Rafoxanide is a synthetic benzimidazole derivative with anthelmintic activity, particularly against liver flukes in ruminants. It is commonly used to treat fascioliasis, a parasitic infection caused by the liver fluke Fasciola hepatica. Rafoxanide acts by inhibiting the synthesis of tubulin, a protein essential for the formation of microtubules. Microtubules play a crucial role in various cellular processes, including cell division, transport, and structure. By disrupting microtubule formation, rafoxanide interferes with the parasite's ability to survive and reproduce. Rafoxanide is typically administered orally to livestock as a drench or in feed. The drug is rapidly absorbed from the gastrointestinal tract and distributed throughout the body. It is metabolized in the liver and excreted in the urine and feces. Research on rafoxanide focuses on optimizing its efficacy, reducing its potential toxicity, and developing new formulations for improved delivery. This research is important because fascioliasis can cause significant economic losses in livestock production due to decreased productivity and mortality. Moreover, there is a growing concern about the emergence of drug resistance in parasites, which necessitates the development of new and effective anthelmintics.'
Rafoxanide: Veterinary anthelmintic for grazing animals; used to treat fluke, hookworm and other infestations. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 31475 |
| CHEMBL ID | 287542 |
| SCHEMBL ID | 118031 |
| MeSH ID | M0018456 |
| Synonym |
|---|
| AC-20061 |
| rafoxanidum [inn-latin] |
| einecs 245-148-9 |
| 3'-chlor-4'-(4-chlorphenoxy)-3,5-diiodsalicylanilid |
| brn 2228187 |
| benzamide, n-(3-chloro-4-(4-chlorophenoxy)phenyl)-2-hydroxy-3,5-diiodo- |
| ai3-29020 |
| nsc 355278 |
| rafoxanida [inn-spanish] |
| 3'-chloro-4'-(p-chlorophenoxy)-3, 5-diiodosalicylanilide |
| salicylanilide, 3'-chloro-4'-(p-chlorophenoxy)-3,5-diiodo- |
| n-(3-chloro-4-(4-chlorophenoxy)phenyl)-2-hydroxy-3,5-diiodobenzamide |
| benzamide, {n-[3-chloro-4-(4-chlorophenoxy)phenyl]-2-hydroxy-3,} 5-diiodo- |
| n-[3-chloro-4-(4-chlorophenoxy)phenyl]-2-hydroxy-3,5-diiodo-benzamide |
| n-[3-chloro-4-(4-chloro-phenoxy)-phenyl]-2-hydroxy-3,5-diiodo-benzamide |
| ranide, veterinary |
| flukanide |
| duofas |
| bovanide |
| disalan |
| rafoxanide |
| nsc355278 |
| nsc-355278 |
| ranide |
| 3'-chloro-4'-(p-chlorophenoxy)-3,5-diiodosalicylanilide |
| salicylanilide,5-diiodo- |
| mk-990 |
| 22662-39-1 |
| wln: qr bi di fvmr cg dor dg |
| D05693 |
| rafoxanide (usan/inn) |
| NCGC00160556-01 |
| MLS001240273 |
| smr000768692 |
| n-[3-chloro-4-(4-chlorophenoxy)phenyl]-2-hydroxy-3,5-diiodobenzamide |
| STK377482 |
| CHEMBL287542 |
| bdbm50022832 |
| AKOS003631075 |
| dtxsid5046227 , |
| tox21_111896 |
| dtxcid3026227 |
| cas-22662-39-1 |
| HMS2233M19 |
| 3'-chloro-4'-(4-chlorophenoxy)-3,5-diiodosalicylanilide |
| 22f4fla7dh , |
| rafoxanidum |
| rafoxanide [usan:inn:ban] |
| unii-22f4fla7dh |
| rafoxanida |
| FT-0630489 |
| rafoxanide [mi] |
| rafoxanide [usan] |
| rafoxanide [inn] |
| rafoxanide [mart.] |
| SCHEMBL118031 |
| R0108 |
| NCGC00160556-02 |
| tox21_111896_1 |
| KS-1309 |
| CS-3979 |
| NEMNPWINWMHUMR-UHFFFAOYSA-N |
| 3,5-diiodo-3'-chloro-4'-(p-chlorophenoxy)-salicylanilide |
| HY-17598 |
| rafoxanide, pestanal(r), analytical standard |
| J-014804 |
| BCP15963 |
| mfcd00682899 |
| phenyl)-2-hydroxy-3,5-diiodobenzamide |
| n-(3-chloro-4-(4-chlorophenoxy) |
| Q12048733 |
| rafoxanide vetranal |
| CCG-270276 |
| C74169 |
| S5093 |
| benzamide, n-[3-chloro-4-(4-chlorophenoxy)phenyl]-2-hydroxy-3,5-diiodo- [ |
| OX9 , |
Rafoxanide is an anthelmintic drug that inhibits tumor growth in certain malignancies. It is not permitted for treating animals whose milk is intended for human consumption.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Rafoxanide is an anthelmintic drug that inhibits tumor growth in certain malignancies." | ( Discovery of rafoxanide as a novel agent for the treatment of non-small cell lung cancer. Chen, Q; Guo, Y; Hu, A; Liu, J; Liu, T; Men, Y; Qin, Y; Wang, Y; Zhang, M, 2023) | 2 |
| "Rafoxanide is an effective treatment for the control of fluke infections in animals, but it is currently not permitted for treating animals whose milk is intended for human consumption. " | ( Investigation of the persistence of rafoxanide residues in bovine milk and fate during processing. Danaher, M; Furey, A; Jordan, K; O'Brien, B; Power, C; Sayers, R; Whelan, M, 2013) | 2.11 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Rafoxanide treatment inhibited tumor growth, with no significant side effects, in an MM mouse xenograft model." | ( Rafoxanide, an organohalogen drug, triggers apoptosis and cell cycle arrest in multiple myeloma by enhancing DNA damage responses and suppressing the p38 MAPK pathway. Bu, W; Chang, S; Chen, G; Gao, L; Kong, Y; Lan, X; Li, B; Shi, J; Sun, X; Wang, Y; Wu, H; Wu, X; Xiao, W; Xie, B; Xie, Y; Xu, Z; Yu, D; Zhu, W, 2019) | 2.68 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " These toxic effects seemed to be reversible and were no longer detectable after a further 3-month administration of Rafoxanide (10 mg kg-1) to rats born of treated dams." | ( Oral toxicity in weanling and adult rats and in vitro genotoxicity of the veterinary anthelmintic rafoxanide. Abjean, JP; Laurentie, M; Poul, JM; Verlinde, V, ) | 0.56 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "05) in time to maximum plasma concentrations (Tmax), distribution half-life (T1/2 alpha), elimination half-life (T1/2 beta) and mean residence time (MRT) were observed." | ( Pharmacokinetics of rafoxanide in suckling and weaned lambs following oral administration. Mülders, MS; Swan, GE, 1993) | 0.61 |
| " In sheep serum, rafoxanide induced a rapid absorption of IVM when given in combined form manifested by a shorter absorption half-life time of IVM by 68." | ( Comparative pharmacokinetics of ivermectin alone and a novel formulation of ivermectin and rafoxanide in calves and sheep. Abd-El-Rahman, S; El-Banna, HA; El-Zorba, H; Goudah, A, 2008) | 0.91 |
The bioavailability of a modified rafoxanide oral suspension was compared to the original innovator product and a generic formulation in a single dose, randomised, parallel design study in sheep.
| Excerpt | Reference | Relevance |
|---|---|---|
| "The bioavailability of a modified rafoxanide oral suspension was compared to the original innovator product and a generic formulation in a single dose, randomised, parallel design study in sheep (n = 30)." | ( Differences in the oral bioavailability of three rafoxanide formulations in sheep. Botha, CJ; Kloeck, A; Minnaar, PP; Mülders, MS; Swan, GE; Taylor, JH, 1995) | 0.82 |
| " The absorption half-life (t(½ab)), C(max), AUMC, AUC and systemic bioavailability (F%) are significantly decreased, whereas elimination half-life (t(½el)) and MRT are increased in goats pre-treated by the three tested anthementics." | ( Effect of three anthelmentics on disposition kinetics of florfenicol in goats. Abd El-Aty, AM; Amer, AM; Atef, M; El-Gendi, AY, 2010) | 0.36 |
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
Two field strains of Haemonchus contortus showed pronounced resistance to rafoxanide at a dosage rate of 7 mg/kg live mass. At dosage rates of 3,75 and 5,0 mg/ kg live mass rafOxanide was 64,6 and 92,6 per cent effective respectively against adult naturally acquired infestations.
| Excerpt | Relevance | Reference |
|---|---|---|
| " Three separate flocks of hill sheep were used in this study in which the aim of the dosing programme followed was to kill the majority of liver flukes (Fasciola hepatica) before they reached adult egg laying stage, thereby eliminating, or considerably reducing, the number of eggs passed on to the pasture." | ( A study of a strategic dosing programme against ovine fascioliasis on a hill farm. Fawcett, AR; Whitelaw, A, 1977) | 0.26 |
| " The halflifes of degradation in blood is depending on the dosage and is 7 days related to the therapeutical dosage of 5 mg/kg bodymass against Fasciola hepatica." | ( [Degradation and residue dynamics of the anthelminthic 131J-rafoxanide in cattle blood, milk, meat and fat after various dosages]. Dedek, W; Liebaug, E; Schwarz, H, 1977) | 0.5 |
| "The effects of a programme of repeated dosing of all stock for fascioliasis over a four year period on a north Devon farm is described." | ( Observations on the repeated treatment for fascioliasis of stock on a farm in south-west England. Whitehead, JD, 1976) | 0.26 |
| " Diamphenethide at a dosage rate of 100 mg/kg body weight was found 99." | ( The comparative efficacy of diamphenethide and rafoxanide against fasciola gigantica in sheep. Kadhim, JK, 1975) | 0.51 |
| " The recommended therapeutic dosage is 3 mg/kg." | ( The safety of injectable rafoxanide in cattle. Schröder, J, 1982) | 0.57 |
| " It is postulated that the adoption of a strategic dosing programme over a period of three to four years would limit egg deposition on pastures close to eradication levels and that several years without needing to use anthelmintics against liver flukes would ensue." | ( Further studies in the control of ovine fascioliasis by strategic dosing. Fawcett, AR; Whitelaw, A, 1981) | 0.26 |
| "Groups of parasite-free lambs which were either housed and fed hay and concentrates or were grazing on pasture were dosed with the oral flukicides rafoxanide and triclabendazole and subsequent plasma concentrations monitored." | ( Effects of dietary variations on plasma concentrations of oral flukicides in sheep. Blanchflower, J; Hewitt, SA; Kennedy, DG; Mallon, TR; Taylor, SM, 1993) | 0.49 |
| "In solid dosage formulations, probing intermolecular interactions between active pharmaceutical ingredients (APIs) and polymeric excipients, which have a mechanistic impact on physical stability as well as bioavailability, remains a challenge." | ( Understanding Molecular Interactions in Rafoxanide-Povidone Amorphous Solid Dispersions from Ultrafast Magic Angle Spinning NMR. Amoureux, JP; Li, M; Lu, X; Meng, F; Su, Y; Tsutsumi, Y; Xu, W; Zhang, F, 2020) | 0.83 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 2.8934 | 0.0447 | 17.8581 | 100.0000 | AID485294; AID485341 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 79.4328 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 32.1968 | 0.0072 | 15.7588 | 89.3584 | AID624030 |
| chaperonin-containing TCP-1 beta subunit homolog | Homo sapiens (human) | Potency | 19.9526 | 3.9811 | 27.7649 | 39.8107 | AID504842 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 25.3735 | 3.1890 | 29.8841 | 59.4836 | AID1224846; AID1224894 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 24.1739 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 53.1764 | 0.0316 | 37.5844 | 354.8130 | AID504865; AID743255 |
| TDP1 protein | Homo sapiens (human) | Potency | 27.4490 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 29.8493 | 0.0007 | 14.5928 | 83.7951 | AID1259369 |
| TSHR protein | Homo sapiens (human) | Potency | 1.5101 | 0.3381 | 19.0466 | 37.9330 | AID602292 |
| AR protein | Homo sapiens (human) | Potency | 22.5315 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID743053; AID743063 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 23.7101 | 0.0006 | 57.9133 | 22,387.1992 | AID1259377 |
| progesterone receptor | Homo sapiens (human) | Potency | 21.2718 | 0.0004 | 17.9460 | 75.1148 | AID1346784; AID1346795 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 12.5706 | 0.0123 | 7.9835 | 43.2770 | AID1346984; AID1645841 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 26.8325 | 0.0002 | 14.3764 | 60.0339 | AID720691 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 32.5548 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159555 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 4.1474 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID1159531 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 32.2774 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 33.4889 | 0.3758 | 27.4851 | 61.6524 | AID743217 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 24.4952 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982; AID1346985 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 28.0477 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID743069; AID743075; AID743079; AID743080; AID743091 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 19.4971 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| 67.9K protein | Vaccinia virus | Potency | 10.0000 | 0.0001 | 8.4406 | 100.0000 | AID720580 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 35.4813 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 18.8322 | 0.0010 | 19.4141 | 70.9645 | AID743191 |
| IDH1 | Homo sapiens (human) | Potency | 29.0929 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 1.4125 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 14.9601 | 0.0007 | 23.0674 | 1,258.9301 | AID743085 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 7.5624 | 19.7391 | 45.9784 | 64.9432 | AID1159509 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 22.3872 | 0.5406 | 17.6392 | 96.1227 | AID2528 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 50.1187 | 0.3548 | 28.0659 | 89.1251 | AID504847 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 29.0929 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
| parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 112.2020 | 3.5481 | 19.5427 | 44.6684 | AID743266 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 25.0927 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 22.6856 | 0.0420 | 27.3789 | 61.6448 | AID743210; AID743228 |
| huntingtin isoform 2 | Homo sapiens (human) | Potency | 12.5893 | 0.0006 | 18.4198 | 1,122.0200 | AID1688 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 50.1187 | 0.1337 | 25.4129 | 89.1251 | AID588795 |
| serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Potency | 23.7781 | 0.1683 | 16.4040 | 67.0158 | AID720504 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 6.6819 | 0.0006 | 27.2152 | 1,122.0200 | AID743219 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 89.1251 | 0.4256 | 12.0591 | 28.1838 | AID504891 |
| DNA polymerase eta isoform 1 | Homo sapiens (human) | Potency | 75.7588 | 0.1000 | 28.9256 | 213.3130 | AID588591; AID720502 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 22.3872 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 25.2171 | 0.0079 | 8.2332 | 1,122.0200 | AID2546; AID2551 |
| geminin | Homo sapiens (human) | Potency | 1.1582 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 13.3714 | 0.0316 | 22.3146 | 100.0000 | AID720501 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 10.1815 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 26.6514 | 0.2512 | 15.8432 | 39.8107 | AID504327 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 33.4915 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
| Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) | Potency | 39.8107 | 6.3096 | 60.2008 | 112.2020 | AID720709 |
| Interferon beta | Homo sapiens (human) | Potency | 33.2940 | 0.0033 | 9.1582 | 39.8107 | AID1347407 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 11.0685 | 0.0023 | 19.5956 | 74.0614 | AID651631; AID720552 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 33.4915 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 31.6228 | 1.9953 | 25.5327 | 50.1187 | AID624288 |
| TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 35.4813 | 1.7783 | 16.2081 | 35.4813 | AID652104 |
| Rap guanine nucleotide exchange factor 4 | Homo sapiens (human) | Potency | 39.8107 | 3.9811 | 46.7448 | 112.2020 | AID720708 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 33.4915 | 0.0119 | 17.9420 | 71.5630 | AID651632 |
| Ataxin-2 | Homo sapiens (human) | Potency | 33.4915 | 0.0119 | 12.2221 | 68.7989 | AID651632 |
| [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) |
|---|---|---|---|---|---|---|---|
| envelope glycoprotein | Human immunodeficiency virus 1 | IC50 (µMol) | 19.7000 | 2.2000 | 14.8200 | 82.2000 | AID1986 |
| 60 kDa heat shock protein, mitochondrial | Homo sapiens (human) | IC50 (µMol) | 2.8000 | 0.1700 | 4.5590 | 10.0000 | AID1423480 |
| 10 kDa heat shock protein, mitochondrial | Homo sapiens (human) | IC50 (µMol) | 2.8000 | 0.1700 | 4.5590 | 10.0000 | AID1423480 |
| Thiosulfate sulfurtransferase | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0600 | 3.9631 | 9.7000 | AID1423472 |
| Chitinase | Onchocerca volvulus | IC50 (µMol) | 0.3400 | 0.3400 | 1.1800 | 1.6000 | AID1158751 |
| Chitinase | Onchocerca volvulus | Ki | 0.1300 | 0.1300 | 0.3560 | 0.4700 | AID1158753 |
| 60 kDa chaperonin | Escherichia coli | IC50 (µMol) | 3.2500 | 0.0390 | 3.5552 | 9.8000 | AID1423469; AID1423470 |
| 10 kDa chaperonin | Escherichia coli | IC50 (µMol) | 3.2500 | 0.0390 | 3.5552 | 9.8000 | AID1423469; AID1423470 |
| [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) |
|---|---|---|---|---|---|---|---|
| streptokinase A precursor | Streptococcus pyogenes M1 GAS | EC50 (µMol) | 0.0600 | 0.0600 | 8.9128 | 130.5170 | AID1902 |
| [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. |
| AID1347161 | Confirmatory screen NINDS Rhodamine 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. |
| AID1347157 | Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS | 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. |
| 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. |
| AID1347169 | Tertiary RLuc qRT-PCR qHTS assay 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. |
| 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. |
| AID1347149 | Furin counterscreen 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. |
| 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. |
| AID1508628 | Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| 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. |
| 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. |
| AID1347167 | Vero cells viability 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. |
| 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. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347153 | Confirmatory 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. |
| AID1508629 | Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| 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. |
| AID1347158 | ZIKV-mCherry secondary 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. |
| AID1347163 | 384 well plate NINDS AMC confirmatory 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. |
| 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. |
| 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. |
| 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. |
| AID1347170 | Vero cells viability counterscreen for qRT-PCR qHTS assay of selected 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. |
| 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. |
| AID1347156 | DAPI mCherry counterscreen 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. |
| 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. |
| AID1508627 | Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| AID1347164 | 384 well plate NINDS Rhodamine confirmatory 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. |
| AID1347152 | Confirmatory screen NINDS 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. |
| AID1347168 | HepG2 cells viability 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347172 | Secondary qRT-PCR qHTS assay for selected 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. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID720501 | qHTS for Inhibitors of Polymerase Kappa: Confirmatory Assay for Cherry-picked Compounds | 2012 | PloS one, , Volume: 7, Issue:10 | A comprehensive strategy to discover inhibitors of the translesion synthesis DNA polymerase κ. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1423480 | Inhibition of human N-terminal octa-His-tagged HSP60 expressed in Escherichia coli Rosetta(DE3) pLysS/human HSP10 expressed in Escherichia coli Rosetta(DE3) assessed as reduction in HSP60/HSP10-mediated denatured MDH refolding after 40 to 60 mins by spect | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
| AID1423474 | Antibacterial activity against Enterococcus faecium ATCC 19434 after 24 hrs by bacterial proliferation assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
| AID1423476 | Antibacterial activity against Klebsiella pneumoniae ATCC 13883 after 6 to 8 hrs by bacterial proliferation assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
| AID1150176 | Fasciolicidal activity against Fasciola hepatica metacercariae infected in po dosed rat assessed as elimination of liver flukes administered as single dose | 1977 | Journal of medicinal chemistry, Sep, Volume: 20, Issue:9 | 4-amino-6-(trichloroethenyl)-1,3-benzenedisulfonamide, a new, potent fasciolicide. |
| AID1158773 | Cytotoxicity against human HEK293T/17 cells assessed as cell viability at 1 to 10 uM for 24 hrs by MTS assay | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
| AID1158754 | Inhibition of Brugia malayi chitinase using 20 uM 4-methylumbelliferyl-N,N',N''-beta-chitotrioside as substrate at 10 uM after 10 mins by microplate reader analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
| AID1423473 | Inhibition of refolded MDH (unknown origin) preincubated with Escherichia coli GroEL/GroES for 45 mins in absence of compound followed by compound addition and measured for 20 to 35 mins by spectrometric analysis | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
| AID1158759 | Drug accumulation in Caenorhabditis elegans at 10 uM after 6 hrs by LC-MS analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
| AID1423478 | Antibacterial activity against Pseudomonas aeruginosa ATCC 10145 after 24 hrs by bacterial proliferation assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
| AID1423470 | Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured rhodanese refolding after 45 mins by spectrometric analysis | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
| AID1158767 | Antiparasitic activity against Onchocerca volvulus assessed as inhibition of L3 to L4 larval molting at 10 uM for 24 hrs measured until 6 days by using inverted microscopic analysis in presence of PBMC | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
| AID1158768 | Antiparasitic activity against Onchocerca volvulus assessed as inhibition of L3 to L4 larval molting at 1 uM for 24 hrs measured until 6 days by using inverted microscopic analysis in presence of PBMC | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
| AID1423477 | Antibacterial activity against Acinetobacter baumannii ATCC 19606 after 24 hrs by bacterial proliferation assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
| AID1158765 | Drug accumulation in Caenorhabditis elegans at 10 uM after 12 hrs by LC-MS analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
| AID1854974 | Binding affinity to Mycobacterium tuberculosis FAAL32 assessed as change in melting temperature at 2.5 uM by NanoDSF assay | 2022 | Bioorganic & medicinal chemistry, 10-01, Volume: 71 | Drug screening approach against mycobacterial fatty acyl-AMP ligase FAAL32 renews the interest of the salicylanilide pharmacophore in the fight against tuberculosis. |
| AID1423475 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC BAA-44 after 6 to 8 hrs by bacterial proliferation assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
| AID1423482 | Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue reporter assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
| AID1158751 | Inhibition of Onchocerca volvulus L3 larvae chitinase using 20 uM 4-methylumbelliferyl-N,N',N''-beta-chitotrioside as substrate after 10 mins by microplate reader analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
| AID1158758 | Protonophoric activity in human HEK293T/17 cells assessed as mitochondrial membrane depolarization at 50 uM for 30 mins by TMRE dye based flow cytometry | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
| AID1158753 | Competitive inhibition of Onchocerca volvulus L3 larvae chitinase using 20 uM 4-methylumbelliferyl-N,N',N''-beta-chitotrioside as substrate after 10 mins by microplate reader analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
| AID1158752 | Inhibition of Onchocerca volvulus L3 larvae chitinase using 20 uM 4-methylumbelliferyl-N,N',N''-beta-chitotrioside as substrate at 10 uM after 10 mins by microplate reader analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
| AID741324 | Induction of internalization of Frizzled1-GFP (unknown origin) expressed in human U2OS cells at 12.5 uM after 6 hrs by confocal microscopy | 2013 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7 | Small molecule modulators of Wnt/β-catenin signaling. |
| AID1158755 | Inhibition of Entamoeba histolytica chitinase using 20 uM 4-methylumbelliferyl-N,N',N''-beta-chitotrioside as substrate at 10 uM after 10 mins by microplate reader analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
| AID1423472 | Inhibition of refolded rhodanese (unknown origin) preincubated with Escherichia coli GroEL/GroES for 60 mins in absence of compound followed by compound addition by spectrometric analysis | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
| AID1158756 | Inhibition of Plasmodium falciparum chitinase using 20 uM 4-methylumbelliferyl-N,N',N''-beta-chitotrioside as substrate at 10 uM after 10 mins by microplate reader analysis | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
| AID192640 | In vitro for fasciolicidal activity against Fasciola hepatica infections in rats following s.c. administration. | 1985 | Journal of medicinal chemistry, Jan, Volume: 28, Issue:1 | Potentiation of fasciolicidal agents by benzoyl side chains. Synthesis of benzoylsalicylanilides. |
| AID1423469 | Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured MDH refolding after 20 to 40 mins by spectrometric analysis | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
| AID1158757 | Protonophoric activity in human HEK293T/17 cells assessed as mitochondrial membrane depolarization at 50 uM for 30 mins by TMRE dye based fluorescence spectrometry | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting. |
| AID1423471 | Antibacterial activity against Staphylococcus aureus ATCC 25923 after 6 to 8 hrs by bacterial proliferation assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
| AID1423479 | Antibacterial activity against Enterobacter cloacae subsp. cloacae ATCC 13047 after 24 hrs by bacterial proliferation assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
| AID1854971 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv incubated for 24 hrs and measured by MTT assay | 2022 | Bioorganic & medicinal chemistry, 10-01, Volume: 71 | Drug screening approach against mycobacterial fatty acyl-AMP ligase FAAL32 renews the interest of the salicylanilide pharmacophore in the fight against tuberculosis. |
| AID1423481 | Cytotoxicity against human THLE3 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue reporter assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 54 (41.86) | 18.7374 |
| 1990's | 18 (13.95) | 18.2507 |
| 2000's | 9 (6.98) | 29.6817 |
| 2010's | 30 (23.26) | 24.3611 |
| 2020's | 18 (13.95) | 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 strong demand-to-supply ratio for research on this compound.
| This Compound (45.12) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 8 (6.02%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 1 (0.75%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 124 (93.23%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||