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

General Information of DTT (ID: TTRMX3V)

• DTT Name: Janus kinase 2 (JAK-2) DTT Info
• UniProt ID: JAK2_HUMAN
• Gene Name: JAK2

Molecule-Related Drug & Molecule List

3 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Baricitinib	DM4ONW5	Rheumatoid arthritis	FA20	Approved	[1]
Fedratinib	DM4ZBK6	Myelofibrosis	2A20.2	Approved	[2]
Ruxolitinib	DM7Q98D	Essential thrombocythemia	3B63.1Z	Approved	[3]

15 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ITF2357	DMFZBNE	Duchenne dystrophy	8C70	Phase 3	[4], [5]
Momelotinib	DMF98Q0	Myelofibrosis	2A20.2	Phase 3	[6], [7]
Pacritinib	DM1T6ZN	Myelofibrosis	2A20.2	Phase 3	[8]
XL019	DMJ6F5C	Solid tumour/cancer	2A00-2F9Z	Phase 3	[4]
AZD1480	DMLK59M	Myeloproliferative syndrome	2A22	Phase 2	[9]
BMS-911543	DMF46PD	Myelofibrosis	2A20.2	Phase 2	[10]
Cerdulatinib	DMSCR2H	B-cell lymphoma	2A86	Phase 2	[11]
CTP-543	DM3SYOK	Asthma	CA23	Phase 2	[12]
CTP-543	DMBT46Y	Alopecia	ED70	Phase 2	[13]
INCB039110	DMD9RV3	Malignant neoplasm	2A00-2F9Z	Phase 2	[14]
LY2784544	DMZASMP	Breast cancer	2C60-2C65	Phase 2	[15]
NS-018	DMU9BCD	Myelofibrosis	2A20.2	Phase 1/2	[16]
AC430	DMPS6U9	leukaemia	2A60-2B33	Phase 1	[1]
Peginterferon beta	DMQ4Z1P	Multiple sclerosis	8A40	Phase 1	[17]
SB-1578	DMXTKYR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[1], [18]

76 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
1,2,4-triazolo[1,5a]pyridine derivative 1	DMIUPSA	N. A.	N. A.	Patented	[19]
1,2,4-triazolo[1,5a]pyridine derivative 2	DMZFILT	N. A.	N. A.	Patented	[19]
Alkynyl-substituted pyrimidinyl-pyrrole derivative 1	DMK7DJ2	N. A.	N. A.	Patented	[20]
Aminooxazole carboxamide derivative 1	DMDHGPN	N. A.	N. A.	Patented	[20]
Aminotriazolopyridine derivative 1	DMW2LZ0	N. A.	N. A.	Patented	[19]
Aromatic bicyclic compound 1	DMVLQ2P	N. A.	N. A.	Patented	[21]
Aromatic bicyclic compound 2	DMKFV67	N. A.	N. A.	Patented	[21]
Aromatic bicyclic compound 3	DMRXN94	N. A.	N. A.	Patented	[21]
Aromatic bicyclic compound 4	DM3E75P	N. A.	N. A.	Patented	[21]
Aromatic bicyclic compound 5	DMALF06	N. A.	N. A.	Patented	[21]
Aromatic bicyclic compound 6	DM8L3KM	N. A.	N. A.	Patented	[21]
Benzimidazole derivative 7	DMDK4RI	N. A.	N. A.	Patented	[19]
Bis-aminopyrimidine derivative 1	DMQL34C	N. A.	N. A.	Patented	[19]
Bis-aminopyrimidine derivative 2	DMJXNO1	N. A.	N. A.	Patented	[19]
Bis-aminopyrimidine derivative 3	DMUNSYX	N. A.	N. A.	Patented	[19]
Bis-aminopyrimidine derivative 4	DMO1ZIG	N. A.	N. A.	Patented	[19]
Bis-aminopyrimidine derivative 5	DMWXLK1	N. A.	N. A.	Patented	[19]
Curcumin analog 1	DM4765M	N. A.	N. A.	Patented	[21]
Curcumin analog 2	DMZ8S6X	N. A.	N. A.	Patented	[21]
Cyanomethyl pypazole carboxamide derivative 1	DMD198F	N. A.	N. A.	Patented	[20]
Cyclic cyanoethypypazole derivative 1	DM2BZI0	N. A.	N. A.	Patented	[20]
Cycloalkyl nitrile pyrazole carboxamide derivative 1	DM3RK0S	N. A.	N. A.	Patented	[20]
Cycloalkyl nitrile pyrazolo pyridone derivative 1	DMD3LK1	N. A.	N. A.	Patented	[20]
Cycloalkyl nitrile pyrazolo pyridone derivative 2	DMW4JB0	N. A.	N. A.	Patented	[20]
Five-and-six-membered heterocyclic compound 1	DM7SK5Q	N. A.	N. A.	Patented	[20]
Geminally-substituted cyanoethylpypazolo pyridone derivative 1	DMK6RFS	N. A.	N. A.	Patented	[20]
Geminally-substituted cyanoethylpypazolo pyridone derivative 2	DMB2INX	N. A.	N. A.	Patented	[20]
Imidazo[4,5-c]pyridine derivative 2	DMFDRJT	N. A.	N. A.	Patented	[19]
Isoxazole derivative 1	DMUMPZX	N. A.	N. A.	Patented	[20]
Isoxazole derivative 2	DMT842O	N. A.	N. A.	Patented	[20]
N-(cyanomethyl)-4-(2-(phenylamino)pyrimidin-4-yl)benzamide derivative 1	DM0OMAL	N. A.	N. A.	Patented	[19]
PMID27774822-Compound-Figure10Compound12	DMFAGOZ	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure10Compound4	DMMJVTW	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure10Example1	DMCTXPQ	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure10Example19	DMNXYZP	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure11Example5	DMAHFXV	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure1Example20	DMCL19N	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure2Example1-1left	DM86M7D	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure2Example1-1right	DM2YPLF	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure3CompoundI-165	DMOENP4	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure7Example63	DMF5IWB	N. A.	N. A.	Patented	[20]
PMID27774822-Compound-Figure8Example5	DMRHZF3	N. A.	N. A.	Patented	[20]
PMID27774824-Compound-Figure11Example1up	DMH1W8F	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure2Example4	DMQHYMJ	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure3Example18	DMYZ6XQ	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure6Example12	DM1CM7S	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure6Example6	DMB18V5	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure7Example10	DMT85AH	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure8Example22	DM6OCSJ	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure8Example99	DM1VOPH	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure9Example2down	DMXAV42	N. A.	N. A.	Patented	[19]
PMID27774824-Compound-Figure9Example2up	DME3TMS	N. A.	N. A.	Patented	[19]
Pyrazolopyridine derivative 3	DM2VQ4P	N. A.	N. A.	Patented	[20]
Pyrazolopyridine derivative 4	DMX7RWV	N. A.	N. A.	Patented	[20]
Pyrazolopyridine derivative 6	DM5OH8D	N. A.	N. A.	Patented	[19]
Pyrazolopyridine derivative 7	DMCTQ9O	N. A.	N. A.	Patented	[19]
Pyrazolo[4,3-c]pyridine derivative 2	DMCDFLQ	N. A.	N. A.	Patented	[19]
Pyrimidopyridazinone derivative 1	DM32N7D	N. A.	N. A.	Patented	[19]
Pyrimidopyridazinone derivative 2	DMD1RT0	N. A.	N. A.	Patented	[19]
Pyrrole derivative 7	DMZCERW	N. A.	N. A.	Patented	[20]
Pyrrole six-membered heteroaryl ring derivative 1	DM1A0VB	N. A.	N. A.	Patented	[20]
Pyrrolo-pyridine derivative 3	DMSNQEJ	N. A.	N. A.	Patented	[20]
Pyrrolo-pyridone derivative 1	DMR6QCE	N. A.	N. A.	Patented	[20]
Pyrrolo-pyridone derivative 2	DMCZ8UV	N. A.	N. A.	Patented	[20]
Pyrrolo[2,3-d]pyrimidine derivative 11	DM983CY	N. A.	N. A.	Patented	[19]
Pyrrolo[2,3-d]pyrimidine derivative 6	DM3D1L6	N. A.	N. A.	Patented	[20]
Pyrrolo[2,3-d]pyrimidine derivative 7	DM30Y8M	N. A.	N. A.	Patented	[20]
Pyrrolo[2,3-d]pyrimidine derivative 8	DMAW6KU	N. A.	N. A.	Patented	[20]
Ruxolitinib derivative 2	DMSJWZ3	N. A.	N. A.	Patented	[19]
Triazolo-pyridine derivative 1	DM0Q9VY	N. A.	N. A.	Patented	[20]
Tricyclic compound 1	DMLBR4F	N. A.	N. A.	Patented	[19]
Tricyclic compound 11	DMJAZ7D	N. A.	N. A.	Patented	[20]
Tricyclic heterocycle derivative 1	DMXLJH4	N. A.	N. A.	Patented	[20]
Tricyclic heterocycle derivative 2	DM1W02D	N. A.	N. A.	Patented	[19]
Tricyclic heterocycle derivative 5	DMG1ESV	N. A.	N. A.	Patented	[20]
Tricyclic pyrrolopyridine compound 1	DMFIXW4	N. A.	N. A.	Patented	[20]

1 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AG490	DM3WKO5	Multiple myeloma	2A83	Terminated	[22], [23]

14 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
1,2,3,4,5,6-hexabromocyclohexane	DMVD702	Liver cancer	2C12	Investigative	[24]
5-phenyl-1H-indazol-3-amine	DMJBEIF	Discovery agent	N.A.	Investigative	[25]
AMG-JAK2-01	DMSQ49N	Myeloproliferative syndrome	2A22	Investigative	[14]
Atropisomer 1	DML3R5Z	Discovery agent	N.A.	Investigative	[26]
AZ960	DM95Y82	Discovery agent	N.A.	Investigative	[27]
BVB-808	DM10UHA	Solid tumour/cancer	2A00-2F9Z	Investigative	[14]
CMP-6	DM241YW	Discovery agent	N.A.	Investigative	[28]
K-454	DMYSMWI	Solid tumour/cancer	2A00-2F9Z	Investigative	[14]
NSC-1771	DMNXDGQ	Discovery agent	N.A.	Investigative	[29]
ON-044580	DMWOHDV	Solid tumour/cancer	2A00-2F9Z	Investigative	[30]
PMID21493067C1d	DMFUQIT	Discovery agent	N.A.	Investigative	[31]
PMID24359159C19a	DM26JYS	Discovery agent	N.A.	Investigative	[32]
SGI-1252	DMZ20A5	Solid tumour/cancer	2A00-2F9Z	Investigative	[14]
WHI-P154	DMYHWS1	Diffuse large B-cell lymphoma	2A81	Investigative	[33]

References

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• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [3] 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
• [4] 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.
• [5] Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
• [6] Genetic determinants of response and survival in momelotinib-treated patients with myelofibrosis.Leukemia.2015 Mar;29(3):741-4.
• [7] CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms.Blood.2010 Jun 24;115(25):5232-40.
• [8] National Cancer Institute Drug Dictionary (drug id 609888).
• [9] The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumors. Cancer Cell. 2009 Dec 8;16(6):487-97.
• [10] Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2. Leukemia. 2012 Feb;26(2):280-8.
• [11] Company report (Portola Pharmaceuticals)
• [12] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [13] Clinical pipeline report, company report or official report of Concert Pharmaceuticals.
• [14] 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).
• [15] Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F. Blood Cancer J. 2013 Apr 12;3:e109.
• [16] Effect of NS-018, a selective JAK2V617F inhibitor, in a murine model of myelofibrosis. Blood Cancer J. 2014 Jan 10;4:e174.
• [17] Comparison of mutated ABL1 and JAK2 as oncogenes and drug targets in myeloproliferative disorders. Leukemia. 2008 Jul;22(7):1320-34.
• [18] SB1578, a novel inhibitor of JAK2, FLT3, and c-Fms for the treatment of rheumatoid arthritis. J Immunol. 2012 Oct 15;189(8):4123-34.
• [19] 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.
• [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] A STAT inhibitor patent review: progress since 2011.Expert Opin Ther Pat. 2015;25(12):1397-421.
• [22] Jak2 tyrosine kinase mediates oxidative stress-induced apoptosis in vascular smooth muscle cells. J Biol Chem. 2004 Aug 13;279(33):34547-52.
• [23] The JAK2 inhibitor AG490 predominantly abrogates the growth of human B-precursor leukemic cells with 11q23 translocation or Philadelphia chromosome. Leukemia. 2001 Nov;15(11):1758-68.
• [24] Identification of 1,2,3,4,5,6-hexabromocyclohexane as a small molecule inhibitor of jak2 tyrosine kinase autophosphorylation [correction of autophophorylation]. J Med Chem. 2005 Apr 7;48(7):2526-33.
• [25] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [26] Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole. J Med Chem. 2009 Dec 24;52(24):7938-41.
• [27] Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2. J Biol Chem. 2008 Nov 21;283(47):32334-43.
• [28] Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. Bioorg Med Chem Lett. 2002 Apr 22;12(8):1219-23.
• [29] In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.
• [30] A Non-ATP-Competitive Dual Inhibitor of JAK2 and BCR-ABL Kinases: Elucidation of a Novel Therapeutic Spectrum Based on Substrate Competitive Inhibition. Genes Cancer. 2010 Apr;1(4):331-45.
• [31] In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors. Bioorg Med Chem Lett. 2011 May 15;21(10):2958-61.
• [32] Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors. J Med Chem. 2014 Jan 9;57(1):144-58.
• [33] The specificity of JAK3 kinase inhibitors. Blood. 2008 Feb 15;111(4):2155-7.