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

General Information of Drug (ID: DMCJXWK)

• Drug Name: URMC-099 Drug Info
• Synonyms: compound 1 [PMID 24044867]

Indication

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

• Cross-matching ID:
  PubChem CID: 54764565
  TTD Drug ID: DMCJXWK

Molecule-Related Drug Atlas

Drug(s) Targeting Leucine-rich repeat kinase 2 (LRRK2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
DNL151	DMZT89C	Parkinson disease	8A00.0	Phase 1	[2]
DNL201	DMFEORD	Parkinson disease	8A00.0	Phase 1	[2]
BIIB094	DMLUO5K	Parkinson disease	8A00.0	Phase 1	[3]
Pyrrolo-pyridine derivative 2	DMVNY5I	N. A.	N. A.	Patented	[4]
Bidentate ligands of Markush derivative 2	DM2QNMC	N. A.	N. A.	Patented	[4]
Oxindole derivative 3	DM0ENF3	N. A.	N. A.	Patented	[4]
Aminopyridine derivative 3	DMSLJE8	N. A.	N. A.	Patented	[4]
Fused thiophene derivative 1	DMV7IX4	N. A.	N. A.	Patented	[4]
Oxindole derivative 4	DM3U58I	N. A.	N. A.	Patented	[4]
Bidentate ligands of Markush derivative 1	DMB08D3	N. A.	N. A.	Patented	[4]

Drug(s) Targeting Mixed lineage kinase 3 (MAP3K11)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CEP-5104	DMV43GY	Discovery agent	N.A.	Investigative	[5]
CEP-6331	DMNXBTD	Discovery agent	N.A.	Investigative	[5]
CEP1349	DMOAZX5	Discovery agent	N.A.	Investigative	[6]
PMID24044867C8	DML4KMP	Discovery agent	N.A.	Investigative	[1]

Drug(s) Targeting Mixed lineage kinase 1 (MAP3K9)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CEP1347	DMXCD69	Asthma	CA23	Phase 2/3	[6]
CEP-5104	DMV43GY	Discovery agent	N.A.	Investigative	[5]
CEP-6331	DMNXBTD	Discovery agent	N.A.	Investigative	[5]

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	[7]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[8]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[9]
Midostaurin	DMI6E0R	Acute myeloid leukaemia	2A60	Approved	[10]
Gilteritinib	DMTI0ZO	Acute myeloid leukaemia	2A60	Approved	[11]
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[12]
Pacritinib	DM1T6ZN	Myelofibrosis	2A20.2	Approved	[7]
Quizartinib	DM8Y4JS	Acute myeloid leukaemia	2A60	Approved	[13]
Lestaurtinib	DMQ2AIJ	Acute myeloid leukaemia	2A60	Approved (orphan drug)	[14]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[15]

Drug(s) Targeting MAPK/ERK kinase kinase 2 (MAP3K2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CI-1040	DMF3DZX	Discovery agent	N.A.	Investigative	[6]
U0126	DM31OGF	Discovery agent	N.A.	Investigative	[6]
Ro092210	DM2DXHO	Discovery agent	N.A.	Investigative	[6]
LLZ16407	DM783BP	Discovery agent	N.A.	Investigative	[6]

Drug(s) Targeting Mixed lineage kinase 2 (MAP3K10)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CEP-5104	DMV43GY	Discovery agent	N.A.	Investigative	[5]
CEP-6331	DMNXBTD	Discovery agent	N.A.	Investigative	[5]
CEP1348	DMA7JO4	Discovery agent	N.A.	Investigative	[6]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Cyclin-dependent kinase-like 2 (CDKL2)	TTMO45N	CDKL2_HUMAN	Inhibitor	[1]
Death-associated protein kinase 3 (DAPK3)	TTERVQN	DAPK3_HUMAN	Inhibitor	[1]
Fms-like tyrosine kinase 3 (FLT-3)	TTGJCWZ	FLT3_HUMAN	Inhibitor	[1]
Leucine-rich repeat kinase 2 (LRRK2)	TTK0FEA	LRRK2_HUMAN	Inhibitor	[1]
MAPK/ERK kinase kinase 2 (MAP3K2)	TTK1N5G	M3K2_HUMAN	Inhibitor	[1]
Mixed lineage kinase 1 (MAP3K9)	TTUNSIX	M3K9_HUMAN	Inhibitor	[1]
Mixed lineage kinase 2 (MAP3K10)	TT9FN4J	M3K10_HUMAN	Inhibitor	[1]
Mixed lineage kinase 3 (MAP3K11)	TTETX6Q	M3K11_HUMAN	Inhibitor	[1]
SRSF protein kinase 2 (SRPK2)	TTCZEJ9	SRPK2_HUMAN	Inhibitor	[1]

References

• [1] Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. J Med Chem. 2013 Oct 24;56(20):8032-48.
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] Clinical pipeline report, company report or official report of Ionis
• [4] Leucine-rich repeat kinase 2 inhibitors: a patent review (2014-2016).Expert Opin Ther Pat. 2017 Jun;27(6):667-676.
• [5] Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-linea... J Med Chem. 2008 Sep 25;51(18):5680-9.
• [6] Pharmacological inhibitors of MAPK pathways. Trends Pharmacol Sci. 2002 Jan;23(1):40-5.
• [7] 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).
• [8] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [9] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [10] 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.
• [11] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [12] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [13] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [14] 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.
• [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.