Amitraz is a formamidine acaricide used to control mites and ticks in agricultural and veterinary settings. It is synthesized through a multi-step process involving the reaction of 2,4-dimethylphenyl isocyanate with N,N-dimethylformamide. Amitraz acts as a non-systemic insecticide, primarily affecting the nervous system of target pests. It is known to interfere with the transmission of nerve impulses by binding to octopamine receptors, leading to paralysis and death. Amitraz is highly effective against a wide range of mites and ticks, including those that are resistant to other acaricides. Its broad-spectrum activity and effectiveness make it a valuable tool in pest control, particularly in agriculture and animal husbandry. However, concerns regarding its potential toxicity to non-target organisms, including bees and fish, have led to restrictions on its use in some countries. Continued research into the environmental fate, toxicology, and development of safer alternatives to amitraz is ongoing. Amitraz is extensively studied due to its effectiveness against various pests, its potential toxicity to beneficial organisms, and the need for sustainable pest control methods. Research focuses on understanding its mode of action, environmental impact, and development of safer alternatives.'
amitraz: ixodicide (tick control); structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
amitraz : A tertiary amino compound that is 1,3,5-triazapenta-1,4-diene substituted by a methyl group at position 3 and 2,4-dimethylphenyl groups at positions 1 and 5. [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 | 36324 |
| CHEMBL ID | 1365675 |
| CHEBI ID | 2665 |
| SCHEMBL ID | 37309 |
| SCHEMBL ID | 13346111 |
| SCHEMBL ID | 19312984 |
| MeSH ID | M0063921 |
| Synonym |
|---|
| AC-12471 |
| AKOS005444180 |
| u-36059 |
| nsc-324552 |
| bts-27419 |
| n'-(2,4-dimethylphenyl)imino]methyl]-n-methylmethanimidamide |
| baam |
| 1,4-dimethylphenyl)-3-methyl-1,3,5-triazapenta-1,4-diene |
| nsc324552 |
| triazid |
| methanimidamide,4-dimethylphenyl)-n-[[(2,4-dimethylphenyl)imino]methyl]-n-methyl- |
| n,4-xylidine] |
| 2, n,n'-(methyliminodimethylidyne)bis- |
| CHEBI:2665 , |
| n'-(2,4-dimethylphenyl)-n-{[(2,4-dimethylphenyl)imino]methyl}-n-methylmethanimidamide |
| n,n'-(methyliminodimethylidyne)bis-2,4-xylidine |
| 1,5-di(2,4-dimethylphenyl)-3-methyl-1,3,5-triazapenta-1,4-diene |
| BSPBIO_003544 |
| STK368623 |
| n'-(2,4-dimethylphenyl)-n-{(e)-[(2,4-dimethylphenyl)imino]methyl}-n-methylimidoformamide (non-preferred name) |
| 33089-61-1 |
| mitac |
| amitraz |
| amitraz, analytical standard |
| D02380 |
| amitraz (usp/inn) |
| NCGC00094572-03 |
| NCGC00094572-04 |
| NCGC00094572-02 |
| NCGC00094572-01 |
| u 36059 |
| epa pesticide chemical code 106201 |
| nsc 324552 |
| acarac |
| bts 27419 |
| ccris 1552 |
| fumilat a |
| formamidine, n-methyl-n'-2,4-xylyl-n-(n-2,4-xylylformimidoyl)- |
| 1,5-di-(2,4-dimethylphenyl)-3-methyl-1,3,5-triazapenta-1,4-diene |
| bts 27,419 |
| mitaban |
| amitraze [french] |
| taktic |
| 2,4-xylidine, n,n'-(methyliminodimethylidyne)bis- |
| n,n'-((methylimino)dimethylidyne)bis(2,4-xylidine) |
| n,n-bis(2,4-xylyliminomethyl)methylamine |
| ent 27967 |
| einecs 251-375-4 |
| azadieno |
| ectodex |
| r.d. 27419 |
| n'-(2,4-dimethylphenyl)-n-(((2,4-dimethylphenyl)imino)methyl)-n-methylmethanimidamide |
| n,n'-((methylimino)dimethylidyne)di-2,4-xylidine |
| hsdb 6939 |
| caswell no. 374a |
| amitrazum [inn-latin] |
| bipin |
| azaform |
| brn 2946590 |
| ai3-27967 |
| 2-methyl-1,3-di(2,4-xylylimino)-2-azapropane |
| edrizar |
| amitraz estrella |
| mitaban (veterinary) |
| u-36,059 |
| n-methylbis(2,4-xylyliminomethyl)amine |
| n-methyl-n'-2,4-xylyl-n-(n-2,4-xylylformimidoyl)formamidine |
| boots bts 27419 |
| n-methyl-bis(2,4-xylyliminomethyl)amin |
| methanimidamide, n'-(2,4-dimethylphenyl)-n-(((2,4-dimethylphenyl)imino)methyl)-n-methyl- |
| n,n-di-(2,4-xylyliminomethyl)methylamine |
| upjohn u-36059 |
| KBIO3_002829 |
| SPBIO_001146 |
| SPECTRUM3_001944 |
| SPECTRUM2_001243 |
| SPECTRUM1505299 |
| n'-(2,4-dimethylphenyl)-n-{(e)-[(2,4-dimethylphenyl)imino]methyl}-n-methylimidoformamide |
| NCGC00094572-06 |
| NCGC00094572-05 |
| HMS2093O18 |
| n'-(2,4-dimethylphenyl)-n-[(2,4-dimethylphenyl)iminomethyl]-n-methylmethanimidamide |
| HMS1922B10 |
| u-36-059 |
| certifect |
| CHEMBL1365675 |
| NCGC00094572-08 |
| NCGC00094572-07 |
| NCGC00254832-01 |
| tox21_300930 |
| NCGC00258909-01 |
| tox21_201357 |
| n'-(2,4-dimethylphenyl)-n-[(2,4-dimethylphenyl)iminomethyl]-n-methyl-formamidine |
| A821615 |
| pharmakon1600-01505299 |
| nsc-758952 |
| nsc758952 |
| dtxcid403871 |
| cas-33089-61-1 |
| dtxsid5023871 , |
| tox21_111299 |
| S3643 |
| CCG-39116 |
| 33iah5017s , |
| amitraz [usan:usp:inn:ban] |
| unii-33iah5017s |
| amitraze |
| amitrazum |
| ovasyn |
| FT-0629369 |
| promeris duo component amitraz |
| amitraz component of promeris duo |
| amitraz [usp-rs] |
| amitraz [usp monograph] |
| amitraz [mi] |
| amitraz [mart.] |
| amitraz [usan] |
| amitraz [hsdb] |
| amitraz [green book] |
| amitraz [ema epar veterinary] |
| amitraz [inn] |
| SCHEMBL37309 |
| NCGC00094572-12 |
| tox21_111299_1 |
| KS-5123 |
| SCHEMBL13346111 |
| CS-4710 |
| amitraz, british pharmacopoeia (bp) reference standard |
| n'-(2,4-dimethylphenyl)-n-([(2,4-dimethylphenyl)imino]methyl)-n-methylimidoformamide |
| triatix |
| oms 1820 |
| istambul |
| tudy |
| acadrex |
| n-methyl-bis(2,4-xylyliminomethyl)amine |
| triatox |
| methanimidamide, n'-(2,4-dimethylphenyl)-n-[[(2,4-dimethylphenyl)imino]methyl]-n-methyl- |
| mtiaban |
| QXAITBQSYVNQDR-UHFFFAOYSA-N |
| n-(2,4-dimethylphenyl)-n-[[(2,4-dimethylphenyl)imino]methyl]-n-methyl-methaniminamide |
| 1,5-bis(2,4-dimethylphenyl)-3-methyl-1,3,5-triazapenta-1,4-diene |
| bumetran |
| n-methylbis-(2,4-xylyliminomethyl)-amine |
| maitac |
| HY-B1111 |
| AB01563057_01 |
| AKOS026750163 |
| sr-05000001653 |
| SR-05000001653-1 |
| amitraz, united states pharmacopeia (usp) reference standard |
| amitraz, pestanal(r), analytical standard |
| EN300-194742 |
| amitraz 10 microg/ml in cyclohexane |
| amitraz 100 microg/ml in acetonitrile |
| SBI-0206759.P001 |
| n'-(2,4-dimethylphenyl)-n-[[(2,4-dimethylphenyl) imino]methyl]-n-methylmethanimidamide |
| pesticide4_amitraz_c19h23n3_n'-(2,4-dimethylphenyl)-n-{(e)-[(2,4-dimethylphenyl)imino]methyl}-n-methylimidoformamide |
| SCHEMBL19312984 |
| (e)-n'-(2,4-dimethylphenyl)-n-((e)-(2,4-dimethylphenylimino)methyl)-n-methylformimidamide |
| Q417878 |
| DB11373 |
| mfcd00069396 |
| HMS3885O17 |
| AMY3584 |
| ruthenium, dicyclopentadienyl- |
| NCGC00094572-11 |
| amitraz 1000 microg/ml in acetonitrile |
| EN300-27122106 |
| (e)-n'-(2,4-dimethylphenyl)-n-{[(2,4-dimethylphenyl)imino]methyl}-n-methylmethanimidamide |
| Z1946820482 |
| (e)-n'-(2,4-dimethylphenyl)-n-[(e)-[(2,4-dimethylphenyl)imino]methyl]-n-methylmethanimidamide |
| EN300-25358173 |
Amitraz is a formamidine group of compounds used in many parts of the world as an agricultural pesticide and an ectoparasiticide. Amitraz is an acaricide that is widely used in veterinary medicine to control the cattle tick Rhipicephalus microplus.
Amitraz has been shown to be successful in controlling mange and lice infestations on pigs. Amitraz has pharmacological activity, including monoamine oxidase inhibition, alpha-adrenergic agonist activity and it inhibits prostaglandin synthesis.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Amitraz has pharmacological activity, including monoamine oxidase inhibition, alpha-adrenergic agonist activity and it inhibits prostaglandin synthesis." | ( Extrapolation from safety data to management of poisoning with reference to amitraz (a formamidine pesticide) and xylene. Bonsall, JL; Turnbull, GJ, 1983) | 1.22 |
| "Amitraz has been shown to be successful in controlling mange and lice infestations on pigs which had failed to respond to diazinon and gamma-BHC, respectively, and by the use of a prophylactic programme to maintain pig herds mange free. " | ( Amitraz in the control of non-ixodide ectoparasites of livestock. Curtis, RJ, 1985) | 3.15 |
Amitraz does not inhibit contractions stimulated by acetylcholine, methacholine or dimethylphenylpiperazinium. Amitraz did not inhibit serum ChE activity.
| Excerpt | Reference | Relevance |
|---|---|---|
| "3. Amitraz did not inhibit contractions stimulated by acetylcholine, methacholine or dimethylphenylpiperazinium." | ( Effect of amitraz on contractions of the guinea-pig ileum in vitro. Pass, MA; Seawright, AA, 1982) | 1.18 |
| "Amitraz did not inhibit serum ChE activity." | ( Effects of amitraz given by different routes on rats. Adam, SE; al-Damegh, MS; al-Qarawi, AA, 1999) | 1.41 |
Treatment with amitraz (0.025%) eliminated the mites and resolved the clinical signs. Treatment with am itraz at 250 p.p.m. was effective and did not cause noticeable side effects.
| Excerpt | Reference | Relevance |
|---|---|---|
| "The amitraz-treated rats at the oral doses of 20 and 50mg/kg bw had no visible injury, i.e., any clinical signs of dysfunction observed in any of the animals." | ( Effects of exposure to amitraz on noradrenaline, serotonin and dopamine levels in brain regions of 30 and 60 days old male rats. Anadón, A; Castellano, V; Del Pino, J; Martínez, MA; Martínez-Larrañaga, MR; Ramos, E, 2013) | 1.18 |
| "Treatment with amitraz (0.025%) eliminated the mites and resolved the clinical signs." | ( Skin lesions associated with Demodex sp. in a llama (Lama glama). [corrected] Eo, KY; Jung, KY; Kim, S; Kwak, D; Kwon, OD; Kwon, SC; Shin, T; Yeo, YG, 2010) | 0.7 |
| "Treatment with amitraz at 250 p.p.m." | ( Demodicosis in nine prairie dogs (Cynomys ludovicianus). Hauptman, K; Jekl, V; Jeklova, E; Knotek, Z, 2006) | 0.67 |
| "Treatment with amitraz was effective and did not cause noticeable side effects." | ( Demodicosis in ferrets (Mustela putorius furo). Noli, C; van der Horst, HH; Willemse, T, 1996) | 0.63 |
Amitraz was reported not to pose unreasonable risks or adverse effects to humans or the environment. The other commercialized member of the formamidine family, chlordimeform, was removed from the market because of carcinogenic effects in animal studies.
| Excerpt | Reference | Relevance |
|---|---|---|
| "To evaluate the toxic effects of amitraz in dogs and their reversal by various doses of atipamezole." | ( Toxicity and kinetics of amitraz in dogs. Berny, PJ; Buronrosse, F; Cadoré, JL; Hugnet, C; Lorgue, G; Pineau, X, 1996) | 0.88 |
| "Based on 48 h LD50 estimates from topical bioassays, cypermethrin was more toxic than permethrin to Helicoverpa zea (Boddie) larvae and adults; however, the two pyrethroids did not differ significantly in their relative toxicities to Spodoptera frugiperda (J." | ( Toxicity of pyrethroids and effect of synergists to larval and adult Helicoverpa zea, Spodoptera frugiperda, and Agrotis ipsilon (Lepidoptera: Noctuidae). Knowles, CO; Usmani, KA, 2001) | 0.31 |
| "This study investigated the potential adverse effects of amitraz on the initiation and maintenance of pregnancy in Sprague-Dawley rats as well as its effects on embryo-fetal development after maternal exposure during the entire pregnancy period." | ( Evaluation of developmental toxicity of amitraz in Sprague-Dawley rats. Chung, MK; Kim, HC; Kim, JC; Kim, SH; Kim, YB; Moon, CJ; Park, SC; Shin, DH; Shin, JY; Yang, YS, 2007) | 0.85 |
| " Results from these four studies indicate repeated use of metaflumizone plus amitraz causes no adverse health effects when used as recommended in dogs as young as 8 weeks of age." | ( Safety of a topically applied spot-on formulation of metaflumizone plus amitraz for flea and tick control in dogs. Heaney, K; Lindahl, RG, 2007) | 0.8 |
| "In search for low-cost, safe and environmentally benign plant-based alternatives to commercial pesticides, the efficacy of Lippia javanica aqueous leaf extracts in controlling ticks on cattle, acute oral toxicity in mice and phytochemistry were evaluated." | ( Acaricidal efficacy against cattle ticks and acute oral toxicity of Lippia javanica (Burm F.) Spreng. Belmain, SR; Hamudikuwanda, H; Hove, T; Madzimure, J; Mvumi, BM; Nyahangare, ET; Stevenson, PC, 2011) | 0.37 |
| " Amitraz was reported not to pose unreasonable risks or adverse effects to humans or the environment unlike the other commercialized member of the formamidine family, chlordimeform, which was removed from the market because of carcinogenic effects in animal studies." | ( Molecular mechanisms of amitraz mammalian toxicity: a comprehensive review of existing data. Anadon, MJ; Capo, MA; del Pino, J; Díaz, MJ; Frejo, MT; Lobo, M; Moyano-Cires, PV, 2015) | 1.63 |
| " In result, it was determined that CYP, AMT and their combinations led to significant changes in the parameters investigated, and it was ascertained that long-term exposure to insecticides and the administration of insecticide combinations produced greater toxic effects in comparison with the administration of insecticides alone." | ( The toxic effect of cypermethrin, amitraz and combinations of cypermethrin-amitraz in rats. Eraslan, G; Kanbur, M; Karabacak, M; Şahin, S; Siliğ, Y; Soyer Sarıca, Z, 2016) | 0.71 |
| " Our results reveal potential secondary effects of amitraz to invertebrates and biomarkers that may aid in the interpretation of sub-lethal toxic responses to amitraz." | ( Amitraz toxicity to the midge Chironomus riparius: Life-history and biochemical responses. Lemos, MFL; Monteiro, HR; Novais, SC; Pestana, JLT; Soares, AMVM, 2019) | 2.21 |
| " Low efficacy and development of Varroa mite resistance to currently used Varroacides has increased the demand for innovative, effective treatment tool options that exhibit high efficacy, while minimizing adverse effects on honey bee fitness." | ( Evaluation of potential miticide toxicity to Varroa destructor and honey bees, Apis mellifera, under laboratory conditions. Bahreini, R; de Herdt, O; Docherty, C; Feindel, D; Muirhead, S; Nasr, M, 2020) | 0.56 |
A controlled clinical trial was carried out to assess the effectiveness of pyriprole, metaflumizone combined with amitraz, and fipronil-(S)-methoprene. Toxicity of the acaricide tau-fluvalinate increased in combination with other acaricides.
| Excerpt | Reference | Relevance |
|---|---|---|
| "A controlled clinical trial was performed to assess the effectiveness of a pyriprole (125 mg/ml) and a metaflumizone (150 mg/ml) combined with amitraz (150 mg/ml) spot-on treatment (recommended dosage) in preventing adult female sandflies (Phlebotomus perniciosus) from feeding on dogs." | ( The effectiveness of a pyriprole (125 mg/ml) and a metaflumizone (150 mg/ml) combined with amitraz (150 mg/ml) spot-on treatment in preventing Phlebotomus perniciosus from feeding on dogs. Franc, M; Roques, M; Thomas, C, 2008) | 0.77 |
| "A controlled clinical trial was carried out to assess the effectiveness of pyriprole, metaflumizone combined with amitraz, and fipronil-(S)-methoprene commercial spot-on products in preventing adult female Culex pipiens pipiens from feeding on dogs." | ( Efficacy of fipronil-(S)-methoprene, metaflumizone combined with amitraz, and pyriprole commercial spot-on products in preventing Culex pipiens pipiens from feeding on dogs. Bouhsira, E; Franc, M; Fysikopoulos, A, 2009) | 0.8 |
| " Toxicity of the acaricide tau-fluvalinate increased in combination with other acaricides and most other compounds tested (15 of 17) while amitraz toxicity was mostly unchanged (1 of 15)." | ( Acaricide, fungicide and drug interactions in honey bees (Apis mellifera). Dahlgren, L; Ellis, MD; Johnson, RM; Siegfried, BD, 2013) | 0.59 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "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 |
Four laboratory studies were conducted in Beagle dogs to evaluate the safety of a novel ectoparasiticide combination of metaflumizone plus amitraz. The dose-response bioassays were carried out using the larval immersion test (amitraz and IVM) and the modified larval packet test (flumethrin and coumaphos)
| Excerpt | Relevance | Reference |
|---|---|---|
| "5 mg/kg), prazosin (35 micrograms/kg) and yohimbine (10 micrograms/kg) in separate experiments antagonized the vasoconstrictor actions of amitraz and produced a parallel shift to the right of the amitraz dose-response curve." | ( Central and peripheral alpha-adrenoceptor actions of amitraz in the dog. Cullen, LK; Reynoldson, JA, 1990) | 0.73 |
| " Amitraz did not significantly shift the dose-response curve to isoprenaline or acetylcholine but antagonized histamine rate responses competitively in the presence of propranolol (2 X 10(-6) M)." | ( The cardiac effects of amitraz in the guinea-pig in vivo and in vitro. Pascoe, AL; Reynoldson, JA, 1986) | 1.49 |
| " Motor activity returned to control levels over 4-5 days after dosing with 100-200 mg/kg AMZ, whereas recovery was evident the day after administration of low doses (1-30 mg/kg)." | ( Investigations of amitraz neurotoxicity in rats. III. Effects on motor activity and inhibition of monoamine oxidase. MacPhail, RC; Moser, VC, 1989) | 0.61 |
| " Results show that amitraz was able: 1) to decrease locomotion and rearing frequencies of rats and to increase their immobility time in an open-field; 2) to displace to the left the control dose-response curve constructed to apomorphine-induced stereotyped behavior; 3) to potentiate both pentobarbital sleeping time and amphetamine effects on open-field behaviour of rats and 4) to increase not only the whole brain levels of noradrenaline but also the striatal levels of dopamine." | ( Effects of amitraz on motor function. Flório, JC; Palermo-Neto, J; Sakate, M, 1993) | 1 |
| " The participation of alpha2-adrenergic receptors in the sedative effect provoked by amitraz was studied by dosing yohimbine (0." | ( Characterization of the antinociceptive and sedative effect of amitraz in horses. Carregaro, AB; Gonçalves, SC; Harkins, JD; Mataqueiro, MI; Queiroz-Neto, A; Tobin, T; Zamur, G, 1998) | 0.76 |
| " Exposure time influenced the slope of the dose-response when paper was used as a substrate for amitraz." | ( Modification of the food and agriculture organization larval packet test to measure amitraz-susceptibility against ixodidae. Davey, RB; George, JE; Miller, RJ, 2002) | 0.76 |
| " However, when resistant strains were evaluated, only the Miller and the Soberanes techniques adequately estimated the dose-response relationship." | ( A comparison of three bioassay techniques to determine amitraz susceptibility in Boophilus microplus (Acari: Ixodidae). Davey, RB; George, JE; Miller, RJ; White, WH, 2007) | 0.59 |
| "Four laboratory studies were conducted in Beagle dogs to evaluate the safety of a novel ectoparasiticide combination of metaflumizone plus amitraz (ProMeris/ProMeris Duo for Dogs, Fort Dodge Animal Health, Overland Park, KS) when applied according to the recommended dosage of >/=20mgmetaflumizonekg(-1) plus >/=20mgamitrazkg(-1), at exaggerated and repeated dosages, and if accidentally orally ingested." | ( Safety of a topically applied spot-on formulation of metaflumizone plus amitraz for flea and tick control in dogs. Heaney, K; Lindahl, RG, 2007) | 0.77 |
| " One hundred eighty one dogs with tick infestation and 170 dogs with flea infestation (plus three dogs harboring both ticks and fleas) qualified as primary patients and were randomly allocated to one of two treatments in a ratio of approximately 2:1 for metaflumizone plus amitraz (minimum dosage of 20 plus 20mg/kg) or fipronil (at the recommended label rate)." | ( Evaluation of the efficacy and safety of a novel formulation of metaflumizone plus amitraz in dogs naturally infested with fleas and ticks in Europe. Adler, K; Delay, RL; Hellmann, K; Parker, L; Pfister, K; Rugg, D, 2007) | 0.74 |
| " Plasma or hair samples were collected from each dog just prior to dosing and periodically through 56 days after treatment." | ( Pharmacokinetics of metaflumizone and amitraz in the plasma and hair of dogs following topical application. Blond-Riou, F; DeLay, RL; Lacoste, E; Mezzasalma, T, 2007) | 0.61 |
| " The compounds were tested at their respective maximum field recommended concentration (MFRC), and, when strong lethal effects were observed, a dose-response assay with a dilution series of the MFRC was undertaken to calculate LC(50) values." | ( Compatibility of traditional and novel acaricides with bumblebees (Bombus terrestris): a first laboratory assessment of toxicity and sublethal effects. Besard, L; Cuvelier, X; Mommaerts, V; Smagghe, G; Sterk, G; Vandeven, J, 2010) | 0.36 |
| " For oral exposures via treated sugar water, the dose-response assay showed the LC(50) values for abamectin, bifenazate, bifenthrin and etoxazole to be 1/15 MFRC (1." | ( Compatibility of traditional and novel acaricides with bumblebees (Bombus terrestris): a first laboratory assessment of toxicity and sublethal effects. Besard, L; Cuvelier, X; Mommaerts, V; Smagghe, G; Sterk, G; Vandeven, J, 2010) | 0.36 |
| " Furthermore, there is missing information about the dose-response relationship for some mechanisms and toxic effects described for amitraz and its metabolites, the mechanism of action by which several toxic effects are produced, and amitraz pharmacokinetics on different species." | ( Molecular mechanisms of amitraz mammalian toxicity: a comprehensive review of existing data. Anadon, MJ; Capo, MA; del Pino, J; Díaz, MJ; Frejo, MT; Lobo, M; Moyano-Cires, PV, 2015) | 0.93 |
| " Therefore, awareness should be created about the high prevalence as well as the application, dosage and dilution of the acaricides to pastoralists, community animal health workers and para veterinarians in the study area." | ( Prevalence of cattle ixodid ticks and acaricides efficacy evaluation in Amibara district of Afar Region, Ethiopia. Aregawi, WG; Bayisa, L; Gutema, F; Hailemariam, T; Tesfaye, J, 2023) | 0.91 |
| Role | Description |
|---|---|
| acaricide | A substance used to destroy pests of the subclass Acari (mites and ticks). |
| xenobiotic | A xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means. |
| environmental contaminant | Any minor or unwanted substance introduced into the environment that can have undesired effects. |
| insecticide | Strictly, a substance intended to kill members of the class Insecta. In common usage, any substance used for preventing, destroying, repelling or controlling insects. |
| [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 |
|---|---|
| tertiary amino compound | A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups. |
| formamidines | Amidines with the general formula R(1)N=CHNR(2)R(3) (R(1), R(2), R(3) can be H). |
| [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, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 31.6228 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 55.0520 | 3.1890 | 29.8841 | 59.4836 | AID1224846; AID1224894 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 37.8585 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 63.7023 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
| AR protein | Homo sapiens (human) | Potency | 54.1455 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID743035; AID743036 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 45.3050 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224893 |
| progesterone receptor | Homo sapiens (human) | Potency | 38.5316 | 0.0004 | 17.9460 | 75.1148 | AID1346784 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 25.1050 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 55.3420 | 0.0002 | 14.3764 | 60.0339 | AID720691; AID720692; AID720719 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 64.3115 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 14.5807 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID1159531 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 51.6885 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 61.9240 | 0.3758 | 27.4851 | 61.6524 | AID743217 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 15.4178 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 40.9310 | 0.0002 | 29.3054 | 16,493.5996 | AID743069; AID743075; AID743078; AID743079; AID743080 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 36.2898 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 39.0190 | 0.0010 | 19.4141 | 70.9645 | AID588536; AID588537; AID743191 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 21.0596 | 0.0237 | 23.2282 | 63.5986 | AID743222; AID743223 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 45.1450 | 0.0007 | 23.0674 | 1,258.9301 | AID651777; AID743085; AID743122 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 68.6943 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 55.0520 | 19.7391 | 45.9784 | 64.9432 | AID1159509 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 35.2907 | 0.0578 | 21.1097 | 61.2679 | AID1159526; AID1159528 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 44.6684 | 0.0100 | 39.5371 | 1,122.0200 | AID588545 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 19.9526 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 51.3344 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 56.5655 | 0.0420 | 27.3789 | 61.6448 | AID743210; AID743228 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 37.2078 | 0.0006 | 27.2152 | 1,122.0200 | AID651741; AID743219 |
| geminin | Homo sapiens (human) | Potency | 33.4983 | 0.0046 | 11.3741 | 33.4983 | AID624297 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 0.0009 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 65.1240 | 0.0023 | 19.5956 | 74.0614 | AID651631; AID720552 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Peroxisome proliferator-activated receptor alpha | Homo sapiens (human) | Potency | 39.8107 | 0.0158 | 23.5273 | 44.6684 | AID651778 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| [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) |
|---|---|---|---|---|---|---|---|
| Alpha-2A adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 0.9269 | 0.0000 | 1.4421 | 7.3470 | AID625201 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 0.3476 | 0.0001 | 0.8074 | 10.0000 | AID625201 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID651635 | Viability Counterscreen for 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. |
| 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| AID547622 | Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease. |
| AID1104470 | Contact toxicity against worker Bombus terrestris (bumblebee) assessed as mortality at 400 mg a.i./l applied on the dorsal thorax for 11 weeks measured everyday for 3 days followed by once a week for 11 weeks | 2010 | Pest management science, Jul, Volume: 66, Issue:7 | Compatibility of traditional and novel acaricides with bumblebees (Bombus terrestris): a first laboratory assessment of toxicity and sublethal effects. |
| 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. |
| AID1104399 | Contact toxicity against worker Bombus terrestris (bumblebee) assessed as reduction in reproduction at 400 mg a.i./l applied on the dorsal thorax for 11 weeks measured once a week for 11 weeks relative to control | 2010 | Pest management science, Jul, Volume: 66, Issue:7 | Compatibility of traditional and novel acaricides with bumblebees (Bombus terrestris): a first laboratory assessment of toxicity and sublethal effects. |
| AID1104446 | Toxicity against worker Bombus terrestris (bumblebee) assessed as mortality at 400 mg a.i./l, po administered through sugar water for 11 weeks measured everyday for 3 days followed by once a week for 11 weeks | 2010 | Pest management science, Jul, Volume: 66, Issue:7 | Compatibility of traditional and novel acaricides with bumblebees (Bombus terrestris): a first laboratory assessment of toxicity and sublethal effects. |
| AID547621 | Cytotoxicity against BESM cells after 88 hrs by HTS assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease. |
| AID1112909 | Agonist activity at Chilo suppressalis (rice stem borer) tyramine receptor TyR1 expressed in HEK293 cells assessed as reduction in forskolin-induced cAMP accumulation at < 1 umol incubated for 20 min | 2013 | Pest management science, Jan, Volume: 69, Issue:1 | Molecular cloning and pharmacological characterisation of a tyramine receptor from the rice stem borer, Chilo suppressalis (Walker). |
| AID1104371 | Toxicity against worker Bombus terrestris (bumblebee) assessed as reduction in reproduction at 400 mg a.i./l, po administered through pollen for 11 weeks measured once a week for 11 weeks | 2010 | Pest management science, Jul, Volume: 66, Issue:7 | Compatibility of traditional and novel acaricides with bumblebees (Bombus terrestris): a first laboratory assessment of toxicity and sublethal effects. |
| AID1104422 | Toxicity against worker Bombus terrestris (bumblebee) assessed as mortality at 400 mg a.i./l, po administered through pollen for 11 weeks measured everyday for 3 days followed by once a week for 11 weeks | 2010 | Pest management science, Jul, Volume: 66, Issue:7 | Compatibility of traditional and novel acaricides with bumblebees (Bombus terrestris): a first laboratory assessment of toxicity and sublethal effects. |
| AID1104389 | Toxicity against worker Bombus terrestris (bumblebee) assessed as reduction in reproduction at 400 mg a.i./l, po administered through sugar water for 11 weeks measured once a week for 11 weeks relative to control | 2010 | Pest management science, Jul, Volume: 66, Issue:7 | Compatibility of traditional and novel acaricides with bumblebees (Bombus terrestris): a first laboratory assessment of toxicity and sublethal effects. |
| AID547804 | Selectivity window, ratio of EC50 for BESM cells to EC50 for Trypanosoma cruzi amastigotes infected in BESM cells | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease. |
| AID1112913 | Agonist activity at Chilo suppressalis (rice stem borer) tyramine receptor TyR1 expressed in HEK293 cells assessed as reduction in forskolin-induced cAMP accumulation at 10 uM incubated for 20 min | 2013 | Pest management science, Jan, Volume: 69, Issue:1 | Molecular cloning and pharmacological characterisation of a tyramine receptor from the rice stem borer, Chilo suppressalis (Walker). |
| AID1104443 | Toxicity against worker Bombus terrestris (bumblebee) assessed as mortality at 400 mg a.i./l, po administered through sugar water measured up to 1 week | 2010 | Pest management science, Jul, Volume: 66, Issue:7 | Compatibility of traditional and novel acaricides with bumblebees (Bombus terrestris): a first laboratory assessment of toxicity and sublethal effects. |
| 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. |
| 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. |
| 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. |
| 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 | 62 (14.73) | 18.7374 |
| 1990's | 59 (14.01) | 18.2507 |
| 2000's | 123 (29.22) | 29.6817 |
| 2010's | 126 (29.93) | 24.3611 |
| 2020's | 51 (12.11) | 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 (51.40) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 37 (8.43%) | 5.53% |
| Reviews | 19 (4.33%) | 6.00% |
| Case Studies | 42 (9.57%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 341 (77.68%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||