DBPR112 is a potent EGFR inhibitor (IC50=487 nM) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. DBPR112), DBPR112
not only displayed a potent inhibitory activity against EGFRL858R/T790M double mutations but also exhibited tenfold potency better than the third-generation inhibitor, osimertinib,against EGFR and HER2 exon 20 insertion mutations. Overall, pharmacokinetic improvement through lead-to-candidate
optimization yielded fourfold oral AUC better that afatinib along with F = 41.5%, an encouraging safety profile, and significant antitumor efficacy in in vivo xenograft models.
UR-144, a synthetic cannabinoid, exhibits high affinity for the peripheral cannabinoid receptor (CB2) with a Ki of 1.8 nM, markedly greater than its affinity for the central cannabinoid receptor (CB1), for which it has a Ki of 150 nM. XLR-11 differs from UR-144 by featuring a fluorine atom on the terminal carbon of the alkyl chain and a methyl group on the C2 carbon of the indole. The specific biological activities of XLR-11 remain uncharacterized. It is designed for forensic and research use only.