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Synonyms: inhibitor 15d [PMID: 18314943] | LY-2157299 | LY2157299
Compound class: Synthetic organic
Comment: Galunisertib is a first-in-class investigational inhibitor of the receptor tyrosine kinase, growth factor-β receptor type I (TGFβRI) [1-2]. It is being evaluated as a novel anticancer agent.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Li HY, McMillen WT, Heap CR, McCann DJ, Yan L, Campbell RM, Mundla SR, King CH, Dierks EA, Anderson BD et al.. (2008)
Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent.
J. Med. Chem., 51 (7): 2302-6. [PMID:18314943]
2. Yingling JM, McMillen WT, Yan L, Huang H, Sawyer JS, Graff J, Clawson DK, Britt KS, Anderson BD, Beight DW et al.. (2018)
Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor.
Oncotarget, 9 (6): 6659-6677. [PMID:29467918]