Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMNBLQ8)

• Drug Name: 4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline Drug Info
• Synonyms: CHEMBL98798; 4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 44331231
  TTD Drug ID: DMNBLQ8

Molecule-Related Drug Atlas

Drug(s) Targeting Platelet-derived growth factor receptor beta (PDGFRB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[2]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[3]
Becaplermin	DM1R5X4	Diabetic complication	5A2Y	Approved	[4]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[5]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[6]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[7]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[8]
SNN-0031	DM2X3BR	Brain injury	NA07.Z	Phase 1/2	[9]
TAK-593	DMNFZOT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
Pyridine derivative 18	DMBZMYT	N. A.	N. A.	Patented	[11]

Drug(s) Targeting Epidermal growth factor receptor (EGFR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[12]
Lapatinib	DM3BH1Y	Breast cancer	2C60-2C65	Approved	[13]
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[14]
Erlotinib	DMCMBHA	Adrenal gland neoplasm		Approved	[15]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[16]
Dacomitinib	DMOH8VY	Non-small-cell lung cancer	2C25.Y	Approved	[17]
BIBW 2992	DMTKD7Q	Non-small-cell lung cancer	2C25.Y	Approved	[18]
SKI-758	DMQ8E9R	Ischemia	8B10-8B11	Approved	[19]
Epidermal growth factor	DMVONE6	Vulnerary	ND56.Z	Approved	[17]
Merimepodib	DM0HS92	Breast cancer	2C60-2C65	Approved	[20]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Epidermal growth factor receptor (EGFR)	TTGKNB4	EGFR_HUMAN	Inhibitor	[1]
Platelet-derived growth factor receptor beta (PDGFRB)	TTI7421	PGFRB_HUMAN	Inhibitor	[1]

References

• [1] A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation, Bioorg. Med. Chem. Lett. 7(23):2935-2940 (1997).
• [2] Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling.Mol Cancer Ther.2008 Oct;7(10):3129-40.
• [3] Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel... J Med Chem. 2003 Mar 27;46(7):1116-9.
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [5] E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405.
• [6] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [7] National Cancer Institute Drug Dictionary (drug id 452042).
• [8] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [9] Company report (Neuronova)
• [10] Biochemical characterization of TAK-593, a novel VEGFR/PDGFR inhibitor with a two-step slow binding mechanism. Biochemistry. 2011 Feb 8;50(5):738-51.
• [11] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
• [12] Nasopharyngeal carcinoma: Current treatment options and future directions. J Nasopharyng Carcinoma, 2014, 1(16): e16.
• [13] Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7.
• [14] Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
• [15] Quantitative prediction of fold resistance for inhibitors of EGFR. Biochemistry. 2009 Sep 8;48(35):8435-48.
• [16] A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
• [17] 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. (Target id: 1797).
• [18] Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
• [19] Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
• [20] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).