Compound class:
Synthetic organic
Comment: This compound is a potent agonist of the stimulator of interferon genes (STING) protein, which is an intracellular detector/receptor of pathogen-derived and self DNA in the cytosol [2]. It was designed to be a systemically active immune-modifying anti-cancer therapeutic, with the potential to outperfom existing modified cyclic dinucleotide-based cGAMP (the endogenous STING agonist) development compounds, which are generally active by intratumoral delivery in a restricted range of accessible tumours. It is one of the chemical structures claimed in GlaxoSmithKline's patent WO2017175147A1 [1].
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. Charnley AK, Darcy MG, Dodson JW, Dong X, Hughes TV, Kang J, Leister LK, Lian Y, Li Y, Mehlmann JF et al.. (2017)
Heterocyclic amides useful as protein modulators. Patent number: WO2017175147A1. Assignee: Glaxosmithkline Intellectual Property Development Limited. Priority date: 07/04/2016. Publication date: 12/10/2017. |
2. Ramanjulu JM, Pesiridis GS, Yang J, Concha N, Singhaus R, Zhang SY, Tran JL, Moore P, Lehmann S, Eberl HC et al.. (2018)
Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature, 564 (7736): 439-443. [PMID:30405246] |