Compound class:
Synthetic organic
Comment: DD-03-171 is a cereblon (CRBN)-engaging degrader (or PROTAC; proteolysis targeting chimera) of BTK protein [1]. The BTK inhibitor portion of DD-03-171 is derived from CGI1746, and this is conjugated to thalidomide using a saturated hydrocarbon linker to create the hybrid molecule. DD-03-171 produces potent antiproliferative effects on lymphoma cells in vitro and on patient-derived xenografts in vivo. It is suggested that DD-03-171's mechanism of action may be able to overcome tumour resistance to ibrutinib therapy.
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. Dobrovolsky D, Wang ES, Morrow S, Leahy C, Faust T, Nowak RP, Donovan KA, Yang G, Li Z, Fischer ES et al.. (2019)
Bruton tyrosine kinase degradation as a therapeutic strategy for cancer. Blood, 133 (9): 952-961. [PMID:30545835] |