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Compound class: Synthetic organic
Comment: HSP90B1 is involved in the regulation of a restricted number of proteins and represents a potential target in many diseases. In the reference for this entry 18c had IC50 of 220 nM, selectivity for HSP90B1 over other paralogs and biological activity in several cellular models of inflammation as well as cancer .
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. Patel HJ, Patel PD, Ochiana SO, Yan P, Sun W, Patel MR, Shah SK, Tramentozzi E, Brooks J, Bolaender A et al.. (2015)
Structure-activity relationship in a purine-scaffold compound series with selectivity for the endoplasmic reticulum Hsp90 paralog Grp94.
J Med Chem, 58 (9): 3922-43. [PMID:25901531]