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Category Archives: Kinases
Discovery of PF-04691502 (PI3K/mTOR dual inhibitor)
Rapamycin and it’s analogues (or rapalogues e.g. CCI-779) modulate the phosphatidylinositol 3-kinase (PI3K) signalling cascade by binding to an allosteric site on the mTORC1 complex (Mammalian target of rapamycin (mTOR), a class IV PI3K protein kinase, forms two functional complexes, … Continue reading →
Posted in Clinical Candidates, Enzyme Inhibitors, Kinase Inhibitors, Kinases, Med Chem Strategy
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Tagged allosteric, cancer, CCI-779, dual inhibitor, H-bond, isostere, kinase, ligand efficiency, LipE, lipophilic efficiency, metabolism, mTOR, mTORC, PDB3ML8, PDB3ML9, PF-04691502, Pfizer, phosphatidylinositol 3-kinase, pI3K, rapalogues, rapamycin, solubility, Structure Based Design, X-ray data
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TAK-733 & CH4987655 (Allosteric MEK Inhibitors)
The mitogen-activated protein kinase (MAPK) signalling cascade is one of the key pathways regulating cell proliferation and differentiation and aberrant activation of this pathway is implicated in a number of cancers. Targeting components of the cascade thus has the potential … Continue reading →
Posted in Clinical Candidates, Enzyme Inhibitors, Kinase Inhibitors, Kinases
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Tagged allosteric, ARRY 142886, AZD-6244, cancer, CH4987655, Chugai, CNS penetration, hydroxamate, kinase, MAPK, MEK, metabolism, mTOR, PD0325901, Phase I, Phase II, RO4987655, Roche, Structure Based Design, TAK-733, Takeda, X-ray data
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Improved PK profile through fluorine and deuterium incorporation
Compound (1) was identified by scientists at Merck as a potent Aurora kinase inhibitor with the potential to be useful in the treatment of various cancers. In this paper the authors reveal that the basic amine which is key to good … Continue reading →
Posted in Kinase Inhibitors, Kinases
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Tagged amine basicity, animal PK, Aurora, cancer, cellular potency, Deuterium, fluorine, kinase, kinetic isotope effect, Merck, metabolism, X-ray data
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