Drug General Information
Drug ID
D06TFI
Former ID
DNCL002630
Drug Name
LY2157299
Drug Type
Small molecular drug
Indication Arteriosclerosis [ICD9: 440; ICD10:I70] Phase 2/3 [524562], [542748]
Company
Eli Lilly
Structure
Download
2D MOL

3D MOL

Formula
C22H19N5O
InChI
InChI=1S/C22H19N5O/c1-13-4-2-5-18(25-13)21-20(19-6-3-11-27(19)26-21)15-9-10-24-17-8-7-14(22(23)28)12-16(15)17/h2,4-5,7-10,12H,3,6,11H2,1H3,(H2,23,28)
InChIKey
IVRXNBXKWIJUQB-UHFFFAOYSA-N
PubChem Compound ID
PubChem Substance ID
Target and Pathway
Target(s) TGF-beta receptor type I Target Info Modulator [533064]
KEGG Pathway MAPK signaling pathway
Cytokine-cytokine receptor interaction
FoxO signaling pathway
Endocytosis
TGF-beta signaling pathway
Osteoclast differentiation
Hippo signaling pathway
Adherens junction
Chagas disease (American trypanosomiasis)
Hepatitis B
HTLV-I infection
Pathways in cancer
Colorectal cancer
Pancreatic cancer
Chronic myeloid leukemia
PANTHER Pathway TGF-beta signaling pathway
Pathway Interaction Database Glypican 1 network
ALK1 signaling events
Beta5 beta6 beta7 and beta8 integrin cell surface interactions
TGF-beta receptor signaling
Reactome TGF-beta receptor signaling activates SMADs
TGF-beta receptor signaling in EMT (epithelial to mesenchymal transition)
SMAD2/3 Phosphorylation Motif Mutants in Cancer
SMAD2/3 MH2 Domain Mutants in Cancer
TGFBR2 Kinase Domain Mutants in Cancer
TGFBR1 KD Mutants in Cancer
TGFBR1 LBD Mutants in Cancer
WikiPathways TGF Beta Signaling Pathway
p38 MAPK Signaling Pathway
MAPK Signaling Pathway
TGF beta Signaling Pathway
Extracellular vesicle-mediated signaling in recipient cells
Cardiac Hypertrophic Response
Signaling by TGF-beta Receptor Complex
Integrated Pancreatic Cancer Pathway
Integrated Breast Cancer Pathway
References
Ref 524562ClinicalTrials.gov (NCT02008318) A Study of LY2157299 in Participants With Myelodysplastic Syndromes. U.S. National Institutes of Health.
Ref 542748(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: 7797).
Ref 533064Cardiac 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.

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