ChemicalBook >?? ???? >GSK2982772
GSK2982772
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GSK2982772 ??
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- 1.40±0.1 g/cm3(Predicted)
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- -20°C
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- DMSO? ???(>25mg/ml)
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- ?? ?? (pKa)
- 8.80±0.40(Predicted)
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- ??? ?? ?????? 2? ?? ??????. DMSO? ???? -20°C?? ?? 1?? ?? ??? ? ????.
- InChIKey
- LYPAFUINURXJSG-AWEZNQCLSA-N
- SMILES
- N1C(C(N[C@@H]2C(=O)N(C)C3=CC=CC=C3OC2)=O)=NC(CC2=CC=CC=C2)=N1
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GSK2982772 C??? ??, ??, ??
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(S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide, also known as GSK2982772, is a first-in-class receptor interacting protein 1(RIP1)-kinase specific clinical candidate for the treatment of inflammatory disease. It is an inhibitor of RIP1 that regulates necroptosis and inflammation and may play an important role in contributing to a variety of human pathologies, including immune-mediated inflammatory diseases. It has excellent activity in blocking many TNF-dependent cellular responses. Highlighting its potential as a novel anti-inflammatory agent, the inhibitor was also able to reduce spontaneous production of cytokines from human ulcerative colitis explants.?? ??
Harris, P. A., et al. "Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases." Journal of Medicinal Chemistry 60.4(2017):1247-1261.Jeong, Jae Uk, et al. "Synthesis of ( S )-3-amino-benzo[ b ][1,4]oxazepin-4-one via Mitsunobu and S N Ar reaction for a first-in-class RIP1 kinase inhibitor GSK2982772 in clinical trials." Tetrahedron Letters 58.23(2017):2306-2308.
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