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

General Information of Drug (ID: DM0VOXN)

• Drug Name: PMID21982499C14k Drug Info
• Synonyms: GTPL8214; BDBM50357587

Indication

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

• Cross-matching ID:
  PubChem CID: 44222958
  TTD Drug ID: DM0VOXN

Molecule-Related Drug Atlas

Drug(s) Targeting Serine/threonine-protein kinase pim-2 (PIM2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LGH-447	DMQN9ME	Multiple myeloma	2A83	Phase 1/2	[2]
AZD1208	DMBEA6V	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
IDDBCP226234	DMBFX5H	Inflammation	1A00-CA43.1	Investigative	[4]

Drug(s) Targeting PIM-3 protein kinase (PIM3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
US9682991, 23	DMGTIP6	N. A.	N. A.	Patented	[5]
US8889696, Staurosporine	DMSYUHK	N. A.	N. A.	Patented	[6]
US8829193, 3	DM5ZGK3	N. A.	N. A.	Patented	[7]
BDBM50061601	DMQ4TUE	N. A.	N. A.	Patented	[8]
US9580418, Example 8	DMGH9B3	N. A.	N. A.	Patented	[9]
BDBM50061608	DM3MRD9	N. A.	N. A.	Patented	[8]
US8481586, 15	DMFEUMZ	N. A.	N. A.	Patented	[10]
US9434725, 315	DM316FB	N. A.	N. A.	Patented	[11]
BDBM50061612	DMM8IDC	N. A.	N. A.	Patented	[8]
US8669361, 102	DM4G3OC	N. A.	N. A.	Patented	[12]

Drug(s) Targeting Serine/threonine-protein kinase pim-1 (PIM1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SEL-24	DMH064K	Acute myeloid leukaemia	2A60	Phase 1/2	[13]
CXR-1002	DM4GJ50	Solid tumour/cancer	2A00-2F9Z	Phase 1	[14]
Benzothiazine derivative 1	DMMVHY4	N. A.	N. A.	Patented	[15]
leucettine L41	DMBYND6	Discovery agent	N.A.	Investigative	[16]
PMID22136433C20	DMI8217	Discovery agent	N.A.	Investigative	[17]
NCGC00167772-01	DMY8RT9	Discovery agent	N.A.	Investigative	[13]
SMI-4a	DMBLWMS	Non-small-cell lung cancer	2C25	Investigative	[18]

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	[19]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[20]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[21]
Midostaurin	DMI6E0R	Acute myeloid leukaemia	2A60	Approved	[22]
Gilteritinib	DMTI0ZO	Acute myeloid leukaemia	2A60	Approved	[23]
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[24]
Pacritinib	DM1T6ZN	Myelofibrosis	2A20.2	Approved	[19]
Quizartinib	DM8Y4JS	Acute myeloid leukaemia	2A60	Approved	[25]
Lestaurtinib	DMQ2AIJ	Acute myeloid leukaemia	2A60	Approved (orphan drug)	[26]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[27]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Casein kinase I gamma-3 (CSNK1G3)	TT34L5N	KC1G3_HUMAN	Inhibitor	[1]
Fms-like tyrosine kinase 3 (FLT-3)	TTGJCWZ	FLT3_HUMAN	Inhibitor	[1]
PIM-3 protein kinase (PIM3)	TTCGOIN	PIM3_HUMAN	Inhibitor	[1]
Serine/threonine-protein kinase pim-1 (PIM1)	TTTN5QW	PIM1_HUMAN	Inhibitor	[1]
Serine/threonine-protein kinase pim-2 (PIM2)	TT69J2Z	PIM2_HUMAN	Inhibitor	[1]

References

• [1] 7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6687-92.
• [2] Pan-PIM kinase inhibition provides a novel therapy for treating hematologic cancers. Clin Cancer Res. 2014 Apr 1;20(7):1834-45.
• [3] AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia. Blood. 2014 Feb 6;123(6):905-13.
• [4] 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: 2159).
• [5] Tricyclic compounds for use as kinase inhibitors. US9682991.
• [6] Substituted pyrido[2,3-d]pyrimidin-7(8H)-ones and therapeutic uses thereof. US8889696.
• [7] PIM kinase inhibitors and methods of their use. US8829193.
• [8] Azole compounds as PIM inhibitors. US9321756.
• [9] Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors. US9580418.
• [10] Pyrrolo[2,3-a] carbazoles and use thereof as PIM kinase inhibitors. US8481586.
• [11] 5-azaindazole compounds and methods of use. US9434725.
• [12] Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use. US9573943.
• [13] 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: 2158).
• [14] 123 Antitumor activity of CXR1002, a novel anti-cancer clinical phase compound that induces ER stress and inhibits PIM kinases: Human tumor xenograft efficacy and in vitro mode of action. EJC Supplements, 2010; 8(7):45-46.
• [15] Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014).Expert Opin Ther Pat. 2015;25(9):953-70.
• [16] Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. J Med Chem. 2011 Jun 23;54(12):4172-86.
• [17] 7,8-dichloro-1-oxo-beta-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes. J Med Chem. 2012 Jan 12;55(1):403-13.
• [18] Pim-1 inhibitor SMI-4a suppresses tumor growth in non-small cell lung cancer via PI3K/AKT/mTOR pathway. Onco Targets Ther. 2019 Apr 23;12:3043-3050.
• [19] 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).
• [20] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [21] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [22] 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.
• [23] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [24] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [25] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [26] 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.
• [27] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.