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

General Information of Drug (ID: DM70YTF)

Drug Name

HTS-466284 Drug Info

Synonyms

4-(3-Pyridin-2-YL-1H-pyrazol-4-YL)quinoline; 396129-53-6; LY-364947; LY364947; 4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)quinoline; 4-(3-PYRIDIN-2-YL-1H-PYRAZOL-4-YL)QUINOLINE; TbetaR-I Inhibitor; LY 364947; ALK5 Inhibitor I; TGF-beta RI Kinase Inhibitor; 4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]quinoline; CHEMBL261454; Transforming Growth Factor-beta Type I Receptor Kinase Inhibitor; 4-(3-pyridin-2-yl)(1h)-pyrazol-4-yl quinoline; 4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]quinoline; [3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole; 4-(3-Pyridin-2-Yl-1h-Pyrazol-4-Yl)Quinoline

Indication

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

Cross-matching ID

PubChem CID: 447966
ChEBI ID: CHEBI:91198
CAS Number: CAS 396129-53-6
TTD Drug ID: DM70YTF

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Preclinical Drug(s)

Discontinued 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	[2]
TEW-7197	DM2LBC3	Myeloproliferative neoplasm	2A20	Phase 2	[3]
Metelimumab	DMENFD6	Scleroderma	4A42	Phase 1/2	[4]
TP-0184	DMJVZBC	Solid tumour/cancer	2A00-2F9Z	Phase 1	[5]
P-2745	DMJ3PNS	Chronic myelogenous leukaemia	2A20.0	Phase 1	[6]
LY3200882	DMQP6VB	Solid tumour/cancer	2A00-2F9Z	Phase 1	[7]
PF-06952229	DMDQJEZ	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]
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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	[1]

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References

1	The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
2	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.
3	Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
4	Development of TGF-beta signalling inhibitors for cancer therapy. Nat Rev Drug Discov. 2004 Dec;3(12):1011-22.
5	Clinical pipeline report, company report or official report of Sumitomo Dainippon Pharma.
6	Novel potent inhibitor of Bcr-Abl mutated imatinib resistant chronic myeloid leukemia cell lines. Cancer Research. 06/2012; 72(8 Supplement):1822-1822.
7	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
8	Targeting the TGF pathway for cancer therapy. Pharmacol Ther. 2015 Mar;147:22-31.
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.