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

General Information of Drug (ID: DMXYT40)

• Drug Name: Pyridine derivative 19 Drug Info
• Synonyms: PMID27646564-Compound-5-1
• Cross-matching ID: TTD Drug ID: DMXYT40

Molecule-Related Drug Atlas

Drug(s) Targeting Macrophage colony-stimulating factor 1 receptor (CSF1R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[2]
Sulfatinib	DMPOTM4	Neuroendocrine cancer	2B72.1	Phase 3	[3]
ARRY-382	DM0VGDC	Solid tumour/cancer	2A00-2F9Z	Phase 2	[3]
BLZ-945	DMG1LVA	Amyotrophic lateral sclerosis	8B60.0	Phase 2	[3]
Cabiralizumab	DMGE058	Pancreatic cancer	2C10	Phase 2	[4]
AMB-05X	DM958C5	Idiopathic pulmonary fibrosis	CB03.4	Phase 2	[5]
FPA-008	DM3ZN6Y	Autoimmune diabetes	5A10	Phase 1/2	[6]
DCC-3014	DMHW289	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[3]
DCC-3014	DMHW289	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[7]
PLX7486	DM0IVGU	Pancreatic cancer	2C10	Phase 1	[3]

Drug(s) Targeting Platelet-derived growth factor receptor alpha (PDGFRA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[8]
Ripretinib	DM958QB	Gastrointestinal stromal tumour	2B5B	Approved	[9]
Olaratumab	DMNYOIX	Soft tissue sarcoma	2B57	Approved	[10]
Avapritinib	DMK2GZX	Gastrointestinal stromal tumour	2B5B	Approved	[11]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[12]
CP-868596	DMZIM37	Gastrointestinal cancer	2C11	Phase 3	[13]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[14]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[15]
MP470	DMELUAK	Solid tumour/cancer	2A00-2F9Z	Phase 2	[16]
MEDI-575	DMI9WVM	Glioblastoma multiforme	2A00.0	Phase 2	[17]

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	[18]
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[19]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[20]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[21]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[21]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[22]
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[2]
Ripretinib	DM958QB	Gastrointestinal stromal tumour	2B5B	Approved	[9]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[14]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[15]

Drug(s) Targeting Proto-oncogene c-Ret (RET)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[23]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[21]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[21]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[18]
Selpercatinib	DMZR15V	Non-small-cell lung cancer	2C25.Y	Approved	[24]
Pralsetinib	DMWU0I2	Non-small-cell lung cancer	2C25.Y	Approved	[25]
MGCD516	DM752PU	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[26]
CEP-32496	DMAO04B	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[3]
TPX-0046	DMIVE67	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[27]
GSK3179106	DM2KCIP	Inflammatory bowel disease	DD72	Phase 1	[28]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Macrophage colony-stimulating factor 1 receptor (CSF1R)	TT7MRDV	CSF1R_HUMAN	Inhibitor	[1]
Platelet-derived growth factor receptor alpha (PDGFRA)	TT8FYO9	PGFRA_HUMAN	Inhibitor	[1]
Proto-oncogene c-Ret (RET)	TT4DXQT	RET_HUMAN	Inhibitor	[1]
Tyrosine-protein kinase Kit (KIT)	TTX41N9	KIT_HUMAN	Inhibitor	[1]

References

• [1] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [3] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [4] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [5] Clinical pipeline report, company report or official report of AmMax Bio
• [6] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [7] Clinical pipeline report, company report or official report of Deciphera Pharmaceuticals.
• [8] 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.
• [9] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [10] A phase I study of olaratumab, an anti-platelet-derived growth factor receptor alpha (PDGFRalpha) monoclonal antibody, in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Mar;73(3):595-604.
• [11] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [12] 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.
• [13] The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations.Invest New Drugs.2015 Apr;33(2):300-9.
• [14] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [15] National Cancer Institute Drug Dictionary (drug id 452042).
• [16] Phase 1B study of amuvatinib in combination with five standard cancer therapies in adults with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Jul;74(1):195-204.
• [17] Clinical pipeline report, company report or official report of MedImmune (2011).
• [18] 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.
• [19] 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.
• [20] 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.
• [21] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [22] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [23] Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. Bioorg Med Chem. 2010 Feb 15;18(4):1482-96.
• [24] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [25] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [26] 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: 2185).
• [27] Clinical pipeline report, company report or official report of Turning Point Therapeutics.
• [28] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)