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

General Information of Drug (ID: DMDQJEZ)

Drug Name

PF-06952229 Drug Info

Synonyms

SCHEMBL16879380; BDBM280355; US10030004, Compound 22; NSC826119; NSC-826119; HY-136244; CS-0120989; PF06952229; ClC=1C=CC(=C(C1)C1=NC=C(C(=C1)NC1=CC=NC=C1C(=O)NC(CO)CO)C(C)C)F; 1801333-55-0; Synthesis of 4-[[2-(5-chloro-2-fluoro-phenyl)-5-isopropyl-4-pyridyl]amino]-N-[2-hydroxy-1-(hydroxymethyl)ethyl]pyridine-3-carboxamide

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]

Cross-matching ID

PubChem CID: 118211239
TTD Drug ID: DMDQJEZ

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Preclinical Drug(s)

Discontinued Drug(s)

Investigative Drug(s)

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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	[3]
TEW-7197	DM2LBC3	Myeloproliferative neoplasm	2A20	Phase 2	[4]
Metelimumab	DMENFD6	Scleroderma	4A42	Phase 1/2	[5]
TP-0184	DMJVZBC	Solid tumour/cancer	2A00-2F9Z	Phase 1	[6]
P-2745	DMJ3PNS	Chronic myelogenous leukaemia	2A20.0	Phase 1	[7]
LY3200882	DMQP6VB	Solid tumour/cancer	2A00-2F9Z	Phase 1	[8]
SB-431542	DM0YOXQ	Pulmonary fibrosis	CB03.4	Preclinical	[9]
SM-16	DMHXJV2	Fibrosis	GA14-GC01	Terminated	[10]
LF-984	DMIYMS2	Fibrosis	GA14-GC01	Terminated	[11]
PMID23639540C13d	DMSTQGH	Discovery agent	N.A.	Investigative	[12]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
TGF-beta receptor type I (TGFBR1)	TTP4520	TGFR1_HUMAN	Inhibitor	[2]

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References

1	ClinicalTrials.gov (NCT03685591) PF-06952229 Treatment in Adult Patients With Advanced Solid Tumors. U.S. National Institutes of Health.
2	Targeting the TGF pathway for cancer therapy. Pharmacol Ther. 2015 Mar;147:22-31.
3	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.
4	Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
5	Development of TGF-beta signalling inhibitors for cancer therapy. Nat Rev Drug Discov. 2004 Dec;3(12):1011-22.
6	Clinical pipeline report, company report or official report of Sumitomo Dainippon Pharma.
7	Novel potent inhibitor of Bcr-Abl mutated imatinib resistant chronic myeloid leukemia cell lines. Cancer Research. 06/2012; 72(8 Supplement):1822-1822.
8	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
9	Pyrazolone based TGFbetaR1 kinase inhibitors. Bioorg Med Chem Lett. 2010 Jan 1;20(1):326-9.
10	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.
11	US patent application no. 2013,0028,978, Compositions and methods for wound treatment.
12	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.