Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T27602 | ||||
Target Name | Trypsin | ||||
Target Type | Clinical Trial |
||||
Drug Potency against Target | 4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine | Drug Info | Ki = 580 nM | [527397] | |
CVS-2139 | Drug Info | Ki = 20.8 nM | [526306] | ||
2-(2-Iodo-phenyl)-benzo[d][1,3]oxazin-4-one | Drug Info | IC50 = 15300 nM | [534598] | ||
Piperidine-1-carboxamidine | Drug Info | Ki = 360 nM | [525858] | ||
L-375378 | Drug Info | Ki = 1800 nM | [526487] | ||
RWJ-56423 | Drug Info | Ki = 8.1 nM | [526956] | ||
4-Indol-1-ylmethyl-benzamidine | Drug Info | Ki = 4590 nM | [533527] | ||
Macrocyclic tripeptide motif | Drug Info | Ki = 1 nM | |||
GRASSYSTATIN A | Drug Info | IC50 = 10000 nM | [530345] | ||
6-Styryl-naphthalene-2-carboxamidine | Drug Info | Ki = 346 nM | [527320] | ||
1,3-Dibenzyl-[1,3]diazetidine-2,4-dione | Drug Info | IC50 = 39 nM | [526092] | ||
2-Propionyl-1H-indole-6-carboxamidine | Drug Info | Ki = 15300 nM | [533527] | ||
1,3-Di-p-tolyl-[1,3]diazetidine-2,4-dione | Drug Info | IC50 = 200 nM | [526092] | ||
8-Bromo-6-styryl-naphthalene-2-carboxamidine | Drug Info | Ki = 480 nM | [527320] | ||
8-Furan-3-yl-6-styryl-naphthalene-2-carboxamidine | Drug Info | Ki = 96 nM | [527320] | ||
BMY-44621 | Drug Info | IC50 = 7200 nM | |||
L-370,518 | Drug Info | Ki = 11000 nM | |||
CI-1031 | Drug Info | Ki = 280 nM | [534797] | ||
1-Benzyl-1H-indole-5-carboxamidine | Drug Info | Ki = 15400 nM | [533527] | ||
4-(5-Nitro-indol-1-ylmethyl)-benzamidine | Drug Info | Ki = 3440 nM | [533527] | ||
1-(3-Amino-benzyl)-1H-indole-5-carboxamidine | Drug Info | Ki = 16800 nM | [533527] | ||
4-(3,4-Diethoxy-benzylamino)-benzamidine | Drug Info | Ki = 2000 nM | [527397] | ||
CVS-2359 | Drug Info | Ki = 12.4 nM | [526306] | ||
2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine | Drug Info | Ki = 8000 nM | [526118] | ||
INOGATRAN | Drug Info | Ki = 675 nM | [534831] | ||
1-(3-Nitro-benzyl)-1H-indole-5-carboxamidine | Drug Info | Ki = 7770 nM | [533527] | ||
RWJ-50353 | Drug Info | Ki = 3.1 nM | [527480] | ||
MELAGATRAN | Drug Info | IC50 = 11.9 nM | [528066] | ||
Tert-butyloxy carbonyl-D-Phe-pro-Arg-H | Drug Info | IC50 = 14 nM | [533588] | ||
GR-133686 | Drug Info | IC50 = 70 nM | [534803] | ||
References | |||||
Ref 527397 | Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors. | ||||
Ref 526306 | Bioorg Med Chem Lett. 2002 Apr 22;12(8):1203-8.Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates. | ||||
Ref 534598 | J Med Chem. 1998 Mar 26;41(7):1060-7.2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease. | ||||
Ref 525858 | J Med Chem. 2000 Aug 10;43(16):3033-44.GRID/CPCA: a new computational tool to design selective ligands. | ||||
Ref 526487 | Bioorg Med Chem Lett. 2003 Jan 20;13(2):161-4.Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'. | ||||
Ref 526956 | J Med Chem. 2004 Feb 12;47(4):769-87.Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G. | ||||
Ref 533527 | J Med Chem. 1983 Feb;26(2):294-8.Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin. | ||||
Ref 530345 | J Med Chem. 2009 Sep 24;52(18):5732-47.Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. | ||||
Ref 527320 | Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8.Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties. | ||||
Ref 526092 | Bioorg Med Chem Lett. 2001 Jul 9;11(13):1691-4.Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones. | ||||
Ref 533527 | J Med Chem. 1983 Feb;26(2):294-8.Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin. | ||||
Ref 526092 | Bioorg Med Chem Lett. 2001 Jul 9;11(13):1691-4.Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones. | ||||
Ref 527320 | Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8.Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties. | ||||
Ref 527320 | Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8.Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties. | ||||
Ref 534797 | Bioorg Med Chem Lett. 1998 Aug 18;8(16):2235-40.Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors. | ||||
Ref 533527 | J Med Chem. 1983 Feb;26(2):294-8.Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin. | ||||
Ref 533527 | J Med Chem. 1983 Feb;26(2):294-8.Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin. | ||||
Ref 533527 | J Med Chem. 1983 Feb;26(2):294-8.Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin. | ||||
Ref 527397 | Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors. | ||||
Ref 526306 | Bioorg Med Chem Lett. 2002 Apr 22;12(8):1203-8.Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates. | ||||
Ref 526118 | J Med Chem. 2001 Aug 16;44(17):2753-71.Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa. | ||||
Ref 534831 | Bioorg Med Chem Lett. 1998 Dec 15;8(24):3603-8.Novel acylguanidine containing thrombin inhibitors with reduced basicity at the P1 moiety. | ||||
Ref 533527 | J Med Chem. 1983 Feb;26(2):294-8.Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin. | ||||
Ref 527480 | J Med Chem. 2005 Mar 24;48(6):1984-2008.In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design. | ||||
Ref 528066 | Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7. Epub 2006 Mar 6.Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. | ||||
Ref 533588 | J Med Chem. 1995 Oct 27;38(22):4446-53.Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions. | ||||
Ref 534803 | Bioorg Med Chem Lett. 1998 Nov 3;8(21):2955-60.5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor. |
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