agents: Synthesis and biological evaluation. |
| AID1576543 | Tmax in rat at 10 to 480 mg/kg, po | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Synergistic effect of tolfenamic acid and glycyrrhizic acid on TPA-induced skin inflammation in mice. |
| AID558029 | Antiviral activity against JC polyomavirus M1/SVEdelta infected in human SVG-A cells assessed as inhibition of viral replication after 3 days | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Identification and characterization of mefloquine efficacy against JC virus in vitro. |
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
| AID1272494 | Anti-inflammatory activity in rat assessed as reduction of carrageenan-induced paw edema at 150 umol/kg, ip after 3.5 hrs relative to control | 2016 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3 | Amides of non-steroidal anti-inflammatory drugs with thiomorpholine can yield hypolipidemic agents with improved anti-inflammatory activity. |
| AID1846055 | Antitumor activity against human D283 Med cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiter-Glo luminescent assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Medulloblastoma drugs in development: Current leads, trials and drawbacks. |
| AID171177 | Body weight change after once daily administration at 760 uM/kg for 4 days in rats was determined | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L-cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity. |
| AID1220242 | Unbound intrinsic clearance in human intestinal microsomes assessed CYP450-mediated glucuronidation clearance | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1239061 | Binding affinity to TTR in human plasma assessed as protein stabilization preincubated for 1 hr followed by urea-mediated denaturation by Western blot analysis | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | Enthalpic Forces Correlate with the Selectivity of Transthyretin-Stabilizing Ligands in Human Plasma. |
| AID1885602 | Anti-migration activity against human HGC-27 cells assessed as decrease in cell migration rate at 10 uM for 48 hrs by crystalline violet staining based assay | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| 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] | |||
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
| AID329528 | Activity at androgen receptor assessed as inhibition of dihydrotestosterone response by GAL4-MMTV luciferase reporter gene assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Oct-09, Volume: 104, Issue:41 | A surface on the androgen receptor that allosterically regulates coactivator binding. |
| AID1220250 | Activity of human UGT2B15 expressed in insect cells assessed as reduction in compound level after 30 mins | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
| AID1220257 | Ratio of drug level in blood to plasma in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' 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] | |||
| AID1239060 | Binding affinity to TTR (unknown origin) by isothermal titration calorimetric analysis | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | Enthalpic Forces Correlate with the Selectivity of Transthyretin-Stabilizing Ligands in Human Plasma. |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID1885593 | Induction of cell cycle arrest in human RKO cells assessed as accumulation at G2/M phase upto 10 uM for 24 hrs by propidium iodide staining based flow cytometry | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| AID1220249 | Activity of human UGT2B7 expressed in insect cells assessed as reduction in compound level after 30 mins | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1885594 | Induction of cell cycle arrest in human HGC-27 cells assessed as accumulation at G2/M phase upto 10 uM for 24 hrs by propidium iodide staining based flow cytometry | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| 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 | |||
| AID1220248 | Activity of human UGT1A9 expressed in insect cells assessed as reduction in compound level after 30 mins | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1220240 | Unbound fraction during CYP4500-mediated metabolism in human intestinal microsomes | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1885612 | Inhibition of LPS induced NO production in mouse RAW264.7 cells at 6.6 uM incubated for 1 hrs followed by LPS stimulation and measured after 24 hrs by Griess reagent based assay | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
| AID313084 | Inhibition of CYP2C9 | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3 | High confidence predictions of drug-drug interactions: predicting affinities for cytochrome P450 2C9 with multiple computational methods. |
| AID112732 | Antiinflammatory activity, administered ip at 150 uM/kg dose was determined against carrageenan-induced mice paw edema model | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L-cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity. |
| AID1256770 | Antiinflammatory activity in rat assessed as reduction of carrageenan-induced paw oedema at 0.15 mmol/kg, ip administered 5 mins before carrageenan challenge measured after 3.5 hrs | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Esters of some non-steroidal anti-inflammatory drugs with cinnamyl alcohol are potent lipoxygenase inhibitors with enhanced anti-inflammatory activity. |
| AID1220255 | Apparent permeability by PAMPA method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID24263 | Ability to undergo in vitro ester hydrolysis in 80% human plasma ( pH of 7.4) at 37 degree Celsius expressed as half life of N,N-diethylglycolamide ester hydrolysis | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Esters of N,N-disubstituted 2-hydroxyacetamides as a novel highly biolabile prodrug type for carboxylic acid agents. |
| AID1220247 | Activity of human UGT1A7 expressed in insect cells assessed as reduction in compound level after 30 mins | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1220237 | Unbound fraction during UGT-mediated glucuronidation in human intestinal microsomes | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1862080 | Inhibition of COX-2 (unknown origin) at 30 uM | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Discovery of dual inhibitors of topoisomerase I and Cyclooxygenase-2 for colon cancer therapy. |
| AID1885558 | Inhibition of human COX-2 assessed as by fluorescence based microplate reader assay | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| AID184536 | Mortality caused by the compound in rats after administration at 760 uM/kg for 4 days | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Synthesis and pharmacological evaluation of amide conjugates of NSAIDs with L-cysteine ethyl ester, combining potent antiinflammatory and antioxidant properties with significantly reduced gastrointestinal toxicity. |
| AID1220244 | Activity of human UGT1A1 expressed in insect cells assessed as reduction in compound level after 30 mins | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID977602 | Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID1220238 | Intrinsic clearance in human intestinal microsomes assessed UGT-mediated glucuronidation clearance | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1811232 | Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | N-2-(phenylamino) benzamide derivatives as novel anti-glioblastoma agents: Synthesis and biological evaluation. |
| AID1885601 | Anti-migration activity against human RKO cells assessed as decrease in cell migration rate at 10 uM for 48 hrs by crystalline violet staining based assay | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| AID1885553 | Antiproliferative activity against mouse CT26.WT cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
| AID1220239 | Unbound intrinsic clearance in human intestinal microsomes assessed UGT-mediated glucuronidation clearance | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1220241 | Intrinsic clearance in human intestinal microsomes assessed CYP450-mediated glucuronidation clearance | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| 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] | |||
| AID1220258 | Renal clearance in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID1885559 | Inhibition of human topoisomerase I assessed as DNA unwinding using DNA pBR322 as substrate at 2 uM incubated for 30 mins by ethidium bromide staining based agarose gel electrophoresis | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
| AID1885554 | Antiproliferative activity against human RKO cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| AID1885609 | Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability at <=11.11 for 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| AID1576545 | Antiinflammatory activity against TPA-induced ear edema in BALB/c mouse assessed as inhibition of ear edema at 50 mg/kg, po administered 6 mins prior to TPA challenge and treated twice in 4 hrs and measured after 6 hrs post administration relative to cont | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10 | Synergistic effect of tolfenamic acid and glycyrrhizic acid on TPA-induced skin inflammation in mice. |
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID1220256 | Total clearance in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9 | Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data. |
| AID302758 | Solubility by shake flask method | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | Poorly soluble marketed drugs display solvation limited solubility. |
| AID1885557 | Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell proliferation incubated for 48 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| AID1885603 | Anti-migration activity against human RKO cells assessed as inhibition of cell migration at 0.37 uM and measured after 24 hrs by wound healing assay | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| AID1885581 | Induction of mitochondrial membrane loss in in human RKO at 10 uM and measured after 36 hrs by TMRE dye based flow cytometry | 2022 | Journal of medicinal chemistry, 08-11, Volume: 65, Issue:15 | |
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| 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] | |||
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
| AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| AID1801103 | Fluorophore Displacement Assay from Article 10.1021/cb5005178: \\Characterization of two distinct modes of drug binding to human intestinal fatty acid binding protein.\\ | 2014 | ACS chemical biology, Nov-21, Volume: 9, Issue:11 | Characterization of two distinct modes of drug binding to human intestinal fatty acid binding protein. |
| AID1799354 | SPA Binding Assay (IC50) from Article 10.1021/cb900143a: \\Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription.\\ | 2009 | ACS chemical biology, Oct-16, Volume: 4, Issue:10 | Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription. |
| AID1345274 | Human AKR1C3 (Prostaglandin synthases) | 2007 | The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11 | Structure-based inhibitor design for an enzyme that binds different steroids: a potent inhibitor for human type 5 17beta-hydroxysteroid dehydrogenase. |
| AID1159550 | Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening | 2015 | Nature cell biology, Nov, Volume: 17, Issue:11 | 6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 42 (14.69) | 18.7374 |
| 1990's | 57 (19.93) | 18.2507 |
| 2000's | 45 (15.73) | 29.6817 |
| 2010's | 110 (38.46) | 24.3611 |
| 2020's | 32 (11.19) | 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 (64.78) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 47 (15.99%) | 5.53% |
| Reviews | 21 (7.14%) | 6.00% |
| Case Studies | 5 (1.70%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 221 (75.17%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| A Phase 2a Randomized, Double-blind, Placebo-controlled Study to Evaluate the Safety and Efficacy of Tolfenamic Acid for the Treatment of Progressive Supranuclear Palsy [NCT04253132] | Phase 1/Phase 2 | 24 participants (Anticipated) | Interventional | 2021-01-01 | Not yet recruiting | ||
| 09.017 - A Phase I Study of Tolfenamic Acid With Gemcitabine and Radiation in Patients With Locally Advanced or Metastatic Pancreatic Cancer Requiring Definitive or Palliative Radiation Therapy [NCT02159248] | Phase 1 | 0 participants (Actual) | Interventional | 2014-03-31 | Withdrawn(stopped due to The study closed prior to enrolling any participants.) | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||