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Compound class: Synthetic organic
Comment: Compound 18 is a type II DFG-out RIPK3 inhibitor . It was identified by a team in Bristol-Myers Squibb Research & Development laboratories.
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. Bryan MC, Rajapaksa NS. (2018)
Kinase Inhibitors for the Treatment of Immunological Disorders: Recent Advances.
J Med Chem, 61 (20): 9030-9058. [PMID:29870256]
2. Hart AC, Abell L, Guo J, Mertzman ME, Padmanabha R, Macor JE, Chaudhry C, Lu H, O'Malley K, Shaw PJ et al.. (2019)
Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage.
ACS Med Chem Lett, Article ASAP. DOI: 10.1021/acsmedchemlett.9b00065
3. Yan B, Liu L, Huang S, Ren Y, Wang H, Yao Z, Li L, Chen S, Wang X, Zhang Z. (2017)
Discovery of a new class of highly potent necroptosis inhibitors targeting the mixed lineage kinase domain-like protein.
Chem Commun (Camb.), 53 (26): 3637-3640. [PMID:28267172]