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

General Information of Drug (ID: DMIUPSA)

• Drug Name: 1,2,4-triazolo[1,5a]pyridine derivative 1 Drug Info
• Synonyms: PMID27774824-Compound-Figure8compoundA
• Cross-matching ID: TTD Drug ID: DMIUPSA

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 Focal adhesion kinase 1 (FAK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
VS-6063	DMGBLI3	Mesothelioma	2C51.2	Phase 2	[11]
BI-853520	DMNOSYW	Solid tumour/cancer	2A00-2F9Z	Phase 1	[12]
PF-562271	DMSLE03	Solid tumour/cancer	2A00-2F9Z	Phase 1	[13]
VS-4718	DMN9JCD	Solid tumour/cancer	2A00-2F9Z	Phase 1	[14]
GSK-2256098	DMR24MI	Pulmonary arterial hypertension	BB01.0	Phase 1	[15]
CEP-37440	DMV632P	Solid tumour/cancer	2A00-2F9Z	Phase 1	[12]
IN10018	DMPXOVA	Metastatic melanoma	2E2Z	Phase 1	[16]
BMS-536924	DMXJB4N	Discovery agent	N.A.	Investigative	[17]
PF-228	DM32FKD	Discovery agent	N.A.	Investigative	[18]
PMID23414845C30	DMNVQ29	Discovery agent	N.A.	Investigative	[19]

Drug(s) Targeting Janus kinase 3 (JAK-3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tofacitinib	DMBS370	Rheumatoid arthritis	FA20	Approved	[20]
Ritlecitinib	DMYKNME	Alopecia areata	ED70.2	Approved	[21]
ASP-015K	DMZ1UOI	Psoriasis vulgaris	EA90	Phase 3	[22]
VX-509	DM2U3MX	Rheumatoid arthritis	FA20	Phase 2/3	[3]
Cerdulatinib	DMSCR2H	B-cell lymphoma	2A86	Phase 2	[21]
ATI-501	DMTY6OF	Alopecia	ED70	Phase 2	[23]
ATI-502	DM8NODR	Alopecia	ED70	Phase 2	[24]
TD-8236	DMTOMJN	Asthma	CA23	Phase 2	[25]
ALXN2075	DM1BSD8	Non-hodgkin lymphoma	2B33.5	Phase 1/2	[26]
SNA-125	DM8L1GJ	Atopic dermatitis	EA80	Phase 1	[21]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Focal adhesion kinase 1 (FAK)	TTON5IT	FAK1_HUMAN	Inhibitor	[1]
Janus kinase 2 (JAK-2)	TTRMX3V	JAK2_HUMAN	Inhibitor	[1]
Janus kinase 3 (JAK-3)	TTT7PJU	JAK3_HUMAN	Inhibitor	[1]

References

• [1] 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.
• [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] Role of focal adhesion kinase in regulating YB-1-mediated paclitaxel resistance in ovarian cancer. J Natl Cancer Inst. 2013 Oct 2;105(19):1485-95.
• [12] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [13] Inhibition of focal adhesion kinase by PF-562,271 inhibits the growth and metastasis of pancreatic cancer concomitant with altering the tumor microenvironment. Mol Cancer Ther. 2011 Nov;10(11):2135-45.
• [14] FAK Inhibition disrupts a beta5 integrin signaling axis controlling anchorage-independent ovarian carcinoma growth. Mol Cancer Ther. 2014 Aug;13(8):2050-61.
• [15] A small molecule FAK kinase inhibitor, GSK2256098, inhibits growth and survival of pancreatic ductal adenocarcinoma cells. Cell Cycle. 2014;13(19):3143-9.
• [16] Clinical pipeline report, company report or official report of InxMed.
• [17] 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.
• [18] Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem. 2007 May 18;282(20):14845-52.
• [19] Structure-based discovery of cellular-active allosteric inhibitors of FAK. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1779-85.
• [20] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [21] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [22] 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: 2049).
• [23] Clinical pipeline report, company report or official report of Aclaris Therapeutics.
• [24] ClinicalTrials.gov (NCT03759340) ATI-502 Topical Solution for the Treatment of Alopecia Areata (AA), Alopecia Universalis (AU) and Alopecia Totalis (AT). U.S. National Institutes of Health.
• [25] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight
• [26] 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.