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

General Information of Drug (ID: DMK7DJ2)

• Drug Name: Alkynyl-substituted pyrimidinyl-pyrrole derivative 1 Drug Info
• Synonyms: PMID27774822-Compound-Figure3compound11
• Cross-matching ID: TTD Drug ID: DMK7DJ2

Molecule-Related Drug Atlas

Drug(s) Targeting Janus kinase 2 (JAK-2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Momelotinib	DMF98Q0	Myelofibrosis	2A20.2	Approved	[2]
Baricitinib	DM4ONW5	Rheumatoid arthritis	FA20	Approved	[3]
Ruxolitinib	DM7Q98D	Essential thrombocythemia	3B63.1Z	Approved	[4]
Pacritinib	DM1T6ZN	Myelofibrosis	2A20.2	Approved	[5]
Fedratinib	DM4ZBK6	Myelofibrosis	2A20.2	Approved	[6]
ITF2357	DMFZBNE	Duchenne dystrophy	8C70	Phase 3	[7]
XL019	DMJ6F5C	Solid tumour/cancer	2A00-2F9Z	Phase 3	[7]
Cerdulatinib	DMSCR2H	B-cell lymphoma	2A86	Phase 2	[8]
CTP-543	DM3SYOK	Alopecia	ED70	Phase 2	[9]
INCB039110	DMD9RV3	Malignant neoplasm	2A00-2F9Z	Phase 2	[10]

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	[11]
JNJ-26483327	DMSQ3AZ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[12]
NG-25	DMC48D9	Discovery agent	N.A.	Investigative	[13]
PMID17600705C23	DMJFOGW	Discovery agent	N.A.	Investigative	[14]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Janus kinase 2 (JAK-2)	TTRMX3V	JAK2_HUMAN	Inhibitor	[1]
Tyrosine-protein kinase Lyn (JTK8)	TT1RWNJ	LYN_HUMAN	Inhibitor	[1]

References

• [1] 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.
• [2] Genetic determinants of response and survival in momelotinib-treated patients with myelofibrosis.Leukemia.2015 Mar;29(3):741-4.
• [3] Selective JAK inhibitors in development for rheumatoid arthritis. Expert Opin Investig Drugs. 2014 Aug;23(8):1067-77.
• [4] 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
• [5] National Cancer Institute Drug Dictionary (drug id 609888).
• [6] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [7] Emerging drugs for the therapy of primary and post essential thrombocythemia, post polycythemia vera myelofibrosis. Expert Opin Emerg Drugs. 2009 Sep;14(3):471-9.
• [8] Company report (Portola Pharmaceuticals)
• [9] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [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: 2048).
• [11] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [12] National Cancer Institute Drug Dictionary (drug id 596693).
• [13] 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.
• [14] 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.