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

General Information of Drug (ID: DMJFOGW)

• Drug Name: PMID17600705C23 Drug Info
• Synonyms: GTPL8146; BDBM26166

Indication

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

• Cross-matching ID:
  PubChem CID: 23657507
  TTD Drug ID: DMJFOGW

Molecule-Related Drug Atlas

Drug(s) Targeting LCK tyrosine protein kinase (LCK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dasatinib	DMJV2EK	Blast phase chronic myelogenous leukemia, BCR-ABL1 positive		Approved	[2]
VX-680	DM93YKJ	Solid tumour/cancer	2A00-2F9Z	Phase 2	[2]
JNJ-26483327	DMSQ3AZ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
ISIS-CRP	DMQDUG4	Cardiovascular disease	BA00-BE2Z	Phase 1	[4]
RO-316233	DMAGLPW	Discovery agent	N.A.	Investigative	[5]
Bisindolylmaleimide-I	DMOQJZC	Discovery agent	N.A.	Investigative	[5]
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole	DMN9YOB	Discovery agent	N.A.	Investigative	[6]
CI-1040	DMF3DZX	Discovery agent	N.A.	Investigative	[5]
AMP-PNP	DMTOK1D	Discovery agent	N.A.	Investigative	[7]
BMS-536924	DMXJB4N	Discovery agent	N.A.	Investigative	[8]

Drug(s) Targeting Tyrosine-protein kinase TXK (TXK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID24915291C38	DMBXT9J	Discovery agent	N.A.	Investigative	[9]
PMID24915291C31	DMN7QB8	Discovery agent	N.A.	Investigative	[9]

Drug(s) Targeting Tyrosine-protein kinase SYK (SYK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fostamatinib	DM6AUHV	Immune thrombocytopenic purpura	3B64.13	Approved	[10]
Fostamatinib disodium	DM3274D	Thrombocytopenia	3B64	Phase 3	[11]
Cerdulatinib	DMSCR2H	B-cell lymphoma	2A86	Phase 2	[12]
TAK-659	DMJH3U0	Diffuse large B-cell lymphoma	2A81	Phase 2	[13]
GS-9876	DM9Q2B6	Cutaneous lupus erythematosus	EB5Z	Phase 2	[14]
GS-9973	DMKWCTR	Acute myeloid leukaemia	2A60	Phase 2	[15]
Cevidoplenib	DM9QU5G	Rheumatoid arthritis	FA20	Phase 2	[16]
HM43239	DMV1SDA	Acute myeloid leukaemia	2A60	Phase 1/2	[17]
ALXN2075	DM1BSD8	Non-hodgkin lymphoma	2B33.5	Phase 1/2	[18]
SKI-O-703	DMTSKXR	Rheumatoid arthritis	FA20	Phase 1	[14]

Drug(s) Targeting Tyrosine-protein kinase Lyn (JTK8)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Bafetinib	DM7586F	Bone disease	FC0Z	Phase 2	[19]
JNJ-26483327	DMSQ3AZ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
Alkynyl-substituted pyrimidinyl-pyrrole derivative 1	DMK7DJ2	N. A.	N. A.	Patented	[20]
NG-25	DMC48D9	Discovery agent	N.A.	Investigative	[21]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
LCK tyrosine protein kinase (LCK)	TT860QF	LCK_HUMAN	Inhibitor	[1]
Tyrosine-protein kinase Lyn (JTK8)	TT1RWNJ	LYN_HUMAN	Inhibitor	[1]
Tyrosine-protein kinase SYK (SYK)	TTOU65C	KSYK_HUMAN	Inhibitor	[1]
Tyrosine-protein kinase TXK (TXK)	TT8M1DP	TXK_HUMAN	Inhibitor	[1]

References

• [1] 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.
• [2] 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.
• [3] National Cancer Institute Drug Dictionary (drug id 596693).
• [4] The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
• [5] Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
• [6] Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem. 2004 Dec 2;47(25):6239-47.
• [7] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [8] Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitum... J Med Chem. 2005 Sep 8;48(18):5639-43.
• [9] Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. J Med Chem. 2014 Jun 26;57(12):5112-28.
• [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: 2230).
• [11] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [12] Company report (Portola Pharmaceuticals)
• [13] J Clin Oncol 32:5s, 2014 (suppl; abstr 8580).
• [14] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [15] 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.
• [16] A novel selective spleen tyrosine kinase inhibitor SKI-O-703 (cevidoplenib) ameliorates lupus nephritis and serum-induced arthritis in murine models. Clin Exp Immunol. 2023 Mar 8;211(1):31-45.
• [17] Clinical pipeline report, company report or official report of Hanmi Pharmaceutical.
• [18] The Dual Syk/JAK Inhibitor Cerdulatinib Antagonizes B-cell Receptor and Microenvironmental Signaling in Chronic Lymphocytic Leukemia. Clin Cancer Res. 2017 May 1;23(9):2313-2324.
• [19] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [20] 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.
• [21] Discovery of type II inhibitors of TGFbeta-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J Med Chem. 2015 Jan 8;58(1):183-96.