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

General Information of Drug (ID: DMHBZ0N)

• Drug Name: PMID23639540C13r Drug Info
• Synonyms: GTPL8144; BDBM50434750

Indication

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

• Cross-matching ID:
  PubChem CID: 60182364
  TTD Drug ID: DMHBZ0N

Molecule-Related Drug Atlas

Drug(s) Targeting Activin receptor-like kinase 2 (ALK-2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
INCB00928	DMFG8TI	Anemia	3A00-3A9Z	Phase 2	[2]
TP-0184	DMJVZBC	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
PMID27774822-Compound-Figure10Compound12	DMFAGOZ	N. A.	N. A.	Patented	[4]
PMID27774822-Compound-Figure10Compound4	DMMJVTW	N. A.	N. A.	Patented	[4]
PMID23639540C13d	DMSTQGH	Discovery agent	N.A.	Investigative	[1]
PMID23639540C13a	DMLXOAQ	Discovery agent	N.A.	Investigative	[1]
LDN-214117	DM57Z8J	Discovery agent	N.A.	Investigative	[5]
ML347	DMR8N36	Discovery agent	N.A.	Investigative	[1]

Drug(s) Targeting Activin receptor-like kinase-1 (ACVRL1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PF-03446962	DMTJWNE	Solid tumour/cancer	2A00-2F9Z	Phase 2	[6]
PMID23639540C13d	DMSTQGH	Discovery agent	N.A.	Investigative	[1]
PMID23639540C13a	DMLXOAQ	Discovery agent	N.A.	Investigative	[1]
LDN-214117	DM57Z8J	Discovery agent	N.A.	Investigative	[5]
ML347	DMR8N36	Discovery agent	N.A.	Investigative	[1]

Drug(s) Targeting Activin receptor type IB (ACVR1B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
US9682983, 1	DM6EQVT	N. A.	N. A.	Patented	[7]
BDBM108945	DMZD6IJ	N. A.	N. A.	Patented	[7]
US10030004, Compound 19	DM0RAPC	N. A.	N. A.	Patented	[8]
US9682983, 33	DM6R1YP	N. A.	N. A.	Patented	[7]
US10030004, Compound 33	DMD0GN6	N. A.	N. A.	Patented	[8]
US10030004, Compound 11a	DMG4T13	N. A.	N. A.	Patented	[8]
PMID23639540C13d	DMSTQGH	Discovery agent	N.A.	Investigative	[1]

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	[9]
TEW-7197	DM2LBC3	Myeloproliferative neoplasm	2A20	Phase 2	[10]
Metelimumab	DMENFD6	Scleroderma	4A42	Phase 1/2	[11]
TP-0184	DMJVZBC	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
P-2745	DMJ3PNS	Chronic myelogenous leukaemia	2A20.0	Phase 1	[12]
LY3200882	DMQP6VB	Solid tumour/cancer	2A00-2F9Z	Phase 1	[13]
PF-06952229	DMDQJEZ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[14]
SB-431542	DM0YOXQ	Pulmonary fibrosis	CB03.4	Preclinical	[15]
SM-16	DMHXJV2	Fibrosis	GA14-GC01	Terminated	[16]
LF-984	DMIYMS2	Fibrosis	GA14-GC01	Terminated	[17]

Drug(s) Targeting Bone morphogenetic protein receptor (BMPR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID23639540C13d	DMSTQGH	Discovery agent	N.A.	Investigative	[1]
PMID23639540C13a	DMLXOAQ	Discovery agent	N.A.	Investigative	[1]
LDN-214117	DM57Z8J	Discovery agent	N.A.	Investigative	[5]
ML347	DMR8N36	Discovery agent	N.A.	Investigative	[1]
AA-184	DMCN4ZD	Kidney injury	NB92.0	Investigative	[18]
AA-204	DMBGTX9	Kidney disease	GC2Z	Investigative	[18]
AA-123	DMW73A8	Prostate cancer	2C82.0	Investigative	[18]
AA-166	DM2BMAZ	Articular cartilage disorder	FA34.Y	Investigative	[18]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Activin receptor type IB (ACVR1B)	TTPKHTZ	ACV1B_HUMAN	Inhibitor	[1]
Activin receptor-like kinase 2 (ALK-2)	TTJNBQA	ACVR1_HUMAN	Inhibitor	[1]
Activin receptor-like kinase-1 (ACVRL1)	TTGYPTC	ACVL1_HUMAN	Inhibitor	[1]
Bone morphogenetic protein receptor (BMPR2)	TTGKF90	BMPR2_HUMAN	Inhibitor	[1]
TGF-beta receptor type I (TGFBR1)	TTP4520	TGFR1_HUMAN	Inhibitor	[1]

References

• [1] 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.
• [2] Clinical pipeline report, company report or official report of Incyte.
• [3] Clinical pipeline report, company report or official report of Sumitomo Dainippon Pharma.
• [4] 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.
• [5] Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. J Med Chem. 2014 Oct 9;57(19):7900-15.
• [6] ALK1 as an emerging target for antiangiogenic therapy of cancer. Blood. 2011 June 30; 117(26): 6999-7006.
• [7] BMP inhibitors and methods of use thereof. US9682983.
• [8] Compounds and methods of use. US10030004.
• [9] 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.
• [10] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [11] Development of TGF-beta signalling inhibitors for cancer therapy. Nat Rev Drug Discov. 2004 Dec;3(12):1011-22.
• [12] Novel potent inhibitor of Bcr-Abl mutated imatinib resistant chronic myeloid leukemia cell lines. Cancer Research. 06/2012; 72(8 Supplement):1822-1822.
• [13] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [14] Targeting the TGF pathway for cancer therapy. Pharmacol Ther. 2015 Mar;147:22-31.
• [15] Pyrazolone based TGFbetaR1 kinase inhibitors. Bioorg Med Chem Lett. 2010 Jan 1;20(1):326-9.
• [16] 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.
• [17] US patent application no. 2013,0028,978, Compositions and methods for wound treatment.
• [18] 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: 1794).