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

General Information of Drug (ID: DM21WBH)

• Drug Name: MK-2461 Drug Info
• Synonyms: MK 2461

Indication

Disease Entry	ICD 11	Status	REF
Alzheimer disease	8A20	Phase 1/2	[1]

• Cross-matching ID:
  PubChem CID: 44137946
  CAS Number: CAS 917879-39-1
  TTD Drug ID: DM21WBH

Molecule-Related Drug Atlas

Drug(s) Targeting Macrophage-stimulating protein receptor (RON)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Anti-RON receptor mabs	DMXACM2	Solid tumour/cancer	2A00-2F9Z	Investigative	[2]
ABC-7	DM2AIE9	Solid tumour/cancer	2A00-2F9Z	Investigative	[2]

Drug(s) Targeting Vascular endothelial growth factor receptor 3 (FLT-4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[3]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[4]
Sulfatinib	DMPOTM4	Neuroendocrine cancer	2B72.1	Phase 3	[5]
Fruquintinib	DMHOSCQ	Solid tumour/cancer	2A00-2F9Z	Phase 3	[6]
PI-88	DMGZPX6	Hepatocellular carcinoma	2C12.02	Phase 3	[7]
Taberminogene vadenovec	DMW5PHL	Vascular restinosis	BE2Z	Phase 3	[8]
ABT-869	DMREDYP	Solid tumour/cancer	2A00-2F9Z	Phase 3	[9]
MGCD516	DM752PU	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[10]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]
VATALANIB	DMY0UEQ	Solid tumour/cancer	2A00-2F9Z	Phase 2	[12]

Drug(s) Targeting Proto-oncogene c-Met (MET)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Crizotinib	DM4F29C	Non-small-cell lung cancer	2C25.Y	Approved	[13]
Cabozantinib	DMIYDT4	Thyroid cancer	2D10	Approved	[14]
Capmatinib	DMYCXKL	Non-small-cell lung cancer	2C25.Y	Approved	[15]
Tepotinib	DMUQ0E8	Non-small cell lung cancer	2C25	Approved	[16]
Amivantamab	DMZ7AMY	Non-small-cell lung cancer	2C25.Y	Phase 3	[17]
RG3638	DMTQJE0	Gastric adenocarcinoma	2B72	Phase 3	[18]
Savolitinib	DMALFKX	Renal cell carcinoma	2C90	Phase 3	[19]
Beperminogene perplasmid	DM6RWBN	Critical limb ischemia	BD4Y	Phase 3	[20]
Tivantinib	DMNVP8Q	Hepatocellular carcinoma	2C12.02	Phase 3	[21]
MGCD516	DM752PU	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[18]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[22]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[23]
Pemigatinib	DM819JF	Cholangiocarcinoma	2C12.10	Approved	[24]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[4]
Sulfatinib	DMPOTM4	Neuroendocrine cancer	2B72.1	Phase 3	[5]
Rosiglitazone + metformin	DMPIDXT	Diabetic complication	5A2Y	Phase 3	[25]
BGJ398	DMNKBEC	Cholangiocarcinoma	2C12.10	Phase 3	[26]
ARQ-087	DM02BVQ	Intrahepatic cholangiocarcinoma	2C12.10	Phase 3	[27]
AZD4547	DM3827C	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[28]
Debio 1347	DMZW50O	Solid tumour/cancer	2A00-2F9Z	Phase 2	[19]

Drug(s) Targeting NT-3 growth factor receptor (TrkC)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Entrectinib	DMMPTLH	Non-small cell lung cancer	2C25	Approved	[29]
Larotrectinib	DM26CQR	Solid tumour/cancer	2A00-2F9Z	Approved	[30]
Altiratinib	DMUJCBT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[31]
PMID28270021-Compound-WO2016054807Example1	DMD5QEL	Chronic pain	MG30	Patented	[32]
PMID28270010-Compound-Figure24-b	DM0QHLK	N. A.	N. A.	Patented	[31]
Pyrrolo[2,3-d]pyrimidine derivative 4	DME0WSR	Chronic pain	MG30	Patented	[32]
3-amino-5-benzyl-substituted indazole derivative 1	DMFDURZ	Chronic pain	MG30	Patented	[32]
PMID28270010-Compound-Figure5-1	DM2YAPJ	N. A.	N. A.	Patented	[31]
PMID28270021-Compound-WO2015042088Example4	DM6KXOQ	Chronic pain	MG30	Patented	[32]
PMID28270010-Compound-Figure5-2	DMK3GRZ	N. A.	N. A.	Patented	[31]

Drug(s) Targeting Tyrosine-protein kinase Mer (MERTK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ONO-7475	DMV6GX7	Acute leukaemia	2A60	Phase 1/2	[33]
RXDX-106	DM6NVTR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[34]
ONO-7475	DMGBKCJ	Acute myeloid leukaemia	2A60	Phase 1	[19]
MRX-2843	DMM5N8P	Solid tumour/cancer	2A00-2F9Z	Phase 1	[35]
PF-07265807	DMSMNRQ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[36]
INCB81776	DMFOXGB	Solid tumour/cancer	2A00-2F9Z	Phase 1	[37]
LDC1267	DMH7R6L	Discovery agent	N.A.	Investigative	[38]
G749	DMC7HIS	Discovery agent	N.A.	Investigative	[39]
UNC2025	DMCU59W	Glioblastoma of brain	2A00.00	Investigative	[40]
UNC569	DMJL6ZM	Acute lymphoblastic leukaemia	2A85	Investigative	[41]

Drug(s) Targeting Fibroblast growth factor receptor 2 (FGFR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pemigatinib	DM819JF	Cholangiocarcinoma	2C12.10	Approved	[24]
Interferon Alfa-2a, Recombinant	DMUTZ8S	Chronic HCV-1 infection	1E51.1	Approved	[42]
Palifermin	DM9JOYP	Oral mucositis	DA01.11	Approved	[43]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[4]
Trafermin	DMLKI2B	Periodontitis	DA0C	Phase 3	[44]
Debio 1347	DMZW50O	Solid tumour/cancer	2A00-2F9Z	Phase 2	[19]
LY2874455	DMZ0DMY	Solid tumour/cancer	2A00-2F9Z	Phase 2	[45]
AEE-788	DMEOS5K	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[25]
BAY1179470	DM7L91K	Solid tumour/cancer	2A00-2F9Z	Phase 1	[46]
Alofanib	DMIEKTF	Gastric adenocarcinoma	2B72	Phase 1	[47]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Hepatocellular carcinoma	2C12.02	Approved	[48]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[49]
Becaplermin	DM1R5X4	Diabetic complication	5A2Y	Approved	[50]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[4]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[51]
SNN-0031	DM2X3BR	Brain injury	NA07.Z	Phase 1/2	[52]
TAK-593	DMNFZOT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[53]
Pyridine derivative 18	DMBZMYT	N. A.	N. A.	Patented	[54]
PMID25656651-Compound-21a	DMCKAON	N. A.	N. A.	Patented	[55]

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	[56]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[13]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[23]
Midostaurin	DMI6E0R	Acute myeloid leukaemia	2A60	Approved	[25]
Gilteritinib	DMWQ4MZ	Acute myeloid leukaemia	2A60	Approved	[30]
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[57]
Lestaurtinib	DMQ2AIJ	Acute myeloid leukaemia	2A60	Approved (orphan drug)	[58]
Pacritinib	DM1T6ZN	Myelofibrosis	2A20.2	Phase 3	[56]
AC220	DM8Y4JS	Acute myeloid leukaemia	2A60	Phase 3	[19]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]

Drug(s) Targeting VEGFR1 messenger RNA (VEGFR1 mRNA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[59]
VATALANIB	DMY0UEQ	Solid tumour/cancer	2A00-2F9Z	Phase 2	[60]
Sirna-027	DMZTQD8	Exudative age-related macular degeneration	9B78.3Z	Phase 1/2	[61]
PMID22765894C8h	DMH5RFU	Discovery agent	N.A.	Investigative	[62]
2-(1H-indazol-3-yl)-1H-benzo[d]imidazole	DM0CSH8	Discovery agent	N.A.	Investigative	[63]
AAL-993	DM35RFH	Discovery agent	N.A.	Investigative	[60]
PMID17935989C25	DML8ZBR	Discovery agent	N.A.	Investigative	[64]
2-(5-Phenyl-oxazol-2-ylamino)-benzonitrile	DMX6QMT	Discovery agent	N.A.	Investigative	[12]
4-Chloro-N-(3-chloro-benzoyl)-benzenesulfonamide	DMI3OR9	Discovery agent	N.A.	Investigative	[65]
(2-Methoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine	DMQWD75	Discovery agent	N.A.	Investigative	[12]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Hepatocellular carcinoma	2C12.02	Approved	[48]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[22]
Regorafenib	DMHSY1I	Metastatic colorectal cancer	2B91	Approved	[13]
Sunitinib	DMCBJSR	Gastrointestinal cancer	2C11	Approved	[66]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[67]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[25]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[68]
Cabozantinib	DMIYDT4	Thyroid cancer	2D10	Approved	[14]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[3]
Lenvatinib	DMB1IU4	Thyroid cancer	2D10	Approved	[69]

Drug(s) Targeting BDNF/NT-3 growth factors receptor (TrkB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Entrectinib	DMMPTLH	Non-small cell lung cancer	2C25	Approved	[29]
Larotrectinib	DM26CQR	Solid tumour/cancer	2A00-2F9Z	Approved	[30]
PMID28270021-Compound-WO2016054807Example1	DMD5QEL	Chronic pain	MG30	Patented	[32]
PMID28270010-Compound-Figure24-b	DM0QHLK	N. A.	N. A.	Patented	[31]
Pyrrolo[2,3-d]pyrimidine derivative 4	DME0WSR	Chronic pain	MG30	Patented	[32]
3-amino-5-benzyl-substituted indazole derivative 1	DMFDURZ	Chronic pain	MG30	Patented	[32]
PMID28270010-Compound-Figure5-1	DM2YAPJ	N. A.	N. A.	Patented	[31]
PMID28270021-Compound-WO2015042088Example4	DM6KXOQ	Chronic pain	MG30	Patented	[32]
PMID28270010-Compound-Figure5-2	DMK3GRZ	N. A.	N. A.	Patented	[31]
PMID28270010-Compound-Figure5-3	DMSOT1R	N. A.	N. A.	Patented	[31]

Drug(s) Targeting Fibroblast growth factor receptor 3 (FGFR3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pemigatinib	DM819JF	Cholangiocarcinoma	2C12.10	Approved	[24]
Trapidil	DMY67U8	Acute coronary syndrome	BA41	Phase 4	[70]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[4]
TKI258	DMYLT67	Renal cell carcinoma	2C90	Phase 3	[25]
BMS-582664	DMDAN8H	Hepatocellular carcinoma	2C12.02	Phase 3	[25]
Debio 1347	DMZW50O	Solid tumour/cancer	2A00-2F9Z	Phase 2	[19]
B-701	DMOMDA4	Bladder cancer	2C94	Phase 2	[71]
Recifercept	DML8N3Y	Achondroplasia	LD24.00	Phase 2	[72]
AEE-788	DMEOS5K	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[25]
Anti-FGFR3	DM6QENU	Multiple myeloma	2A83	Phase 1	[73]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
BDNF/NT-3 growth factors receptor (TrkB)	TTKN7QR	NTRK2_HUMAN	Inhibitor	[1]
Fibroblast growth factor receptor 1 (FGFR1)	TTRLW2X	FGFR1_HUMAN	Inhibitor	[1]
Fibroblast growth factor receptor 2 (FGFR2)	TTGJVQM	FGFR2_HUMAN	Inhibitor	[1]
Fibroblast growth factor receptor 3 (FGFR3)	TTST7KB	FGFR3_HUMAN	Inhibitor	[1]
Fms-like tyrosine kinase 3 (FLT-3)	TTGJCWZ	FLT3_HUMAN	Inhibitor	[1]
Macrophage-stimulating protein receptor (RON)	TTBQ3OC	RON_HUMAN	Inhibitor	[1]
NT-3 growth factor receptor (TrkC)	TTXABCW	NTRK3_HUMAN	Inhibitor	[1]
Platelet-derived growth factor receptor beta (PDGFRB)	TTI7421	PGFRB_HUMAN	Inhibitor	[1]
Proto-oncogene c-Met (MET)	TTNDSF4	MET_HUMAN	Inhibitor	[1]
Tyrosine-protein kinase Mer (MERTK)	TTO7LKR	MERTK_HUMAN	Inhibitor	[1]
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Inhibitor	[1]
Vascular endothelial growth factor receptor 3 (FLT-4)	TTDCBX5	VGFR3_HUMAN	Inhibitor	[1]
VEGFR1 messenger RNA (VEGFR1 mRNA)	TT1VAUK	VGFR1_HUMAN	Inhibitor	[1]

References

• [1] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [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. (Target id: 1816).
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
• [4] 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.
• [5] Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
• [6] 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.
• [7] Company report (Medigen)
• [8] Advances in kinase targeting: current clinical use and clinical trials. Trends Pharmacol Sci. 2014 Nov;35(11):604-20.
• [9] Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol Cancer Ther. 2006 Apr;5(4):995-1006.
• [10] 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: 1814).
• [11] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [12] Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. J Med Chem. 2005 Mar 10;48(5):1610-9.
• [13] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [14] Clinical pipeline report, company report or official report of Exelixis (2011).
• [15] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [16] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
• [17] Antitumor Activity of Amivantamab (JNJ-61186372), an EGFR-MET Bispecific Antibody, in Diverse Models of EGFR Exon 20 Insertion-Driven NSCLC. Cancer Discov. 2020 Aug;10(8):1194-1209.
• [18] 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: 1815).
• [19] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [20] Beperminogene perplasmid for the treatment of critical limb ischemia. Expert Rev Cardiovasc Ther. 2014 Oct;12(10):1145-56.
• [21] 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: 7948).
• [22] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [23] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [24] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [25] 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.
• [26] Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets. J Bone Miner Res. 2013 Apr;28(4):899-911.
• [27] 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).
• [28] 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.
• [29] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [30] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [31] Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part I.Expert Opin Ther Pat. 2017 Jun;27(6):733-751.
• [32] Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part II.Expert Opin Ther Pat. 2017 Jul;27(7):831-849.
• [33] Clinical pipeline report, company report or official report of Ono Pharmaceutical.
• [34] National Cancer Institute Drug Dictionary (drug name RXDX106).
• [35] The MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia. JCI Insight. 2016 Mar;1(3):e85630.
• [36] National Cancer Institute Drug Dictionary (drug name PF-07265807).
• [37] A Potent and Selective Dual Inhibitor of AXL and MERTK Possesses Both Immunomodulatory and Tumor-Targeted Activity. Front Oncol. 2020 Dec 7;10:598477.
• [38] The E3 ligase Cbl-b and TAM receptors regulate cancer metastasis via natural killer cells. Nature. 2014 Mar 27;507(7493):508-12.
• [39] G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia. Blood. 2014 Apr 3;123(14):2209-19.
• [40] MerTK as a therapeutic target in glioblastoma. Neuro Oncol. 2018 Jan 10;20(1):92-102.
• [41] UNC569, a novel small-molecule mer inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo. Mol Cancer Ther. 2013 Nov;12(11):2367-77.
• [42] DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6.
• [43] Keratinocyte growth factor. Expert Opin Biol Ther. 2009 Jun;9(6):779-87.
• [44] Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
• [45] Company report (Eli Lilly) (drug: LY2874455)
• [46] National Cancer Institute Drug Dictionary (drug id 751593).
• [47] Corrigendum to 'Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models' [Eur J Cancer 61 (2016) 20-28]. Eur J Cancer. 2017 Jan;70:156.
• [48] 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.
• [49] 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.
• [50] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [51] National Cancer Institute Drug Dictionary (drug id 452042).
• [52] Company report (Neuronova)
• [53] 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.
• [54] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
• [55] Bcr-Abl tyrosine kinase inhibitors: a patent review.Expert Opin Ther Pat. 2015 Apr;25(4):397-412.
• [56] 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).
• [57] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [58] 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.
• [59] 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.
• [60] Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1913-9.
• [61] 2011 Pipeline of Sirna Therapeutics.
• [62] The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85.
• [63] Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9.
• [64] Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and prelimina... Bioorg Med Chem Lett. 2007 Dec 1;17(23):6593-601.
• [65] Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents. J Med Chem. 2004 Oct 21;47(22):5367-80.
• [66] 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
• [67] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [68] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [69] Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36.
• [70] Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
• [71] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [72] In vitro and in vivo characterization of Recifercept, a soluble fibroblast growth factor receptor 3, as treatment for achondroplasia. PLoS One. 2020 Dec 28;15(12):e0244368.
• [73] Clinical pipeline report, company report or official report of Genentech (2011).