1NC6
 
 | | Potent, small molecule inhibitors of human mast cell tryptase. Anti-asthmatic action of a dipeptide-based transition state analogue containing benzothiazole ketone | | 分子名称: | (2S,4R)-1-ACETYL-N-[(1S)-4-[(AMINOIMINOMETHYL)AMINO]-1-(2-BENZOTHIAZOLYLCARBONYL)BUTYL]-4-HYDROXY-2-PYRROLIDINECARBOXAMIDE, CALCIUM ION, SULFATE ION, ... | | 著者 | Costanzo, M.J, Yabut, S.C, Almond Jr, H.R, Andrade-Gordon, P, Corcoran, T.W, de Garavilla, L, Kauffman, J.A, Abraham, W.M, Recacha, R, Chattopadhyay, D, Maryanoff, B.E. | | 登録日 | 2002-12-04 | | 公開日 | 2003-09-23 | | 最終更新日 | 2024-10-23 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Potent, Small-Molecule Inhibitors of Human Mast Cell Tryptase. Antiasthmatic Action of a Dipeptide-Based Transition-State Analogue Containing a Benzothiazole Ketone.
J.Med.Chem., 46, 2003
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2ZA5
 | | Crystal Structure of human tryptase with potent non-peptide inhibitor | | 分子名称: | (5-(aminomethyl)-2H-spiro[benzofuran-3,4'-piperidine]-1'-yl)(5-(phenylethynyl)furan-2-yl)methanone, Tryptase beta 2 | | 著者 | Spurlino, J.C, Barnakov, S.A, Lewandowski, F, Milligan, C. | | 登録日 | 2007-10-02 | | 公開日 | 2008-02-26 | | 最終更新日 | 2024-10-30 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Potent, nonpeptide inhibitors of human mast cell tryptase. Synthesis and biological evaluation of novel spirocyclic piperidine amide derivatives
Bioorg.Med.Chem.Lett., 18, 2008
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3KXO
 | | An orally active inhibitor bound at the active site of HPGDS | | 分子名称: | 6-(3-fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide, GLUTATHIONE, Glutathione-requiring prostaglandin D synthase, ... | | 著者 | Kiefer, J.R, Day, J.E, Thorarensen, A. | | 登録日 | 2009-12-03 | | 公開日 | 2010-09-01 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Discovery of an oral potent selective inhibitor of hematopoietic prostaglandin D synthase
TO BE PUBLISHED
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2ZEB
 | | Potent, Nonpeptide Inhibitors of Human Mast Cell Tryptase | | 分子名称: | 1-(1'-{[3-(methylsulfanyl)-2-benzothiophen-1-yl]carbonyl}spiro[1-benzofuran-3,4'-piperidin]-5-yl)methanamine, Tryptase beta 2 | | 著者 | Spurlino, J.C, Lewandowski, F, Milligan, C. | | 登録日 | 2007-12-08 | | 公開日 | 2008-12-09 | | 最終更新日 | 2024-11-06 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Potent, nonpeptide inhibitors of human mast cell tryptase. Synthesis and biological evaluation of novel spirocyclic piperidine amide derivatives
Bioorg.Med.Chem.Lett., 18, 2008
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2ZEC
 | | Potent, Nonpeptide Inhibitors of Human Mast Cell Tryptase | | 分子名称: | 1-[1'-(3-phenylacryloyl)spiro[1-benzofuran-3,4'-piperidin]-5-yl]methanamine, Tryptase beta 2 | | 著者 | Spurlino, J.C, Lewandowski, F, Milligan, C. | | 登録日 | 2007-12-08 | | 公開日 | 2008-12-09 | | 最終更新日 | 2024-10-30 | | 実験手法 | X-RAY DIFFRACTION (2.059 Å) | | 主引用文献 | Potent, nonpeptide inhibitors of human mast cell tryptase. Synthesis and biological evaluation of novel spirocyclic piperidine amide derivatives
Bioorg.Med.Chem.Lett., 18, 2008
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1T32
 | | A Dual Inhibitor of the Leukocyte Proteases Cathepsin G and Chymase with Therapeutic Efficacy in Animals Models of Inflammation | | 分子名称: | 2-[3-({METHYL[1-(2-NAPHTHOYL)PIPERIDIN-4-YL]AMINO}CARBONYL)-2-NAPHTHYL]-1-(1-NAPHTHYL)-2-OXOETHYLPHOSPHONIC ACID, Cathepsin G, SULFATE ION | | 著者 | de Garavilla, L, Greco, M.N, Giardino, E.C, Wells, G.I, Haertlein, B.J, Kauffman, J.A, Corcoran, T.W, Derian, C.K, Eckardt, A.J, Abraham, W.M, Sukumar, N, Chen, Z, Pineda, A.O, Mathews, F.S, Di Cera, E, Andrade-Gordon, P, Damiano, B.P, Maryanoff, B.E. | | 登録日 | 2004-04-23 | | 公開日 | 2005-03-01 | | 最終更新日 | 2023-08-23 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | A novel, potent dual inhibitor of the leukocyte proteases cathepsin G and chymase: molecular mechanisms and anti-inflammatory activity in vivo.
J.Biol.Chem., 280, 2005
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1T31
 | | A Dual Inhibitor of the Leukocyte Proteases Cathepsin G and Chymase with Therapeutic Efficacy in Animals Models of Inflammation | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 2-[3-({METHYL[1-(2-NAPHTHOYL)PIPERIDIN-4-YL]AMINO}CARBONYL)-2-NAPHTHYL]-1-(1-NAPHTHYL)-2-OXOETHYLPHOSPHONIC ACID, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | de Garavilla, L, Greco, M.N, Giardino, E.C, Wells, G.I, Haertlein, B.J, Kauffman, J.A, Corcoran, T.W, Derian, C.K, Eckardt, A.J, Abraham, W.M, Sukumar, N, Chen, Z, Pineda, A.O, Mathews, F.S, Di Cera, E, Andrade-Gordon, P, Damiano, B.P, Maryanoff, B.E, Pereira, P.J.B, Wang, Z.M, Rubin, H, Huber, R, Bode, W, Schechter, N.M, Strobl, S. | | 登録日 | 2004-04-23 | | 公開日 | 2005-03-01 | | 最終更新日 | 2024-10-30 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | A novel, potent dual inhibitor of the leukocyte proteases cathepsin G and chymase: molecular mechanisms and anti-inflammatory activity in vivo.
J.Biol.Chem., 280, 2005
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