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

General Information of Drug (ID: DMQXJA1)

• Drug Name: 3-Benzimidazol-2-ylhydroquinolin-2-one Drug Info

Indication

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

• Cross-matching ID:
  PubChem CID: 5329370
  TTD Drug ID: DMQXJA1

Molecule-Related Drug Atlas

Drug(s) Targeting Fibroblast growth factor receptor 1 (FGFR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[2]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[3]
Pemigatinib	DM819JF	Cholangiocarcinoma	2C12.10	Approved	[4]
Infigratinib	DMNKBEC	Cholangiocarcinoma	2C12.10	Approved	[5]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[6]
Sulfatinib	DMPOTM4	Neuroendocrine cancer	2B72.1	Phase 3	[7]
ARQ-087	DM02BVQ	Intrahepatic cholangiocarcinoma	2C12.10	Phase 3	[8]
AZD4547	DM3827C	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[9]
Debio 1347	DMZW50O	Solid tumour/cancer	2A00-2F9Z	Phase 2	[10]
AM-001	DMGVQI8	Actinic keratosis	EK90.0	Phase 2	[11]

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	[12]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[13]
Becaplermin	DM1R5X4	Diabetic complication	5A2Y	Approved	[14]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[6]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[15]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[16]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[17]
SNN-0031	DM2X3BR	Brain injury	NA07.Z	Phase 1/2	[18]
TAK-593	DMNFZOT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[19]
Pyridine derivative 18	DMBZMYT	N. A.	N. A.	Patented	[20]

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	[12]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[2]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[21]
Sunitinib	DMCBJSR	Acute undifferentiated leukemia		Approved	[22]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[23]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[24]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[25]
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[26]
Cabozantinib	DMIYDT4	Medullary thyroid gland carcinoma		Approved	[27]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[28]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Fibroblast growth factor receptor 1 (FGFR1)	TTRLW2X	FGFR1_HUMAN	Inhibitor	[1]
Platelet-derived growth factor receptor beta (PDGFRB)	TTI7421	PGFRB_HUMAN	Inhibitor	[1]
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Inhibitor	[1]

References

• [1] Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor... J Med Chem. 2009 Jan 22;52(2):278-92.
• [2] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [3] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [5] Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets. J Bone Miner Res. 2013 Apr;28(4):899-911.
• [6] 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.
• [7] Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
• [8] 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: 1808).
• [9] AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 2012 Apr 15;72(8):2045-56.
• [10] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [11] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029917)
• [12] 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.
• [13] 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.
• [14] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [15] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [16] National Cancer Institute Drug Dictionary (drug id 452042).
• [17] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [18] Company report (Neuronova)
• [19] 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.
• [20] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
• [21] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [22] 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
• [23] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [24] 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.
• [25] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [26] 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.
• [27] Clinical pipeline report, company report or official report of Exelixis (2011).
• [28] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services