Methoxychlor is an organochlorine insecticide that was widely used in the mid-20th century. It is a synthetic compound, similar in structure to DDT. It was initially considered less toxic to mammals than DDT, and it was used to control a wide range of insect pests, particularly those affecting crops and livestock. However, concerns about its potential environmental and health effects, including its persistence in the environment and its ability to disrupt endocrine function, led to its gradual phase-out in many countries. Methoxychlor is synthesized through a multi-step process that involves the reaction of 2,2-bis(p-chlorophenyl)-1,1,1-trichloroethane (DDT) with methanol in the presence of a catalyst. Its effects on organisms include disruption of endocrine function, particularly in insects, leading to reproductive problems and population decline. It can also affect the nervous system and immune function. It is studied due to its potential for environmental contamination and its historical use as an insecticide, particularly in relation to its persistence in the environment and its potential to bioaccumulate in food chains. Ongoing research focuses on understanding its long-term impacts on ecosystems and human health, as well as exploring alternative methods of pest control.'
Methoxychlor: An insecticide. Methoxychlor has estrogenic effects in mammals, among other effects. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 4115 |
| CHEMBL ID | 362919 |
| CHEBI ID | 6842 |
| SCHEMBL ID | 116390 |
| MeSH ID | M0013601 |
| Synonym |
|---|
| EU-0084224 |
| BIDD:PXR0108 |
| BIDD:ER0613 |
| benzene, 1,1'-(2,2,2-trichloroethylidene)bis[4-methoxy- |
| ethane, 1,1,1-trichloro-2,2-bis(p-methoxyphenyl)- |
| 1-methoxy-4-[2,2,2-trichloro-1-(4-methoxyphenyl)ethyl]benzene |
| DIVK1C_006684 |
| 1,1'-(2,2,2-trichloroethane-1,1-diyl)bis[4-(methyloxy)benzene] |
| SPECTRUM_001949 |
| dmdt |
| methoxo |
| dimethoxy-dt |
| wln: gxggyr do1&r do1 |
| methoxcide |
| moxie |
| 1,1-trichloro-2,2-di(4-methoxyphenyl)ethane |
| methoxy-ddt |
| nsc8945 |
| 1,2,2-trichloroethylidene)bis(4-methoxybenzene) |
| p,p'-(dimethoxydiphenyl)trichloroethane |
| benzene,1'-(2,2,2-trichloroethylidene)bis[4-methoxy- |
| p,p'-dmdt |
| nsc-8945 |
| nci-c00497 |
| ethane,2-bis(p-anisyl)-1,1,1-trichloro- |
| p,p'-methoxychlor |
| 1,1-trichloro-2,2-bis(p-methoxyphenyl)ethane |
| ent 1,716 |
| metox |
| marlate |
| metoksychlor |
| ethane,1,1-trichloro-2,2-bis(p-methoxyphenyl)- |
| 1,1-trichloro-2,2-bis(p-anisyl)ethane |
| di(p-methoxyphenyl)trichloromethyl methane |
| meocl |
| maralate |
| dimethoxy-ddt |
| BSPBIO_002507 |
| MLS001055458 |
| NCGC00090760-01 |
| methoxychlor [95%] |
| NCGC00090760-02 |
| inchi=1/c16h15cl3o2/c1-20-13-7-3-11(4-8-13)15(16(17,18)19)12-5-9-14(21-2)10-6-12/h3-10,15h,1-2h |
| 1,1'-(2,2,2-trichloroethylidene)bis(4-methoxybenzene) |
| 2,2,2-trichloro-1,1-bis(4-methoxyphenyl)ethane |
| dimethoxydiphenyltrichloroethane |
| brn 2057367 |
| benzene, 1,1'-(2,2,2-trichloroethylidene)bis(4-methoxy- |
| oms 466 |
| 2,2-di-(p-methoxyphenyl)-1,1,1-trichloroethane |
| 4,4-(2,2,2-trichloroethylidene)dianisole |
| ethane, 2,2-bis(p-anisyl)-1,1,1-trichloro- |
| methoxychlor 2 ec |
| higalmetox |
| 2,2-di-p-anisyl-1,1,1-trichloroethane |
| 1,1,1-trichlor-2,2-bis(4-methoxy-phenyl)-aethan [german] |
| ccris 380 |
| nsc 8945 |
| 1,1,1-trichloro-2,2-bis(4-methoxyphenyl)ethane |
| rcra waste no. u247 |
| mezox k |
| dianisyltrichlorethane |
| metoksychlor [polish] |
| flo pro mcseed protectant |
| epa pesticide chemical code 034001 |
| caswell no. 550 |
| methoxychlor [bsi:iso] |
| p,p'-dimethoxydiphenyltrichloroethane |
| einecs 200-779-9 |
| hsdb 1173 |
| methoxychlore [iso-french] |
| 1,1-bis(p-methoxyphenyl)-2,2,2-trichloroethane |
| p,p'-dwumetoksydwufenylotrojchloroetan [polish] |
| dianisyl trichloroethane |
| methoxychlor, technical |
| rcra waste number u247 |
| double-m ec |
| 72-43-5 |
| methoxychlor |
| methoxychlor, analytical standard |
| 1,1,1-trichloro-2,2-di(4-methoxyphenyl)ethane |
| 1,1,1-trichloro-2,2-bis(p-methoxyphenyl)ethane |
| 1,1,1-trichloro-2,2-bis(p-anisyl)ethane |
| 2,2-bis(p-methoxyphenyl)-1,1,1-trichloroethane |
| 2,2-bis(p-anisyl)-1,1,1-trichloroethane |
| 1,1'-(2,2,2-trichloroethane-1,1-diyl)bis(4-methoxybenzene) |
| 2,2-di(p-methoxyphenyl)-1,1,1-trichloroethane |
| CHEBI:6842 , |
| NCGC00090760-03 |
| NCGC00090760-05 |
| NCGC00090760-04 |
| KBIOGR_001227 |
| KBIO2_002495 |
| KBIO2_005063 |
| KBIO1_001628 |
| KBIOSS_002503 |
| KBIO3_002007 |
| KBIO2_007631 |
| SPECTRUM2_001890 |
| SPECTRUM4_000704 |
| SPBIO_001800 |
| SPECPLUS_000588 |
| SPECTRUM3_000864 |
| SPECTRUM330077 |
| SPECTRUM5_002050 |
| NCGC00090760-07 |
| NCGC00090760-06 |
| methoxychlor (mxc) (1,1,1-trichloro-2,2-bis(p-methoxyphenyl)ethane) |
| MLS001065605 |
| smr000568481 |
| MXC , |
| M1736 |
| 1,1-bis(4-methoxyphenyl)-2,2,2-trichloroethane |
| CHEMBL362919 |
| AKOS001025493 |
| NCGC00090760-09 |
| NCGC00090760-10 |
| NCGC00090760-08 |
| NCGC00090760-11 |
| ria79ud69l , |
| methoxychlore |
| 1,1,1-trichlor-2,2-bis(4-methoxy-phenyl)-aethan |
| p,p'-dwumetoksydwufenylotrojchloroetan |
| unii-ria79ud69l |
| HMS3039K10 |
| dtxcid30827 |
| tox21_400075 |
| dtxsid9020827 , |
| cas-72-43-5 |
| CCG-39337 |
| bdbm50410535 |
| 1,1,1-trichloro-2,2-bis-(p-methoxyphenyl)ethane |
| FT-0603090 |
| benzene,1,1'-(2,2,2-trichloroethylidene)bis[4-methoxy- |
| methoxychlor [hsdb] |
| methoxychlor [mart.] |
| methoxychlor [mi] |
| methoxychlor [iso] |
| methoxychlor [who-dd] |
| methoxychlor [iarc] |
| SCHEMBL116390 |
| mesox k |
| pmethoxychlor |
| 2,2-di(p-anisyl)-1,1,1-trichloroethane |
| benzene, 1,1'-(2,2,2-trichloroethylidene)bis*4-methoxy- |
| 2,2-bis (p-methoxyphenol)-1,1,1-trichloroethane |
| 1-methoxy-4-[2,2,2-trichloro-1-(4-methoxyphenyl)ethyl]benzene # |
| marlate 300 flowable (salt/mix) |
| IAKOZHOLGAGEJT-UHFFFAOYSA-N |
| mfcd00000803 |
| methoxychlor, pestanal(r), analytical standard |
| 1644449-82-0 |
| methoxychlor 10 microg/ml in acetonitrile |
| methoxychlor 100 microg/ml in cyclohexane |
| methoxychlor 10 microg/ml in isooctane |
| 4,4'-(2,2,2-trichloroethane-1,1-diyl)bis(methoxybenzene) |
| Q411958 |
| STL575014 |
| dmdt;dimethoxy-ddt; marlate; mesox k; methoxcide; methoxy-ddt |
| methoxychlor (methoxy-ddt) |
| D91527 |
| 1,1,1-trichloro-2,2-bis (4-methoxyphenyl)ethane |
| BS-44127 |
| methoxychlor-d6 |
| pesticide mix 14 10 microg/ml in cyclohexane |
| methoxychlor-d14) |
| Z56755662 |
Methoxychlor (MXC) is an organopesticide classified as a "Proposed Persistent Organic Pollutant" in the Stockholm Convention. Recent studies revealed that MXC could induce DNA strand breaks, whereas its underlying mechanisms were underinvestigated.
Methoxychlor (MXC) has adverse effects on fertility and rat uteri via its active metabolite HPTE. Both methoxychlor and HPTE have been credited with estrogenic properties and have a weak anti-androgenic activity.
| Excerpt | Reference | Relevance |
|---|---|---|
| "The methoxychlor-mediated increase in CYP2B and 3A proteins was considerably larger than the increase in the corresponding enzymatic activities." | ( Induction of the hepatic CYP2B and CYP3A enzymes by the proestrogenic pesticide methoxychlor and by DDT in the rat. Effects on methoxychlor metabolism. Dehal, SS; Kupfer, D; Li, HC, 1995) | 1 |
Methoxychlor treatment did not significantly affect testicular morphology in the FVB mice, but markedly reduced the number of developing spermatocytes. Methoxychlor pretreatment significantly reduced intestinal metabolite formation from 32 +/- 4 to 15 +/- 6 pmol/min/mg.
| Excerpt | Reference | Relevance |
|---|---|---|
| " Recently we have shown that false-positive results can still be obtained due to cytotoxicity when loss of membrane integrity is a late event in toxic cell death relative to the induction of endonucleolytic DNA degradation." | ( Revalidation of the in vitro alkaline elution/rat hepatocyte assay for DNA damage: improved criteria for assessment of cytotoxicity and genotoxicity and results for 81 compounds. Barnum, JE; DeLuca, JG; Elia, MC; Harmon, LS; Kraynak, AR; McKelvey, TW; Nichols, WW; Storer, RD, 1996) | 0.29 |
| " In particular, the adverse effects were effectively detected in organ weights of accessory sex organs and histopathological examination." | ( A repeated 28-day oral dose toxicity study of methoxychlor in rats, based on the 'enhanced OECD test guideline 407' for screening endocrine-disrupting chemicals. Hatayama, K; Hirose, M; Katsumata, T; Kitamura, Y; Nakamura, A; Nakamura, H; Nishikawa, A; Nishimura, S; Okazaki, K; Okazaki, S; Tsuda, T, 2001) | 0.57 |
| " Cytochrome P450 enzymes metabolize MXC to mono-OH MXC (1,1,1-trichloro-2-(4-hydroxyphenyl)-2-(4-methoxyphenyl)ethane [mono-OH]) and bis-OH MXC (1,1,1-trichloro-2,2-bis(4-hydroxyphenyl)ethane [HPTE]), two compounds that are proposed to be more toxic than the parent compound, can interact with the estrogen receptor (ER), and are proposed to be responsible for ovarian toxicity." | ( Methoxychlor metabolites may cause ovarian toxicity through estrogen-regulated pathways. Flaws, JA; Gupta, RK; Miller, KP, 2006) | 1.78 |
| " The use of vtg1 mRNA induction in zebrafish embryos and larvae was found to be a sensitive biomarker of exposure to these organic compounds, and was helpful in elucidating their adverse effects and setting water quality guidelines." | ( Toxicity assessment and vitellogenin expression in zebrafish (Danio rerio) embryos and larvae acutely exposed to bisphenol A, endosulfan, heptachlor, methoxychlor and tetrabromobisphenol A. Chan, KM; Chan, WK; Chow, WS, 2013) | 0.59 |
| " Immunotoxicology focuses on the evaluation of the potential adverse effects of xenobiotics on immune mechanisms that can lead to harmful changes in host responses such as: increased susceptibility to infectious diseases and tumorigenesis; the induction of hypersensitivity reactions; or an increased incidence of autoimmune disease." | ( Immunotoxicity in mice induced by short-term exposure to methoxychlor, parathion, or piperonyl butoxide. Fukuyama, T; Harada, T; Hayashi, K; Kosaka, T; Miyashita, L; Nishino, R; Tajima, Y; Ueda, H; Wada, K, ) | 0.38 |
| " The previous toxic effects were neutralized by the administration of propolis in MXC+propolis group." | ( The ameliorative effect of propolis against methoxychlor induced ovarian toxicity in rat. Aamer, AA; Abdel-Hafeez, MM; El-Sharkawy, EE; Elsherif, WM; Kames, AO; Nafady, AM; Nisr, NA; Sayed, SM; Wahba, NM, 2014) | 0.66 |
| 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 |
Rainbow trout and common carp were dosed orally with feed containing the pesticide methoxychlor (MXC) for 14days. GT1-7 cells were treated with methoxy chlor or chlorpyrifos for 24 h in dose-response experiments. GnRH gene expression and peptide l were measured as adults.
| Excerpt | Relevance | Reference |
|---|---|---|
| " The early pregnancy protocol provides dose-response information on the effects of short-term exposure of animals to compounds during early pregnancy." | ( Toxicological mechanisms of implantation failure. Cummings, AM, 1990) | 0.28 |
| " On Days 2 and 3 of pregnancy, 200 and 500 mg/kg/day MXC were found to accelerate embryo transport into the uterus; the 500 mg/kg/day dosage also reduced the total number of embryos recovered from the tract." | ( Methoxychlor accelerates embryo transport through the rat reproductive tract. Cummings, AM; Perreault, SD, 1990) | 1.72 |
| " Dose-response changes were observed in the oviduct and uterus but not vagina." | ( Morphological and biochemical alterations in reproductive tracts of neonatal female mice treated with the pesticide methoxychlor. Cooke, PS; Eroschenko, VP, 1990) | 0.49 |
| " In our studies rats were dosed from weaning through puberty , gestation, and lactation." | ( The development of a protocol to assess reproductive effects of toxicants in the rat. Cooper, R; Ferrell, J; Goldman, J; Gray, LE; Laskey, J; Linder, R; Ostby, J; Rehnberg, G; Sigmon, R, 1988) | 0.27 |
| " To address the short-term effects of MXC on fertility, the differential effects of MXC dosage and timing of administration (relative to implantation) on several gestational parameters were investigated." | ( Antifertility effect of methoxychlor in female rats: dose- and time-dependent blockade of pregnancy. Cummings, AM; Gray, LE, 1989) | 0.58 |
| "In the present study rats were dosed from weaning, through puberty and gestation, to Day 15 of lactation with methoxychlor at 25, 50, 100, or 200 mg/kg/day." | ( A dose-response analysis of methoxychlor-induced alterations of reproductive development and function in the rat. Cooper, R; Ferrell, J; Goldman, J; Gray, LE; Laskey, J; Linder, R; Ostby, J; Rehnberg, G; Slott, V, 1989) | 0.78 |
| " In another study, ovx female rats were dosed with M at 200 mg/kg/day and then with progesterone (P)." | ( Methoxychlor induces estrogen-like alterations of behavior and the reproductive tract in the female rat and hamster: effects on sex behavior, running wheel activity, and uterine morphology. Ferrell, JM; Goldman, JM; Gray, LE; Ostby, JS; Sigmon, ER, 1988) | 1.72 |
| "0 ppm in samples from the low and high dosage sprays." | ( Methoxychlor residues in milk of cattle treated with Marlate 50 insecticide as a dermal spray. Clark, KJ; Coppock, CE; Ivey, MC; Ivie, GW, 1983) | 1.71 |
| " Following priming with estrone, ovariectomized rats were treated with estrone plus progesterone, progesterone alone, or progesterone plus various dosage levels of MXC." | ( Replacement of estrogen by methoxychlor in the artificially-induced decidual cell response in the rat. Cummings, AM, 1993) | 0.58 |
| "The aim of this study was to perform a dose-response test to determine whether bovine oocytes exposed to dichlorodiphenyltrichloroethane (DDT), hexachlorocyclohexane (gammaHCH), or methoxychlor (MXC) in vitro would exhibit changes in maturation rates, cleavage rates at Day 2, or blastocyst rates at Day 7 to 8 after fertilization in vitro (IVF)." | ( Influence of organochlorine pesticides on maturation and postfertilization development of bovine oocytes in vitro. Alm, H; Kanitz, W; Tiemann, U; Torner, H, ) | 0.32 |
| " Weanling male Long-Evans hooded rats were dosed daily with M (po) at 0, 200, 300, or 400 mg kg-1 day-1 for 10 months." | ( The estrogenic and antiandrogenic pesticide methoxychlor alters the reproductive tract and behavior without affecting pituitary size or LH and prolactin secretion in male rats. Cooper, RL; Gray, LE; Kelce, WR; Ostby, J, ) | 0.39 |
| " In vivo studies indicated that the 3-day uterotrophic assay in prepubertal rats was the best method for detecting estrogenic activity when compared with all other end points, based upon the dose-response data for ethynyl estradiol (0." | ( Estrogenic activity of octylphenol, nonylphenol, bisphenol A and methoxychlor in rats. Bodman, GJ; Carey, SA; Cooper, RL; Ferrell, JM; Laws, SC, 2000) | 0.54 |
| "Temporal and dose-response relationships of vitellogenin (VTG) mRNA induction and subsequent plasma VTG accumulation were established for sheepshead minnows (Cyprinodon variegatus) treated with p-nonylphenol (an alkylphenol) and the organochlorine pesticides methoxychlor and endosulfan." | ( Effects of p-nonylphenol, methoxychlor, and endosulfan on vitellogenin induction and expression in sheepshead minnow (Cyprinodon variegatus). Bowman, CJ; Denslow, ND; Folmar, LC; Hemmer, BL; Hemmer, MJ; Hoglund, MD; Kroll, KJ; Marcovich, D, 2001) | 0.79 |
| " In most cases, however, the dose-response relationships were complex (non-monotonic), with effects at the highest dose examined being opposite to effects seen at lower doses." | ( Effects of prenatal exposure to low doses of diethylstilbestrol, o,p'DDT, and methoxychlor on postnatal growth and neurobehavioral development in male and female mice. Palanza, P; Parmigiani, S; vom Saal, FS, 2001) | 0.54 |
| " Basic performance of the task was established prior to dosing, training with simultaneous presentation of sample and choice stimuli continued during dosing, and delays (1/2, 1 or 2 s) were introduced near the end of the dosing period." | ( Cognitive testing (delayed non-match to sample) during oral treatment of female adolescent monkeys with the estrogenic pesticide methoxychlor. Golub, MS, ) | 0.34 |
| " We dosed chicks orally with estradiol benzoate (EB; 1, 10, 100, and 1000 nmol/g of body mass per day, days 5-11 posthatch), the non-ionic surfactant octylphenol (100 and 1000 nmol/g), or the pesticides methoxychlor (100 and 1000 nmol/g) and dicofol (100 nmol/g) and measured their song control nuclei as adults." | ( Oral estrogen masculinizes female zebra finch song system. Craig-Veit, CB; Erichsen, AL; Fry, DM; Millam, JR; Quaglino, AE; Viant, MR, 2002) | 0.5 |
| " Resulting male pups (14-16 per group) then were dosed directly from postnatal day 7 to 42." | ( The hidden effect of estrogenic/antiandrogenic methoxychlor on spermatogenesis. Chapin, RE; Hardy, VB; Harris, MW; Johnson, L; Staub, C, 2002) | 0.57 |
| " GT1-7 cells were treated with methoxychlor or chlorpyrifos for 24 h in dose-response experiments, and GnRH gene expression and peptide levels were quantified." | ( Organochlorine pesticides directly regulate gonadotropin-releasing hormone gene expression and biosynthesis in the GT1-7 hypothalamic cell line. Gore, AC, 2002) | 0.6 |
| " To test this hypothesis, cycling female CD-1 mice (39 days) were dosed with MXC (8, 16, or 32 mg/kg/day), kepone (KPN, 8 mg/kg/day, positive control), or sesame oil (vehicle control) via intraperitoneal injection for 10 or 20 days." | ( Methoxychlor may cause ovarian follicular atresia and proliferation of the ovarian epithelium in the mouse. Borgeest, C; Flaws, JA; Hoyer, PB; Mayer, LP; Symonds, D, 2002) | 1.76 |
| " We thus found opposite effects of fetal exposure to a low and a high dose of DES on the uterine response to estradiol (inverted-U dose-response relationship)." | ( Uterine responsiveness to estradiol and DNA methylation are altered by fetal exposure to diethylstilbestrol and methoxychlor in CD-1 mice: effects of low versus high doses. Alworth, LC; Besch-Williford, CL; Day, JK; Howdeshell, KL; Huang, TH; Lubahn, DB; Ruhlen, RL; vom Saal, FS, 2002) | 0.53 |
| " Resulting male pups (15/group) then were dosed directly from postnatal day 7 to 42." | ( The pesticide methoxychlor given orally during the perinatal/juvenile period, reduced the spermatogenic potential of males as adults by reducing their Sertoli cell number. Chapin, RE; Harris, MW; Johnson, L; Silge, RL; Staub, C, ) | 0.49 |
| "We previously performed dose-response studies of genistein, diisononyl phthalate, 4-nonylphenol, methoxychlor (MXC), and bisphenol A to examine the impact of maternal dietary exposure from gestational day 15 to postnatal day 10 on the development of rat reproductive system in later life." | ( Alteration of pituitary hormone-immunoreactive cell populations in rat offspring after maternal dietary exposure to endocrine-active chemicals. Hirose, M; Lee, KY; Masutomi, N; Shibutani, M; Takagi, H; Uneyama, C, 2004) | 0.54 |
| " CD-1 mice were dosed with 8-64 mg kg(-1) day(-1) MXC or vehicle (sesame oil)." | ( Methoxychlor-induced atresia in the mouse involves Bcl-2 family members, but not gonadotropins or estradiol. Borgeest, C; Flaws, JA; Greenfeld, C; Gupta, R; Hoyer, P; Hruska, KS; Miller, KP, 2004) | 1.77 |
| "Assessing for interactions among chemicals in a mixture involves the comparison of actual mixture responses to those predicted under the assumption of zero interaction (additivity), based on individual chemical dose-response data." | ( A novel flexible approach for evaluating fixed ratio mixtures of full and partial agonists. Carchman, RA; Carney, EW; Carter, WH; Charles, GD; Gennings, C; Gollapudi, BB, 2004) | 0.32 |
| " Dose-response relationships of individual agents were characterized over a 6-log concentration range (1 X 10(-2) to 1 X 10(4) ppb)." | ( Interactive effects of p,p'-dichlorodiphenyldichloroethylene and methoxychlor on hormone synthesis in largemouth bass ovarian cultures. Borgert, CJ; Gross, TS; Guiney, PD; Osimitz, TG; Price, B; Wells, C, 2004) | 0.56 |
| " Visual discrimination performance (simultaneous nonmatch-to-sample with trial-unique stimuli) conducted during dosing demonstrated delayed improvement and poorer performance in the MXC50 group, with some similar effects in the DES group." | ( Endocrine disruption and cognitive function in adolescent female rhesus monkeys. Germann, SL; Golub, MS; Hogrefe, CE, ) | 0.13 |
| " We dosed female controls and ERalpha overexpressors with sesame oil (vehicle control) or MXC (32 and 64 mg/kg/day) for 20 days." | ( Methoxychlor induces atresia of antral follicles in ERalpha-overexpressing mice. Babus, JK; Flaws, JA; Frech, MS; Furth, PA; Gupta, RK; Koos, RD; Tomic, D, 2006) | 1.78 |
| " For the in vivo experiments, adult cycling CD-1 mice were dosed with either vehicle (sesame oil) or MXC for 20 days." | ( Methoxychlor causes mitochondrial dysfunction and oxidative damage in the mouse ovary. Fiskum, G; Flaws, JA; Gupta, RK; Schuh, RA, 2006) | 1.78 |
| " Adult female CD1 mice were dosed with either vehicle (sesame oil) or mxc (16, 32, or 64 mg/kg/day) for 20 consecutive days." | ( Effects of the organochlorine pesticide methoxychlor on dopamine metabolites and transporters in the mouse brain. Fiskum, G; Flaws, JA; Gupta, RK; Richardson, JR; Schuh, RA, 2009) | 0.62 |
| " For in vivo studies, adult cycling CD-1 mice were dosed with MXC or vehicle for 20 days." | ( Methoxychlor inhibits growth of antral follicles by altering cell cycle regulators. Flaws, JA; Gupta, RK; Hernández-Ochoa, I; Meachum, S; Peretz, J; Yao, HH, 2009) | 1.8 |
| " ESR1 OE mice dosed with MXC 64 mg/kg/day had an increased percentage of atretic antral follicles compared to controls." | ( Estrogen receptor alpha overexpressing mouse antral follicles are sensitive to atresia induced by methoxychlor and its metabolites. Craig, ZR; Flaws, JA; Hannon, PR; Paulose, T; Peretz, J, 2012) | 0.6 |
| " In the 20-day treatment, mice were dosed with either the vehicle or MXC at 64 or 96 mg/kg/day, whereas in the 30-day treatment, mice were dosed with vehicle or MXC at 48, 64, or 96 mg/kg/day." | ( Methoxychlor-induced ovarian follicle toxicity in mice: dose and exposure duration-dependent effects. Borgeest, C; Flaws, JA; Paulose, T; Tannenbaum, LV, 2012) | 1.82 |
| " Interestingly, mice dosed with MXC96 had an increased percentage of atretic antral follicles after 30 days, but not after 20 days of treatment compared with vehicle-treated mice." | ( Methoxychlor-induced ovarian follicle toxicity in mice: dose and exposure duration-dependent effects. Borgeest, C; Flaws, JA; Paulose, T; Tannenbaum, LV, 2012) | 1.82 |
| " To test this hypothesis, adult CD-1 female mice were dosed with vehicle control or MXC (64 mg/kg/day) for 20 days." | ( Exposure Duration-Dependent Ovarian Recovery in Methoxychlor-Treated Mice. Flaws, JA; Tannenbaum, LV, 2015) | 0.67 |
| " In order to evaluate the potential of in vitro fish hepatocyte assays to provide information on in vivo metabolite patterns of pesticides in farmed fish, the present study addressed the following questions: Are in vitro and in vivo metabolite patterns comparable? Are species specific differences of metabolite patterns in vivo reflected in vitro? Are metabolite patterns obtained from cryopreserved hepatocytes comparable to those from freshly isolated cells? Rainbow trout and common carp were dosed orally with feed containing the pesticide methoxychlor (MXC) for 14days." | ( Hepatocytes as in vitro test system to investigate metabolite patterns of pesticides in farmed rainbow trout and common carp: Comparison between in vivo and in vitro and across species. Bischof, I; Köster, J; Schlechtriem, C; Segner, H, 2016) | 0.59 |
| " PBK models were developed using a generic approach and in vitro concentration-response data from the MCF-7 proliferation assay and the yeast estrogen screening assay were translated into in vivo dose-response data." | ( Development of a Generic Physiologically Based Kinetic Model to Predict In Vivo Uterotrophic Responses Induced by Estrogenic Chemicals in Rats Based on In Vitro Bioassays. Rietjens, IMCM; van Ravenzwaay, B; Zhang, M, 2020) | 0.56 |
| Class | Description |
|---|---|
| organochlorine insecticide | Any organochlorine pesticide that has been used as an insecticide. |
| [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, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 22.3872 | 0.0040 | 23.8416 | 100.0000 | AID485290 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 50.1187 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 31.6228 | 0.0020 | 14.6779 | 39.8107 | AID1476 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 56.0595 | 0.0072 | 15.7588 | 89.3584 | AID1224835 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 31.6228 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 89.1251 | 0.1000 | 20.8793 | 79.4328 | AID588453 |
| pregnane X receptor | Rattus norvegicus (Norway rat) | Potency | 34.8250 | 0.0251 | 27.9203 | 501.1870 | AID651751 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 27.3707 | 3.1890 | 29.8841 | 59.4836 | AID1224846 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 51.2060 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 35.4813 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 39.8107 | 0.0316 | 37.5844 | 354.8130 | AID504865 |
| TDP1 protein | Homo sapiens (human) | Potency | 22.1429 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 25.5169 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
| AR protein | Homo sapiens (human) | Potency | 34.9757 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID588516; AID743035; AID743042; AID743054; AID743063 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 14.1254 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
| PINK1 | Homo sapiens (human) | Potency | 44.6684 | 2.8184 | 18.8959 | 44.6684 | AID624263 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 39.8107 | 0.0013 | 18.0743 | 39.8107 | AID926; AID938 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 49.0236 | 0.0006 | 57.9133 | 22,387.1992 | AID1259377; AID1259378 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 4.3098 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224839; AID1224893 |
| progesterone receptor | Homo sapiens (human) | Potency | 11.0826 | 0.0004 | 17.9460 | 75.1148 | AID1346784; AID1346795 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 14.0815 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 32.0553 | 0.0002 | 14.3764 | 60.0339 | AID588533; AID720691; AID720692 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 39.4879 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 17.5857 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID1159531; AID588544 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 38.3070 | 0.0015 | 30.6073 | 15,848.9004 | AID1224820; AID1224841; AID1224848; AID1224849; AID1259401; AID1259403 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 19.4399 | 0.3758 | 27.4851 | 61.6524 | AID588526; AID743217; AID743220 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 26.9781 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982; AID720659 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 28.3575 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID588513; AID588514; AID743069; AID743075; AID743078; AID743079; AID743080 |
| G | Vesicular stomatitis virus | Potency | 0.4996 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| polyprotein | Zika virus | Potency | 35.4813 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| Parkin | Homo sapiens (human) | Potency | 44.6684 | 0.8199 | 14.8306 | 44.6684 | AID624263 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 39.8107 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 26.2827 | 0.0010 | 24.5048 | 61.6448 | AID588535; AID743212; AID743215 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 33.4230 | 0.0010 | 19.4141 | 70.9645 | AID588537; AID743191 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 35.7817 | 0.0237 | 23.2282 | 63.5986 | AID588543; AID743222 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 24.3365 | 0.0007 | 23.0674 | 1,258.9301 | AID743085 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 9.6295 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 21.4290 | 0.0016 | 28.0151 | 77.1139 | AID1224843; AID1224895; AID1259385; AID1259395 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 27.3707 | 0.1434 | 27.6121 | 59.8106 | AID1159516 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 17.2698 | 19.7391 | 45.9784 | 64.9432 | AID1159509 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 19.3770 | 0.0578 | 21.1097 | 61.2679 | AID1159526 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 50.1187 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 16.1936 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
| transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 11.2202 | 0.7943 | 21.2757 | 50.1187 | AID624246 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 28.6057 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743066; AID743067 |
| histone deacetylase 9 isoform 3 | Homo sapiens (human) | Potency | 60.7578 | 0.0376 | 17.0823 | 61.1927 | AID1259364 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 34.6998 | 0.0420 | 27.3789 | 61.6448 | AID743210; AID743228 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 1.2589 | 0.0398 | 16.7842 | 39.8107 | AID995 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 100.0000 | 0.1337 | 25.4129 | 89.1251 | AID588795 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 44.7581 | 0.0006 | 27.2152 | 1,122.0200 | AID651741; AID720636; AID743202 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 89.1251 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
| lethal(3)malignant brain tumor-like protein 1 isoform I | Homo sapiens (human) | Potency | 31.6228 | 0.0752 | 15.2253 | 39.8107 | AID485360 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 100.0000 | 0.0316 | 22.3146 | 100.0000 | AID588579 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 8.8006 | 0.0200 | 10.7869 | 31.6228 | AID912 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 68.1713 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
| Interferon beta | Homo sapiens (human) | Potency | 0.4996 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 0.4996 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 23.7915 | 0.0023 | 19.5956 | 74.0614 | AID651631; AID651743; AID720552 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 68.1713 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
| Nuclear receptor ROR-gamma | Homo sapiens (human) | Potency | 34.3832 | 0.0266 | 22.4482 | 66.8242 | AID651802 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1.0000 | 10.4756 | 28.1838 | AID1457 |
| Rap guanine nucleotide exchange factor 4 | Homo sapiens (human) | Potency | 44.6684 | 3.9811 | 46.7448 | 112.2020 | AID720708 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 0.4996 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 0.4996 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Androgen receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 28.1838 | 0.0010 | 1.9794 | 14.1600 | AID255211 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| 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. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID345540 | Decrease in wild type mouse CAR activation expressed in HEK293 cells at 10 uM by mammalian one-hybrid transactivation assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| 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. |
| AID345564 | Effect on mouse CAR H213A mutant expressed in HEK293 cells at 10 uM by mammalian one-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345549 | Activation of mouse CAR F171A mutant expressed in HEK293 cells at 10 uM by mammalian one-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345608 | Enhancement of steroid receptor coactivator 1 binding to mouse CAR F171L mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345658 | Decrease in steroid receptor coactivator 1 binding to mouse CAR Y336A mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345655 | Decrease in nuclear co-repressor receptor binding to mouse CAR Y336A mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345676 | Decrease in nuclear co-repressor receptor binding to mouse CAR L353A mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345538 | Activation of wild type mouse CAR expressed in HEK293 cells at 2 uM by mammalian one-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345631 | Effect on steroid receptor coactivator 1 binding to mouse CAR H213A mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345577 | Effect on mouse CAR L253F mutant expressed in HEK293 cells at 10 uM by mammalian one-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345552 | Decrease in mouse CAR F171L mutant activation expressed in HEK293 cells at 10 uM by mammalian one-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345628 | Decrease in nuclear co-repressor receptor binding to mouse CAR H213A mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345568 | Decrease in mouse CAR S251L mutant activation expressed in HEK293 cells at 10 uM by mammalian one-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345623 | Enhancement of steroid receptor co-activator 1 binding to mouse CAR L212A mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID255211 | Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) | 2005 | Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18 | Impact of induced fit on ligand binding to the androgen receptor: a multidimensional QSAR study to predict endocrine-disrupting effects of environmental chemicals. |
| AID345651 | Effect on steroid receptor coactivator 1 binding to mouse CAR L253F mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345543 | Enhancement of steroid receptor coactivator 1 binding to wild type mouse CAR expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345683 | Cytotoxicity against HEK293 cells | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345615 | Decrease in steroid receptor coactivator 1 binding to mouse CAR N175A mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345634 | Decrease in nuclear co-repressor receptor binding to mouse CAR S251L mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345580 | Activation of mouse CAR Y336A mutant expressed in HEK293 cells at 10 uM by mammalian one-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345599 | Effect on steroid receptor co-activator 1 binding to mouse CAR F171A mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345647 | Effect on nuclear co-repressor receptor binding to mouse CAR L253F mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345542 | Enhancement of steroid receptor coactivator 1 binding to wild type mouse CAR expressed in HEK293 cells at 2 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345641 | Enhancement of steroid receptor coactivator 1 binding to mouse CAR I252L mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345592 | Enhancement of nuclear co-repressor receptor binding to mouse CAR F171A mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345601 | Effect on nuclear co-repressor receptor binding to mouse CAR F171L mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345643 | Enhancement of steroid receptor coactivator 1 binding to mouse CAR I252L mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| 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. |
| AID345666 | Effect on steroid receptor coactivator 1 binding to mouse CAR T350A mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345681 | Effect on steroid receptor coactivator 1 binding to mouse CAR L353A mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345611 | Decrease in nuclear co-repressor receptor binding to mouse CAR N175A mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345619 | Decrease in nuclear co-repressor receptor binding to mouse CAR L212A mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345541 | Enhancement of steroid receptor coactivator 1 binding to wild type mouse CAR expressed in HEK293 cells at 1 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345584 | Decrease in mouse CAR T350A mutant activation expressed in HEK293 cells at 10 uM by mammalian one-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345672 | Effect on steroid receptor coactivator 1 binding to mouse CAR T350M mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345636 | Effect on steroid receptor coactivator 1 binding to mouse CAR S251L mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345669 | Decrease in nuclear co-repressor receptor binding to mouse CAR T350M mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345589 | Effect on mouse CAR T350M mutant expressed in HEK293 cells at 2 uM by mammalian one-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345572 | Decrease in mouse CAR I252L mutant activation expressed in HEK293 cells at 10 uM by mammalian one-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345560 | Activation of mouse CAR L212A mutant expressed in HEK293 cells at 10 uM by mammalian one-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID345545 | Increase in nuclear co-repressor receptor binding to wild type mouse CAR expressed in HEK293 cells at 2 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID679012 | TP_TRANSPORTER: drug resistance in MRP1-expressing NIH/3T3 cells | 2003 | Toxicology letters, Apr-30, Volume: 142, Issue:1-2 | The multidrug resistance-associated protein 1 transports methoxychlor and protects the seminiferous epithelium from injury. |
| AID345663 | Decrease in nuclear co-repressor receptor binding to mouse CAR T350A mutant expressed in HEK293 cells at 10 uM by yeast two-hybrid assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | Ligand specificity of constitutive androstane receptor as probed by induced-fit docking and mutagenesis. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| 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 | 133 (28.60) | 18.7374 |
| 1990's | 57 (12.26) | 18.2507 |
| 2000's | 159 (34.19) | 29.6817 |
| 2010's | 99 (21.29) | 24.3611 |
| 2020's | 17 (3.66) | 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 (41.90) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (0.19%) | 5.53% |
| Reviews | 27 (5.09%) | 6.00% |
| Case Studies | 4 (0.75%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 498 (93.96%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||