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

General Information of Drug (ID: DM4G09S)

Drug Name

SB-505124 Drug Info

Synonyms

SB-505124; 694433-59-5; SB505124; SB 505124; 2-(4-(benzo[d][1,3]dioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl)-6-methylpyridine; CHEMBL226838; 2-[4-(1,3-Benzodioxol-5-yl)-2-(tert-butyl)-1H-imidazol-5-yl]-6-methylpyridine; 2-[5-(1,3-Benzodioxol-5-yl)-2-(1,1-dimethylethyl)-1H-imidazol-4-yl]-6-methylpyridine; 2-[4-(2H-1,3-benzodioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl]-6-methylpyridine; MLS006010969; SCHEMBL373422; GTPL6049; CTK8E3615; KS-00000XPS; EX-A217; DTXSID50431926; AOB1766; AOB5688; MolPort-021-804-897; CHEBI:100922

Indication

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

Cross-matching ID

PubChem CID: 9858940
ChEBI ID: CHEBI:100922
CAS Number: CAS 694433-59-5
TTD Drug ID: DM4G09S

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	[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]
PF-06952229	DMDQJEZ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[9]
SB-431542	DM0YOXQ	Pulmonary fibrosis	CB03.4	Preclinical	[10]
SM-16	DMHXJV2	Fibrosis	GA14-GC01	Terminated	[11]
LF-984	DMIYMS2	Fibrosis	GA14-GC01	Terminated	[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	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. (Ligand id: 6049).
2	Synthesis and biological evaluation of 2-pyridyl-substituted pyrazoles and imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors, Bioorg. Med. Chem. Lett. 20(14):4228-4232 (2010).
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	Targeting the TGF pathway for cancer therapy. Pharmacol Ther. 2015 Mar;147:22-31.
10	Pyrazolone based TGFbetaR1 kinase inhibitors. Bioorg Med Chem Lett. 2010 Jan 1;20(1):326-9.
11	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.
12	US patent application no. 2013,0028,978, Compositions and methods for wound treatment.