Synonyms: ASP-5878 | compound 27 [PMID: 35219181]
Compound class:
Synthetic organic
Comment: ASP5878 is an investigational, oral pan-FGFR inhibitor that was developed for potential to combat solid tumours [1-2].
Ligand Activity Visualisation ChartsThese 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. ✖ |
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References |
1. Kikuchi A, Suzuki T, Nakazawa T, Iizuka M, Nakayama A, Ozawa T, Kameda M, Shindoh N, Terasaka T, Hirano M et al.. (2017)
ASP5878, a selective FGFR inhibitor, to treat FGFR3-dependent urothelial cancer with or without chemoresistance. Cancer Sci, 108 (2): 236-242. [PMID:27885740] |
2. Kuriwaki I, Kameda M, Iikubo K, Hisamichi H, Kawamoto Y, Kikuchi S, Moritomo H, Terasaka T, Iwai Y, Noda A et al.. (2022)
Discovery of ASP5878: Synthesis and structure-activity relationships of pyrimidine derivatives as pan-FGFRs inhibitors with improved metabolic stability and suppressed hERG channel inhibitory activity. Bioorg Med Chem, 59: 116657. [PMID:35219181] |