General Information of Drug (ID: DMGKEO5)

Drug Name
GW0742X Drug Info
Synonyms GW0742; GW-0742X
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
9934458
ChEBI ID
CHEBI:79991
CAS Number
CAS 317318-84-6
TTD Drug ID
DMGKEO5

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Patented Agent(s)
Discontinued Drug(s)
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
GFT-505 DM7ZOAE Non-alcoholic steatohepatitis DB92.1 Phase 3 [5]
MBX-8025 DMNTCV4 Obesity 5B81 Phase 2/3 [6]
T3D-959 DMR3245 Alzheimer disease 8A20 Phase 2 [7]
T3D-959 DMR3245 Alzheimer disease 8A20 Phase 2 [8]
KD3010 DMNFDYE Metabolic disorder 5C50-5D2Z Phase 1 [9]
SAR351034 DM15PG9 Dyslipidemia 5C80-5C81 Phase 1 [10]
CER-002 DMLBKZV Dyslipidemia 5C80-5C81 Phase 1 [11]
PMID25416646-Compound-Figure5-C DM17FKL N. A. N. A. Patented [12]
GW-501516 DMPL2KM Type-1 diabetes 5A10 Discontinued in Phase 4 [13]
Sodelglitazar DMJ816F Hyperlipidaemia 5C80 Discontinued in Phase 2 [14]
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Drug(s) Affected By Nitric oxide synthase 3 (NOS3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [15]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [16]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [17]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [18]
Methotrexate DM2TEOL Anterior urethra cancer Approved [19]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [20]
Quercetin DM3NC4M Obesity 5B81 Approved [21]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [22]
Fructose DM43AN2 Vomiting MD90 Approved [23]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [24]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Capivasertib DM9SKW8 Breast cancer 2C60-2C65 Approved [25]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [26]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [27]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [28]
Gefitinib DM15F0X Colon adenocarcinoma Approved [29]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [30]
Imiquimod DM1TMA3 Alopecia areata ED70.2 Approved [31]
Selenium DM25CGV N. A. N. A. Approved [32]
Methimazole DM25FL8 Hyperthyroidism 5A02 Approved [33]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [34]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Perilipin-2 (PLIN2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [35]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [36]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [37]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [38]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [39]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [40]
Leflunomide DMR8ONJ Arthritis FA20 Approved [41]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [42]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [43]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [44]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Aspirin DM672AH Acute coronary syndrome BA41 Approved [17]
Quercetin DM3NC4M Obesity 5B81 Approved [45]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [46]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [47]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [40]
Leflunomide DMR8ONJ Arthritis FA20 Approved [41]
Clodronate DM9Y6X7 Hypercalcaemia 5B91.0 Approved [40]
Cidofovir DMA13GD Cytomegalovirus infection 1D82 Approved [40]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [48]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [43]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Peroxisome proliferator-activated receptor delta (PPARD) TT2JWF6 PPARD_HUMAN Agonist [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Angiopoietin-related protein 4 (ANGPTL4) OTQL5SPX ANGL4_HUMAN Gene/Protein Processing [3]
Nitric oxide synthase 3 (NOS3) OTLDT7NR NOS3_HUMAN Post-Translational Modifications [4]
Perilipin-2 (PLIN2) OTRXJ9UN PLIN2_HUMAN Gene/Protein Processing [3]
RAC-alpha serine/threonine-protein kinase (AKT1) OT8H2YY7 AKT1_HUMAN Post-Translational Modifications [4]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2686).
2 Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity. Bioorg Med Chem Lett. 2003 May 5;13(9):1517-21.
3 Regulation of peroxisome proliferator-activated receptor-beta/delta by the APC/beta-CATENIN pathway and nonsteroidal antiinflammatory drugs. Mol Carcinog. 2009 Oct;48(10):942-52. doi: 10.1002/mc.20546.
4 Endothelium-dependent vasodilator effects of peroxisome proliferator-activated receptor beta agonists via the phosphatidyl-inositol-3 kinase-Akt pathway. J Pharmacol Exp Ther. 2010 Feb;332(2):554-61. doi: 10.1124/jpet.109.159806. Epub 2009 Nov 11.
5 Dual peroxisome proliferator-activated receptor / agonist GFT505 improves hepatic and peripheral insulin sensitivity in abdominally obese subjects.Diabetes Care.2013 Oct;36(10):2923-30.
6 ClinicalTrials.gov (NCT00701883) Safety and Benefit of MBX-8025 With and Without Commonly Used Statins in Moderately Overweight Patients With High Cholesterol. U. S. National Institute of Health. 2008.
7 Phrma report (2013 Alzheimers disease)
8 T3D-959: A Multi-Faceted Disease Remedial Drug Candidate for the Treatment of Alzheimer's Disease. J Alzheimers Dis. 2016;51(1):123-38.
9 Kalypsys nearing completion of phase Ia study of KD3010 for metabolic disorders. Kalypsys. 2007.
10 Addressing Unmet Medical Needs in Type 2 Diabetes: A Narrative Review of Drugs under Development. Curr Diabetes Rev. 2015 March; 11(1): 17-31.
11 Fibrates, glitazones, and peroxisome proliferator-activated receptors. Arterioscler Thromb Vasc Biol. 2010 May; 30(5): 894-899.
12 PPAR ligands and their therapeutic applications: a patent review (2008 - 2014).Expert Opin Ther Pat. 2015 Feb;25(2):175-91.
13 Lipid effects of peroxisome proliferator-activated receptor- agonist GW501516 in subjects with low high-density lipoprotein cholesterol: characteristics of metabolic syndrome.Arterioscler Thromb Vasc Biol.2012 Sep;32(9):2289-94.
14 Docking and molecular dynamics simulations of peroxisome proliferator activated receptors interacting with pan agonist sodelglitazar. Protein Pept Lett. 2011 Oct;18(10):1021-7.
15 Protective effects of S-carvedilol on doxorubicin-induced damages to human umbilical vein endothelial cells and rats. J Appl Toxicol. 2019 Aug;39(8):1233-1244. doi: 10.1002/jat.3809. Epub 2019 May 7.
16 Oxidative stress in kidney transplant patients with calcineurin inhibitor-induced hypertension: effect of ramipril. J Cardiovasc Pharmacol. 2002 Oct;40(4):625-31.
17 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
18 Hydrogen peroxide decreases endothelial nitric oxide synthase promoter activity through the inhibition of Sp1 activity. DNA Cell Biol. 2009 Mar;28(3):119-29.
19 Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
20 Simvastatin inhibits cigarette smoking-induced emphysema and pulmonary hypertension in rat lungs. Am J Respir Crit Care Med. 2005 Oct 15;172(8):987-93. doi: 10.1164/rccm.200501-041OC. Epub 2005 Jul 7.
21 A blend of polyphenolic compounds explains the stimulatory effect of red wine on human endothelial NO synthase. Nitric Oxide. 2005 Mar;12(2):97-104.
22 The thiazolidinedione drug troglitazone up-regulates nitric oxide synthase expression in vascular endothelial cells. J Diabetes Complications. 2006 Sep-Oct;20(5):336-42.
23 Fructose induces the inflammatory molecule ICAM-1 in endothelial cells. J Am Soc Nephrol. 2008 Sep;19(9):1712-20.
24 Upregulation of nitric oxide production in vascular endothelial cells by all-trans retinoic acid through the phosphoinositide 3-kinase/Akt pathway. Circulation. 2005 Aug 2;112(5):727-36. doi: 10.1161/CIRCULATIONAHA.104.500959. Epub 2005 Jul 25.
25 Inhibition of cholesterol metabolism underlies synergy between mTOR pathway inhibition and chloroquine in bladder cancer cells. Oncogene. 2016 Aug 25;35(34):4518-28. doi: 10.1038/onc.2015.511. Epub 2016 Feb 8.
26 Nicotine-induced survival signaling in lung cancer cells is dependent on their p53 status while its down-regulation by curcumin is independent. Mol Cancer. 2010 Aug 20;9:220.
27 Role of miRNA in the regulation of cannabidiol-mediated apoptosis in neuroblastoma cells. Oncotarget. 2019 Jan 1;10(1):45-59. doi: 10.18632/oncotarget.26534. eCollection 2019 Jan 1.
28 -Carotene Induces Apoptosis in Human Esophageal Squamous Cell Carcinoma Cell Lines via the Cav-1/AKT/NF-B Signaling Pathway. J Biochem Mol Toxicol. 2016 Mar;30(3):148-57. doi: 10.1002/jbt.21773. Epub 2016 Jan 6.
29 Dihydromyricetin suppresses tumor growth via downregulation of the EGFR/Akt/survivin signaling pathway. J Biochem Mol Toxicol. 2023 Jun;37(6):e23328. doi: 10.1002/jbt.23328. Epub 2023 Feb 19.
30 Oxidative stress induces parallel autophagy and mitochondria dysfunction in human glioma U251 cells. Toxicol Sci. 2009 Aug;110(2):376-88. doi: 10.1093/toxsci/kfp101. Epub 2009 May 18.
31 Effect of toll-like receptor 7 and 9 targeted therapy to prevent the development of hepatocellular carcinoma. Liver Int. 2015 Mar;35(3):1063-76. doi: 10.1111/liv.12626. Epub 2014 Jul 30.
32 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
33 Low-expressional IGF1 mediated methimazole-induced liver developmental toxicity in fetal mice. Toxicology. 2018 Sep 1;408:70-79. doi: 10.1016/j.tox.2018.07.004. Epub 2018 Jul 7.
34 Ribavirin augments doxorubicin's efficacy in human hepatocellular carcinoma through inhibiting doxorubicin-induced eIF4E activation. J Biochem Mol Toxicol. 2018 Jan;32(1). doi: 10.1002/jbt.22007. Epub 2017 Nov 7.
35 Gene expression profiling of rheumatoid arthritis synovial cells treated with antirheumatic drugs. J Biomol Screen. 2007 Apr;12(3):328-40. doi: 10.1177/1087057107299261. Epub 2007 Mar 22.
36 Transcriptomic analysis of untreated and drug-treated differentiated HepaRG cells over a 2-week period. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):27-35.
37 Retinoic acid-induced downmodulation of telomerase activity in human cancer cells. Exp Mol Pathol. 2005 Oct;79(2):108-17.
38 Temporal changes in gene expression in the skin of patients treated with isotretinoin provide insight into its mechanism of action. Dermatoendocrinol. 2009 May;1(3):177-87.
39 Essential role of cell cycle regulatory genes p21 and p27 expression in inhibition of breast cancer cells by arsenic trioxide. Med Oncol. 2011 Dec;28(4):1225-54.
40 Transcriptomics hit the target: monitoring of ligand-activated and stress response pathways for chemical testing. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):7-18.
41 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
42 Detection of the mechanism of immunotoxicity of cyclosporine A in murine in vitro and in vivo models. Arch Toxicol. 2015 Dec;89(12):2325-37. doi: 10.1007/s00204-014-1365-9. Epub 2014 Sep 17.
43 Integrated 'omics analysis reveals new drug-induced mitochondrial perturbations in human hepatocytes. Toxicol Lett. 2018 Jun 1;289:1-13.
44 Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
45 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
46 Effects of ciglitazone and troglitazone on the proliferation of human stomach cancer cells. World J Gastroenterol. 2009 Jan 21;15(3):310-20.
47 Systems analysis of transcriptome and proteome in retinoic acid/arsenic trioxide-induced cell differentiation/apoptosis of promyelocytic leukemia. Proc Natl Acad Sci U S A. 2005 May 24;102(21):7653-8.
48 Integrative "-Omics" analysis in primary human hepatocytes unravels persistent mechanisms of cyclosporine A-induced cholestasis. Chem Res Toxicol. 2016 Dec 19;29(12):2164-2174.