General Information of Drug (ID: DMPAWBN)

Drug Name
GSK525762 Drug Info
Synonyms GSK-525762
Indication
Disease Entry ICD 11 Status REF
Haematological malignancy 2B33.Y Phase 1 [1]
Solid tumour/cancer 2A00-2F9Z Phase 1 [2]
Cross-matching ID
PubChem CID
46943432
ChEBI ID
CHEMBL1232461
CAS Number
CAS 1260907-17-2
TTD Drug ID
DMPAWBN

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Patented Agent(s)
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
CPI-0610 DMPXOYJ Myelofibrosis 2A20.2 Phase 3 [3]
OTX-015 DMI8RG1 Acute myeloid leukaemia 2A60 Phase 1/2 [3]
PLX2853 DMX168L Acute myeloid leukaemia 2A60 Phase 1/2 [1]
RVX-208 DM1LO8K Alzheimer disease 8A20 Phase 1/2 [3]
INCB57643 DMBGU7V Advanced malignancy 2A00-2F9Z Phase 1/2 [1]
ABBV-744 DMTEA9C Acute myeloid leukaemia 2A60 Phase 1 [1]
(+)-JQ1 DM1CZSJ Testicular cancer 2C80 Phase 1 [6]
TEN010 DM4UOY5 Advanced solid tumour 2A00-2F9Z Phase 1 [3]
AZD5153 DMW4GM2 Solid tumour/cancer 2A00-2F9Z Phase 1 [1]
PMID26924192-Compound-104 DM346EU N. A. N. A. Patented [7]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
CPI-0610 DMPXOYJ Myelofibrosis 2A20.2 Phase 3 [1]
ZEN-3694 DM6VQTF Prostate cancer 2C82.0 Phase 2 [8]
OTX-015 DMI8RG1 Acute myeloid leukaemia 2A60 Phase 1/2 [1]
BMS-986158 DM6LDI4 Solid tumour/cancer 2A00-2F9Z Phase 1/2 [1]
INCB054329 DM7TZL0 Refractory hematologic malignancy 2A85.5 Phase 1/2 [9]
INCB057643 DMG65CV Solid tumour/cancer 2A00-2F9Z Phase 1/2 [10]
ODM-207 DMOKVJD Solid tumour/cancer 2A00-2F9Z Phase 1/2 [11]
(+)-JQ1 DM1CZSJ Testicular cancer 2C80 Phase 1 [12]
PLX51107 DMXLHVW Haematological malignancy 2B33.Y Phase 1 [1]
BI 894999 DM7W5N2 Solid tumour/cancer 2A00-2F9Z Phase 1 [1]
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Drug(s) Affected By Protein-lysine 6-oxidase (LOX)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [13]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [14]
Quercetin DM3NC4M Obesity 5B81 Approved [15]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [16]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [17]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [18]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [19]
Ethanol DMDRQZU Chronic pain MG30 Approved [20]
Ampicillin DMHWE7P Acute epiglottitis Approved [15]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [21]
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Drug(s) Affected By Carbonic anhydrase 9 (CA9)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetazolamide DM1AF5U Absence epilepsy Approved [22]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [14]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [23]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [24]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [25]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [18]
Ampicillin DMHWE7P Acute epiglottitis Approved [15]
Temozolomide DMKECZD Adenocarcinoma 2D40 Approved [26]
Bortezomib DMNO38U Leukemia Approved [27]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [28]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Quercetin DM3NC4M Obesity 5B81 Approved [15]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [29]
Acetic Acid, Glacial DM4SJ5Y infection in the ear canal AA0Y Approved [30]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [31]
Leflunomide DMR8ONJ Arthritis FA20 Approved [32]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [18]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [33]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [34]
Ethanol DMDRQZU Chronic pain MG30 Approved [35]
Motexafin gadolinium DMEJKRF Brain cancer 2A00 Approved [30]
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Drug(s) Affected By Protein GREB1 (GREB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [36]
Spironolactone DM2AQ5N Chronic heart failure BD1Z Approved [37]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [38]
Testosterone DM7HUNW Hot flushes GA30 Approved [39]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [40]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [41]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [19]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [37]
Nandrolone DMFWKG1 Osteoporosis FB83.0 Approved [42]
Mestranol DMG3F94 Contraception QA21 Approved [37]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [43]
Methotrexate DM2TEOL Anterior urethra cancer Approved [44]
Quercetin DM3NC4M Obesity 5B81 Approved [45]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [29]
Panobinostat DM58WKG Chronic graft versus host disease Approved [46]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [47]
Leflunomide DMR8ONJ Arthritis FA20 Approved [32]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [18]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [19]
Ketorolac DMI4EL5 Postoperative inflammation 1A00-CA43.1 Approved [47]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Bromodomain and extraterminal domain protein (BET) TTE4BSY NOUNIPROTAC Inhibitor [1]
Bromodomain-containing protein 4 (BRD4) TTRA6BO BRD4_HUMAN Modulator [3]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) OT25JBA3 F263_HUMAN Gene/Protein Processing [4]
Carbonic anhydrase 9 (CA9) OTNA51XT CAH9_HUMAN Gene/Protein Processing [4]
Endothelial PAS domain-containing protein 1 (EPAS1) OTRE3O8U EPAS1_HUMAN Gene/Protein Processing [4]
Protein GREB1 (GREB1) OTU6ZA26 GREB1_HUMAN Gene/Protein Processing [5]
Protein-lysine 6-oxidase (LOX) OT1C2HIU LYOX_HUMAN Gene/Protein Processing [4]
Vascular endothelial growth factor A, long form OTIM9MZ3 VEGFA_HUMAN Gene/Protein Processing [4]

References

1 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2 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: 7033).
3 Targeting bromodomains: epigenetic readers of lysine acetylation.Nat Rev Drug Discov.2014 May;13(5):337-56.
4 The BET inhibitor JQ1 selectively impairs tumour response to hypoxia and downregulates CA9 and angiogenesis in triple negative breast cancer. Oncogene. 2017 Jan 5;36(1):122-132. doi: 10.1038/onc.2016.184. Epub 2016 Jun 13.
5 An epigenomic approach to therapy for tamoxifen-resistant breast cancer. Cell Res. 2014 Jul;24(7):809-19. doi: 10.1038/cr.2014.71. Epub 2014 May 30.
6 Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73.
7 BET inhibitors in cancer therapeutics: a patent review.Expert Opin Ther Pat. 2016;26(4):505-22.
8 Clinical pipeline report, company report or official report of Zenith Epigenetics.
9 The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies. Clin Cancer Res. 2019 Jan 1;25(1):300-311.
10 Development of 2 Bromodomain and Extraterminal Inhibitors With Distinct Pharmacokinetic and Pharmacodynamic Profiles for the Treatment of Advanced Malignancies. Clin Cancer Res. 2020 Mar 15;26(6):1247-1257.
11 First-in-human Phase 1 open label study of the BET inhibitor ODM-207 in patients with selected solid tumours. Br J Cancer. 2020 Dec;123(12):1730-1736.
12 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
13 Unique signatures of stress-induced senescent human astrocytes. Exp Neurol. 2020 Dec;334:113466. doi: 10.1016/j.expneurol.2020.113466. Epub 2020 Sep 17.
14 NO-sulindac inhibits the hypoxia response of PC-3 prostate cancer cells via the Akt signalling pathway. Int J Cancer. 2009 Jan 1;124(1):223-32. doi: 10.1002/ijc.23934.
15 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.
16 Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
17 Large-scale in silico and microarray-based identification of direct 1,25-dihydroxyvitamin D3 target genes. Mol Endocrinol. 2005 Nov;19(11):2685-95.
18 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
19 Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
20 Chronic ethanol exposure increases goosecoid (GSC) expression in human embryonic carcinoma cell differentiation. J Appl Toxicol. 2014 Jan;34(1):66-75.
21 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
22 Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. J Med Chem. 2011 Oct 13;54(19):6905-18.
23 Synergistic effects of arsenic trioxide and silibinin on apoptosis and invasion in human glioblastoma U87MG cell line. Neurochem Res. 2012 Feb;37(2):370-80. doi: 10.1007/s11064-011-0620-1. Epub 2011 Oct 4.
24 Keratinocyte-derived IL-36gama plays a role in hydroquinone-induced chemical leukoderma through inhibition of melanogenesis in human epidermal melanocytes. Arch Toxicol. 2019 Aug;93(8):2307-2320.
25 Identification of vitamin D3 target genes in human breast cancer tissue. J Steroid Biochem Mol Biol. 2016 Nov;164:90-97.
26 Temozolomide induces activation of Wnt/-catenin signaling in glioma cells via PI3K/Akt pathway: implications in glioma therapy. Cell Biol Toxicol. 2020 Jun;36(3):273-278. doi: 10.1007/s10565-019-09502-7. Epub 2019 Nov 22.
27 A phase II trial with pharmacodynamic endpoints of the proteasome inhibitor bortezomib in patients with metastatic colorectal cancer. Clin Cancer Res. 2005 Aug 1;11(15):5526-33. doi: 10.1158/1078-0432.CCR-05-0081.
28 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
29 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.
30 Motexafin gadolinium and zinc induce oxidative stress responses and apoptosis in B-cell lymphoma lines. Cancer Res. 2005 Dec 15;65(24):11676-88.
31 Expression profile analysis of colon cancer cells in response to sulindac or aspirin. Biochem Biophys Res Commun. 2002 Mar 29;292(2):498-512.
32 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
33 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
34 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.
35 Gene expression signatures after ethanol exposure in differentiating embryoid bodies. Toxicol In Vitro. 2018 Feb;46:66-76.
36 Arsenite and cadmium promote the development of mammary tumors. Carcinogenesis. 2020 Jul 14;41(7):1005-1014. doi: 10.1093/carcin/bgz176.
37 A Gene Expression Biomarker Identifies Chemical Modulators of Estrogen Receptor in an MCF-7 Microarray Compendium. Chem Res Toxicol. 2021 Feb 15;34(2):313-329. doi: 10.1021/acs.chemrestox.0c00243. Epub 2021 Jan 6.
38 Arsenic induces functional re-expression of estrogen receptor by demethylation of DNA in estrogen receptor-negative human breast cancer. PLoS One. 2012;7(4):e35957. doi: 10.1371/journal.pone.0035957. Epub 2012 Apr 27.
39 The exosome-like vesicles derived from androgen exposed-prostate stromal cells promote epithelial cells proliferation and epithelial-mesenchymal transition. Toxicol Appl Pharmacol. 2021 Jan 15;411:115384. doi: 10.1016/j.taap.2020.115384. Epub 2020 Dec 25.
40 Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
41 Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
42 Evaluation of an imaging-based in vitro screening platform for estrogenic activity with OECD reference chemicals. Toxicol In Vitro. 2022 Jun;81:105348. doi: 10.1016/j.tiv.2022.105348. Epub 2022 Mar 18.
43 MS4A3-HSP27 target pathway reveals potential for haematopoietic disorder treatment in alimentary toxic aleukia. Cell Biol Toxicol. 2023 Feb;39(1):201-216. doi: 10.1007/s10565-021-09639-4. Epub 2021 Sep 28.
44 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
45 Flavonoids-induced accumulation of hypoxia-inducible factor (HIF)-1alpha/2alpha is mediated through chelation of iron. J Cell Biochem. 2008 Apr 15;103(6):1989-98. doi: 10.1002/jcb.21588.
46 A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
47 Ibuprofen-mediated reduction of hypoxia-inducible factors HIF-1alpha and HIF-2alpha in prostate cancer cells. Clin Cancer Res. 2003 Aug 1;9(8):3150-7.