| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T73992 | ||||
| Target Name | Beta-secretase | ||||
| Target Type | Clinical Trial |
||||
| Drug Potency against Target | GRL-7234 | Drug Info | IC50 = 39 nM | [528786] | |
| KUSHENOL A | Drug Info | IC50 = 2600 nM | [529543] | ||
| OM00-3 | Drug Info | IC50 = 6 nM | [528788] | ||
| KURARINONE | Drug Info | IC50 = 3300 nM | [529543] | ||
| (2S)-2'-methoxy kurarinone | Drug Info | IC50 = 6700 nM | [529543] | ||
| Glu-Leu-Asp-Leu-(CHOH-CH2)-Ala-Ala-Glu-Phe | Drug Info | Ki = 0.3 nM | [527272] | ||
| (-)-CATECHINGALLATE | Drug Info | IC50 = 6000 nM | [526870] | ||
| GSK-188909 | Drug Info | IC50 = 30 nM | [530119] | ||
| DIOXINODEHYDROECKOL | Drug Info | IC50 = 5350 nM | [530909] | ||
| LEACHIANONE A | Drug Info | IC50 = 8400 nM | [529543] | ||
| TRIPHLOROETHOL A | Drug Info | IC50 = 11680 nM | [530909] | ||
| DIECKOL | Drug Info | IC50 = 2210 nM | [530909] | ||
| AP-2243 | Drug Info | IC50 = 238 nM | [529149] | ||
| Bis-7-tacrine | Drug Info | IC50 = 7500 nM | [530301] | ||
| CTS-21166 | Drug Info | IC50 = 0.12~20 nM/L | [552839] | ||
| PHLOROFUCOFUROECKOL A | Drug Info | IC50 = 2130 nM | [530909] | ||
| 5,5-Diphenyl-2-iminohydantoin | Drug Info | IC50 = 12000 nM | [530611] | ||
| Carbocyclic Peptidomimetic | Drug Info | IC50 = 16 nM | [527675] | ||
| Eckol | Drug Info | IC50 = 12200 nM | [530909] | ||
| 7-Phloroethol | Drug Info | IC50 = 8590 nM | [530909] | ||
| Action against Disease Model | CTS-21166 | CTS-21166 has cellular activity of IC50 = 1.2-3.6 nM, reduced brain A|??levels by over 35% and plaque load by 40%. | [553062] | Drug Info | |
| The Effect of Target Knockout, Knockdown or Genetic Variations | secretase knockout mice are de?cient in Abetat production;the knockout mice are normal in terms of gross morphology and anatomy,tissue histology, hematology and clinical chemistry | [528786] | |||
| References | |||||
| Ref 528786 | J Med Chem. 2007 May 17;50(10):2399-407. Epub 2007 Apr 14.Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands. | ||||
| Ref 529543 | Bioorg Med Chem. 2008 Jul 15;16(14):6669-74. Epub 2008 Jun 5.BACE1 inhibitory effects of lavandulyl flavanones from Sophora flavescens. | ||||
| Ref 528788 | Bioorg Med Chem. 2007 Jun 15;15(12):4136-43. Epub 2007 Mar 30.Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1). | ||||
| Ref 529543 | Bioorg Med Chem. 2008 Jul 15;16(14):6669-74. Epub 2008 Jun 5.BACE1 inhibitory effects of lavandulyl flavanones from Sophora flavescens. | ||||
| Ref 529543 | Bioorg Med Chem. 2008 Jul 15;16(14):6669-74. Epub 2008 Jun 5.BACE1 inhibitory effects of lavandulyl flavanones from Sophora flavescens. | ||||
| Ref 527272 | J Med Chem. 2004 Nov 4;47(23):5791-7.Efficient evaluation of binding free energy using continuum electrostatics solvation. | ||||
| Ref 526870 | Bioorg Med Chem Lett. 2003 Nov 17;13(22):3905-8.Green tea catechins as a BACE1 (beta-secretase) inhibitor. | ||||
| Ref 530119 | Bioorg Med Chem Lett. 2009 Jul 1;19(13):3664-8. Epub 2009 Apr 17.Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics. | ||||
| Ref 530909 | Bioorg Med Chem Lett. 2010 Jun 1;20(11):3211-5. Epub 2010 Apr 24.Molecular docking studies of phlorotannins from Eisenia bicyclis with BACE1 inhibitory activity. | ||||
| Ref 529543 | Bioorg Med Chem. 2008 Jul 15;16(14):6669-74. Epub 2008 Jun 5.BACE1 inhibitory effects of lavandulyl flavanones from Sophora flavescens. | ||||
| Ref 530909 | Bioorg Med Chem Lett. 2010 Jun 1;20(11):3211-5. Epub 2010 Apr 24.Molecular docking studies of phlorotannins from Eisenia bicyclis with BACE1 inhibitory activity. | ||||
| Ref 530909 | Bioorg Med Chem Lett. 2010 Jun 1;20(11):3211-5. Epub 2010 Apr 24.Molecular docking studies of phlorotannins from Eisenia bicyclis with BACE1 inhibitory activity. | ||||
| Ref 529149 | Bioorg Med Chem Lett. 2008 Jan 1;18(1):423-6. Epub 2007 Oct 4.Multi-target-directed coumarin derivatives: hAChE and BACE1 inhibitors as potential anti-Alzheimer compounds. | ||||
| Ref 530301 | J Med Chem. 2009 Sep 10;52(17):5365-79.Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds. | ||||
| Ref 552839 | beta-Secretase as a therapeutic target for Alzheimer's disease. Neurotherapeutics. 2008 Jul;5(3):399-408. doi: 10.1016/j.nurt.2008.05.007. | ||||
| Ref 530909 | Bioorg Med Chem Lett. 2010 Jun 1;20(11):3211-5. Epub 2010 Apr 24.Molecular docking studies of phlorotannins from Eisenia bicyclis with BACE1 inhibitory activity. | ||||
| Ref 553062 | Inhibition of BACE1 for therapeutic use in Alzheimer's disease. Int J Clin Exp Pathol. 2010 Jul 8;3(6):618-28. | ||||
| Ref 530611 | J Med Chem. 2010 Feb 11;53(3):951-65.Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation. | ||||
| Ref 527675 | J Med Chem. 2005 Aug 11;48(16):5175-90.Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics. | ||||
| Ref 530909 | Bioorg Med Chem Lett. 2010 Jun 1;20(11):3211-5. Epub 2010 Apr 24.Molecular docking studies of phlorotannins from Eisenia bicyclis with BACE1 inhibitory activity. | ||||
| Ref 530909 | Bioorg Med Chem Lett. 2010 Jun 1;20(11):3211-5. Epub 2010 Apr 24.Molecular docking studies of phlorotannins from Eisenia bicyclis with BACE1 inhibitory activity. | ||||
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