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

General Information of Drug (ID: DMUB0EJ)

• Drug Name: Pyrazolo[1,5-a]pyrimidine 3G Drug Info
• Synonyms: KDR/Flk-1 kinase inhibitor IV; pyrazolo[1,5-a]pyrimidine 3g

Indication

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

• Cross-matching ID:
  PubChem CID: 5329468
  ChEBI ID: CHEBI:93078
  CAS Number: CAS 216661-57-3
  TTD Drug ID: DMUB0EJ

Molecule-Related Drug Atlas

Drug(s) Targeting Vascular endothelial growth factor receptor 2 (KDR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[2]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[3]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[4]
Sunitinib	DMCBJSR	Acute undifferentiated leukemia		Approved	[5]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[6]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[7]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[8]
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[9]
Cabozantinib	DMIYDT4	Medullary thyroid gland carcinoma		Approved	[10]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Inhibitor	[1]

References

• [1] Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharm... Bioorg Med Chem Lett. 2002 Dec 16;12(24):3537-41.
• [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] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [5] 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
• [6] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [7] 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.
• [8] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [9] Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.
• [10] Clinical pipeline report, company report or official report of Exelixis (2011).
• [11] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services