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

General Information of Drug (ID: DMK1IWD)

• Drug Name: 4-(4-aminophenyl)-1H-indazol-3yl-amine Drug Info
• Synonyms: 4-(4-aminophenyl)-1H-indazol-3-amine; 819058-89-4; CHEMBL222778; Flt3 Inhibitor IV; 4-(4-aminophenyl)-1H-indazol-3yl-amine; SCHEMBL421242; DTXSID90583110; 3-amino-4-(4-aminophenyl)indazole; BDBM50207472; ZINC35324130; AKOS025401748; QC-1103; AC-25079; 1H-Indazol-3-amine,4-(4-aminophenyl)-

Indication

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

• Cross-matching ID:
  PubChem CID: 16125106
  CAS Number: CAS 819058-89-4
  TTD Drug ID: DMK1IWD

Molecule-Related Drug Atlas

Drug(s) Targeting Tyrosine-protein kinase Kit (KIT)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[2]
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[3]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[4]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[5]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[5]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[6]
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[7]
Ripretinib	DM958QB	Gastrointestinal stromal tumour	2B5B	Approved	[8]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[9]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[10]

Drug(s) Targeting Fms-like tyrosine kinase 3 (FLT-3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[11]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[5]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[12]
Midostaurin	DMI6E0R	Acute myeloid leukaemia	2A60	Approved	[2]
Gilteritinib	DMTI0ZO	Acute myeloid leukaemia	2A60	Approved	[13]
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[7]
Pacritinib	DM1T6ZN	Myelofibrosis	2A20.2	Approved	[11]
Quizartinib	DM8Y4JS	Acute myeloid leukaemia	2A60	Approved	[14]
Lestaurtinib	DMQ2AIJ	Acute myeloid leukaemia	2A60	Approved (orphan drug)	[15]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[9]

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	[3]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[16]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[5]
Sunitinib	DMCBJSR	Acute undifferentiated leukemia		Approved	[17]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[18]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[2]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[6]
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[19]
Cabozantinib	DMIYDT4	Medullary thyroid gland carcinoma		Approved	[20]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[21]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Fms-like tyrosine kinase 3 (FLT-3)	TTGJCWZ	FLT3_HUMAN	Inhibitor	[1]
Tyrosine-protein kinase Kit (KIT)	TTX41N9	KIT_HUMAN	Inhibitor	[1]
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Inhibitor	[1]

References

• [1] Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted ... J Med Chem. 2007 Apr 5;50(7):1584-97.
• [2] 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.
• [3] 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.
• [4] New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven a... J Med Chem. 2000 Jun 15;43(12):2310-23.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [6] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [7] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [8] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [9] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [10] National Cancer Institute Drug Dictionary (drug id 452042).
• [11] 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: 1807).
• [12] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [13] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [14] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [15] Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with ... Blood. 2008 Jun 15;111(12):5663-71.
• [16] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [17] 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
• [18] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [19] 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.
• [20] Clinical pipeline report, company report or official report of Exelixis (2011).
• [21] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services