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Mizolastine (SL 850324) is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis) hives and other allergic reactions
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Azathioprine(BW 57-322) is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.
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RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM in cell-free assays RAF265 (CHIR-265) induces cell cycle arrest and apoptosis Phase 2
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CTEP (RO4956371) is a novel long-acting orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2 2 nM shows 1000-fold selectivity over other mGlu receptors
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Dabigatran Etexilate (BIBR-1048) is the prodrug of dabigatran a potent nonpeptidic small molecule that specifically and reversibly inhibits both free and clot-bound thrombin by binding to the active site of the thrombin molecule
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BAY-1436032 is a highly selective potent and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1) It is a double-digit nanomolar and selective pan-inhibitor of the enzymatic activity of various IDH1-R132X mutants in vitro and displays potent inhibition of 2-HG release (nanomolar range) in patient derived and engineered cell lines expressing different IDH1 mutants
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