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Bristol Myers Squibb RET compound 39: sourced facts only. name: "LDD 39 demonstrated high in vitro inhibitory and degradation potency against both RET wild-type and the two representative mutants, V804M and G810R." [PMID:39437163]; target: "LDD 39 demonstrated high in vitro inhibitory and degradation potency against both RET wild-type and the two representative mutants, V804M and G810R." [PMID:39437163]; developer: "Discovery Chemistry, Bristol Myers Squibb, Princeton, New Jersey 08540, United States." [PMID:39437163]; modality: "We describe the design, synthesis, and structure-activity relationship (SAR) of heterobifunctional RET ligand-directed degraders (LDDs) derived from three different second-generation RET inhibitors." [PMID:39437163]; stage: "Robust and sustained degradation of total-RET (tRET) protein and inhibition of phospho-RET (pRET) signaling were observed in TPC-1 xenograft tumors driven by RET and the RET/G810R mutant following a single dose of LDD 39 at 15 and 75 mg/kg, respectively." [PMID:39437163]
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