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

General Information of Drug (ID: DMU2X59)

• Drug Name: PMID16539403C15b Drug Info
• Synonyms: GTPL8194; BDBM50184490

Indication

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

• Cross-matching ID:
  PubChem CID: 10361101
  TTD Drug ID: DMU2X59

Molecule-Related Drug Atlas

Drug(s) Targeting TGF-beta receptor type II (TGFBR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
TGF-BR2 mab	DMWBQ2Z	Solid tumour/cancer	2A00-2F9Z	Phase 1	[2]
PMID23639540C13d	DMSTQGH	Discovery agent	N.A.	Investigative	[3]
PMID23639540C13a	DMLXOAQ	Discovery agent	N.A.	Investigative	[3]
LY2109761	DMAWTG3	Discovery agent	N.A.	Investigative	[4]

Drug(s) Targeting TGF-beta receptor type I (TGFBR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LY2157299	DMP8HW1	Arteriosclerosis	BD40	Phase 2/3	[5]
TEW-7197	DM2LBC3	Myeloproliferative neoplasm	2A20	Phase 2	[6]
Metelimumab	DMENFD6	Scleroderma	4A42	Phase 1/2	[7]
TP-0184	DMJVZBC	Solid tumour/cancer	2A00-2F9Z	Phase 1	[8]
P-2745	DMJ3PNS	Chronic myelogenous leukaemia	2A20.0	Phase 1	[9]
LY3200882	DMQP6VB	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
PF-06952229	DMDQJEZ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[11]
SB-431542	DM0YOXQ	Pulmonary fibrosis	CB03.4	Preclinical	[12]
SM-16	DMHXJV2	Fibrosis	GA14-GC01	Terminated	[13]
LF-984	DMIYMS2	Fibrosis	GA14-GC01	Terminated	[14]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
MLK-related kinase (MLTK)	TTTUZ3O	M3K20_HUMAN	Inhibitor	[1]
TGF-beta receptor type I (TGFBR1)	TTP4520	TGFR1_HUMAN	Inhibitor	[1]
TGF-beta receptor type II (TGFBR2)	TTZE3P7	TGFR2_HUMAN	Inhibitor	[1]

References

• [1] Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity vers... J Med Chem. 2006 Mar 23;49(6):2138-42.
• [2] 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: 1795).
• [3] Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3248-52.
• [4] LY2109761, a novel transforming growth factor beta receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis. Mol Cancer Ther. 2008 Apr;7(4):829-40.
• [5] Cardiac Safety of TGF-beta Receptor I Kinase Inhibitor LY2157299 Monohydrate in Cancer Patients in a First-in-Human Dose Study. Cardiovasc Toxicol. 2015 Oct;15(4):309-23.
• [6] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [7] Development of TGF-beta signalling inhibitors for cancer therapy. Nat Rev Drug Discov. 2004 Dec;3(12):1011-22.
• [8] Clinical pipeline report, company report or official report of Sumitomo Dainippon Pharma.
• [9] Novel potent inhibitor of Bcr-Abl mutated imatinib resistant chronic myeloid leukemia cell lines. Cancer Research. 06/2012; 72(8 Supplement):1822-1822.
• [10] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [11] Targeting the TGF pathway for cancer therapy. Pharmacol Ther. 2015 Mar;147:22-31.
• [12] Pyrazolone based TGFbetaR1 kinase inhibitors. Bioorg Med Chem Lett. 2010 Jan 1;20(1):326-9.
• [13] TGF-beta type I receptor kinase inhibitor down-regulates rheumatoid synoviocytes and prevents the arthritis induced by type II collagen antibody. Int Immunol. 2007 Feb;19(2):117-26.
• [14] US patent application no. 2013,0028,978, Compositions and methods for wound treatment.