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

General Information of DTT (ID: TTOU65C)

• DTT Name: Tyrosine-protein kinase SYK (SYK) DTT Info
• UniProt ID: KSYK_HUMAN
• Gene Name: SYK

Molecule-Related Drug & Molecule List

1 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fostamatinib	DM6AUHV	Immune thrombocytopenic purpura	3B64.13	Approved	[1]

12 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fostamatinib disodium	DM3274D	Thrombocytopenia	3B64	Phase 3	[2]
Cerdulatinib	DMSCR2H	B-cell lymphoma	2A86	Phase 2	[3]
GS-9876	DM9Q2B6	Cutaneous lupus erythematosus	EB5Z	Phase 2	[4], [5]
GS-9973	DMKWCTR	Acute myeloid leukaemia	2A60	Phase 2	[6]
TAK-659	DMJH3U0	Diffuse large B-cell lymphoma	2A81	Phase 2	[7]
HM43239	DMV1SDA	Acute myeloid leukaemia	2A60	Phase 1/2	[8]
GSK2646264	DMQOM5V	Cutaneous lupus erythematosus	EB5Z	Phase 1	[5]
HMPL-523	DMXZ1A8	Non-hodgkin lymphoma	2B33.5	Phase 1	[9]
PRT-062607	DMBL7CW	Chronic lymphocytic leukaemia	2A82.0	Phase 1	[10]
PRT6207	DMP5CLY	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
SKI-O-703	DMTSKXR	Rheumatoid arthritis	FA20	Phase 1	[4]
tamatinib	DMGANIC	Solid tumour/cancer	2A00-2F9Z	Clinical trial	[11]

4 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pyrimidopyridazinone derivative 1	DM32N7D	N. A.	N. A.	Patented	[12]
Pyrimidopyridazinone derivative 2	DMD1RT0	N. A.	N. A.	Patented	[12]
Pyrrolo-pyrazine derivative 3	DMLM6DT	N. A.	N. A.	Patented	[13]
Pyrrolo-pyrazine derivative 4	DMD1S92	N. A.	N. A.	Patented	[13]

2 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
R-343	DMEJNM1	Asthma	CA23	Discontinued in Phase 2	[14]
PF-3526299	DMMU1W3	Asthma	CA23	Discontinued in Phase 1	[15]

10 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CG-103065	DMGW9QL	Solid tumour/cancer	2A00-2F9Z	Investigative	[1]
DNX-2000	DMC5RL7	Autoimmune diabetes	5A10	Investigative	[1]
ELLAGIC ACID	DMX8BS5	Discovery agent	N.A.	Investigative	[16]
K00592a	DM1RP5Q	Discovery agent	N.A.	Investigative	[17]
N-Benzyl-4-(2,5-dihydroxy-benzylamino)-benzamide	DMUD85N	Discovery agent	N.A.	Investigative	[18]
PMID17600705C23	DMJFOGW	Discovery agent	N.A.	Investigative	[19]
PMID23312943C21	DMOJ8QR	Discovery agent	N.A.	Investigative	[20]
PRT-060318	DMQPEA7	Thrombosis	DB61-GB90	Investigative	[1]
SBB007833	DMU8KGB	Discovery agent	N.A.	Investigative	[21]
VRT-750018	DMFT49S	Allergy	4A80-4A85	Investigative	[1]

References

• [1] 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: 2230).
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] Company report (Portola Pharmaceuticals)
• [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 the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [6] An open-label phase 2 trial of entospletinib (GS-9973), a selective spleen tyrosine kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2015 Apr 9;125(15):2336-43.
• [7] J Clin Oncol 32:5s, 2014 (suppl; abstr 8580).
• [8] Clinical pipeline report, company report or official report of Hanmi Pharmaceutical.
• [9] Clinical pipeline report, company report or official report of Hutchison MediPharma.
• [10] Advances in kinase inhibition: treating rheumatic diseases and beyond. Curr Opin Rheumatol. 2014 March; 26(2): 237-243.
• [11] Pharmacophore modeling study based on known spleen tyrosine kinase inhibitors together with virtual screening for identifying novel inhibitors. Bioorg Med Chem Lett. 2009 Apr 1;19(7):1944-9.
• [12] Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 1.Expert Opin Ther Pat. 2017 Feb;27(2):127-143.
• [13] Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 2.Expert Opin Ther Pat. 2017 Feb;27(2):145-161.
• [14] A novel Syk kinase inhibitor suitable for inhalation: R-343(. Expert Opin Ther Pat. 2009 Oct;19(10):1469-72.
• [15] Pipeline report of RIGEL Pharmaceuticals.
• [16] Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application. J Med Chem. 2006 Apr 20;49(8):2363-6.
• [17] Synthetic studies on novel Syk inhibitors. Part 1: Synthesis and structure-activity relationships of pyrimidine-5-carboxamide derivatives. Bioorg Med Chem. 2005 Aug 15;13(16):4936-51.
• [18] Design, synthesis, and biological evaluation of a series of lavendustin A analogues that inhibit EGFR and Syk tyrosine kinases, as well as tubulin ... J Med Chem. 2001 Feb 1;44(3):441-52.
• [19] N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: indazoles as phenol isosteres with improved pharmacokinetics. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4363-8.
• [20] Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. Bioorg Med Chem Lett. 2013 Feb 15;23(4):1051-5.
• [21] Synthesis and pharmacological evaluation of novel beta-nitrostyrene derivatives as tyrosine kinase inhibitors with potent antiplatelet activity. Biochem Pharmacol. 2007 Aug 15;74(4):601-11.