2cji
From Proteopedia
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CRYSTAL STRUCTURE OF A HUMAN FACTOR XA INHIBITOR COMPLEX
Overview
A series of novel, non-basic, 3-(6-chloronaphth-2-ylsulfonyl)aminopyrrolidin-2-one-based factor Xa (fXa), inhibitors, incorporating an alanylamide P4 group, was designed and, synthesised. Within this series, the N-2-(morpholin-4-yl)-2-oxoethyl, derivative 24 was shown to be a potent, selective fXa inhibitor with good, anticoagulant activity. Moreover, 24 possessed highly encouraging rat and, dog pharmacokinetic profiles with excellent oral bioavailabilities in both, species.
About this Structure
2CJI is a [Single protein] structure of sequence from [Homo sapiens] with CA and GSK as [ligands]. Active as [[1]], with EC number [3.4.21.6]. Full crystallographic information is available from [OCA].
Reference
Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors., Watson NS, Brown D, Campbell M, Chan C, Chaudry L, Convery MA, Fenwick R, Hamblin JN, Haslam C, Kelly HA, King NP, Kurtis CL, Leach AR, Manchee GR, Mason AM, Mitchell C, Patel C, Patel VK, Senger S, Shah GP, Weston HE, Whitworth C, Young RJ, Bioorg Med Chem Lett. 2006 Jul 15;16(14):3784-8. Epub 2006 May 11. PMID:16697194
Page seeded by OCA on Mon Oct 29 21:00:48 2007
Categories: Homo sapiens | Single protein | Campbell, M. | Chan, C. | Convery, M.A. | Hamblin, J.N. | Kelly, H.A. | King, N.P. | Mason, A.M. | Mitchell, C. | Patel, V.K. | Senger, S. | Shah, G.P. | Watson, N.S. | Weston, H.E. | Whitworth, C. | Young, R.J. | CA | GSK | Blood coagulation | Calcium | Egf-like domain | Gamma-carboxyglutamic acid | Glycoprotein | Hydrolase | Hydroxylation | Polymorphism | Protease | Serine protease | Zymogen
