| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T46465 | ||||
| Target Name | Plasmepsin 2 | ||||
| Target Type | Discontinued |
||||
| Drug Potency against Target | PS-444035 | Drug Info | Ki = 220 nM | [534798] | |
| PS-777621 | Drug Info | Ki = 58.9 nM | [528560] | ||
| KNI-764 | Drug Info | IC50 = 30 nM | [530280] | ||
| KNI-10761 | Drug Info | Ki = 17 nM | [531036] | ||
| KNI-10762 | Drug Info | Ki = 8.5 nM | [531036] | ||
| KNI-10758 | Drug Info | Ki = 4.2 nM | [531036] | ||
| PS-725074 | Drug Info | Ki = 500 nM | [534798] | ||
| KNI-10332 | Drug Info | Ki = 18 nM | [528767] | ||
| KNI-10125 | Drug Info | Ki = 10 nM | [529771] | ||
| KNI-10368 | Drug Info | Ki = 12 nM | [528767] | ||
| KNI-10232 | Drug Info | Ki = 0.2 nM | [528767] | ||
| KNI-10113 | Drug Info | Ki = 132 nM | [529771] | ||
| KNI-10283 | Drug Info | Ki = 25 nM | [529771] | ||
| KNI-10094 | Drug Info | Ki = 479 nM | [529771] | ||
| KNI-10092 | Drug Info | Ki = 153 nM | [529771] | ||
| KNI-10743 | Drug Info | Ki = 0.1 nM | [531036] | ||
| KNI-10255 | Drug Info | Ki = 38 nM | [529771] | ||
| KNI-10217 | Drug Info | Ki = 10 nM | [529771] | ||
| KNI-10155 | Drug Info | Ki = 5 nM | [529771] | ||
| KNI-10093 | Drug Info | Ki = 4 nM | [529771] | ||
| KNI-227 | Drug Info | Ki = 36 nM | [528767] | ||
| KNI-10033 | Drug Info | Ki = 3 nM | [528767] | ||
| KNI-272 | Drug Info | Ki = 1000 nM | [528767] | ||
| KNI-10527 | Drug Info | Ki = 6 nM | [529771] | ||
| KNI-10369 | Drug Info | Ki = 112 nM | [529771] | ||
| PS-154636-1 | Drug Info | Ki = 590 nM | [534798] | ||
| KNI-10313 | Drug Info | Ki = 5 nM | [528767] | ||
| KNI-10081 | Drug Info | Ki = 55 nM | [529771] | ||
| KNI-10265 | Drug Info | Ki = 14 nM | [529771] | ||
| KNI-10538 | Drug Info | Ki = 10 nM | [531036] | ||
| KNI-10316 | Drug Info | Ki = 17 nM | [528767] | ||
| KNI-1293 | Drug Info | Ki = 23 nM | [529771] | ||
| KNI-10763 | Drug Info | Ki = 9.1 nM | [531036] | ||
| KNI-10074 | Drug Info | Ki = 39 nM | [529771] | ||
| KNI-10372 | Drug Info | Ki = 4 nM | [528767] | ||
| KNI-10266 | Drug Info | Ki = 19 nM | [529771] | ||
| KNI-10282 | Drug Info | Ki = 21 nM | [529771] | ||
| KNI-10759 | Drug Info | Ki = 10 nM | [531036] | ||
| KNI-10124 | Drug Info | Ki = 9 nM | [529771] | ||
| KNI-10541 | Drug Info | Ki = 26 nM | [529771] | ||
| PS-662477 | Drug Info | Ki = 220 nM | [534798] | ||
| KNI-10342 | Drug Info | Ki = 4 nM | [528767] | ||
| KNI-10740 | Drug Info | Ki = 1.2 nM | [531036] | ||
| KNI-10106 | Drug Info | Ki = 126 nM | [529771] | ||
| KNI-10087 | Drug Info | Ki = 29 nM | [529771] | ||
| KNI-10006 | Drug Info | Ki = 0.5 nM | [531036] | ||
| KNI-10737 | Drug Info | Ki = 6.5 nM | [531036] | ||
| KNI-10742 | Drug Info | Ki = 0.1 nM | [531036] | ||
| KNI-10539 | Drug Info | Ki = 30 nM | [529771] | ||
| KNI-10079 | Drug Info | Ki = 145 nM | [529771] | ||
| KNI-10152 | Drug Info | Ki = 23 nM | [529771] | ||
| KNI-10256 | Drug Info | Ki = 25 nM | [529771] | ||
| KNI-10260 | Drug Info | Ki = 782 nM | [529771] | ||
| KNI-10216 | Drug Info | Ki = 10 nM | [529771] | ||
| KNI-10314 | Drug Info | Ki = 9 nM | [528767] | ||
| KNI-10760 | Drug Info | Ki = 5.1 nM | [531036] | ||
| KNI-10088 | Drug Info | Ki = 28 nM | [529771] | ||
| KNI-10526 | Drug Info | Ki = 21 nM | [529771] | ||
| KNI-10315 | Drug Info | Ki = 4 nM | [528767] | ||
| KNI-10741 | Drug Info | Ki = 0.68 nM | [531036] | ||
| KNI-10341 | Drug Info | Ki = 16 nM | [528767] | ||
| KNI-10062 | Drug Info | Ki = 9 nM | [528767] | ||
| KNI-10061 | Drug Info | Ki = 15 nM | [528767] | ||
| PS-222036 | Drug Info | Ki = 440 nM | [534798] | ||
| KNI-10529 | Drug Info | Ki = 7 nM | [529771] | ||
| KNI-10080 | Drug Info | Ki = 42 nM | [529771] | ||
| KNI-10095 | Drug Info | Ki = 55 nM | [529771] | ||
| References | |||||
| Ref 534798 | Bioorg Med Chem Lett. 1998 Sep 8;8(17):2315-20.Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library. | ||||
| Ref 528560 | J Med Chem. 2006 Dec 14;49(25):7440-9.High antiplasmodial activity of novel plasmepsins I and II inhibitors. | ||||
| Ref 530280 | Bioorg Med Chem. 2009 Aug 15;17(16):5933-49. Epub 2009 Jul 3.alpha-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases. | ||||
| Ref 531036 | Bioorg Med Chem Lett. 2010 Aug 15;20(16):4836-9. Epub 2010 Jun 25.Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. | ||||
| Ref 531036 | Bioorg Med Chem Lett. 2010 Aug 15;20(16):4836-9. Epub 2010 Jun 25.Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. | ||||
| Ref 531036 | Bioorg Med Chem Lett. 2010 Aug 15;20(16):4836-9. Epub 2010 Jun 25.Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. | ||||
| Ref 534798 | Bioorg Med Chem Lett. 1998 Sep 8;8(17):2315-20.Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library. | ||||
| Ref 528767 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52. Epub 2007 Mar 21.Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 528767 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52. Epub 2007 Mar 21.Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. | ||||
| Ref 528767 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52. Epub 2007 Mar 21.Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 531036 | Bioorg Med Chem Lett. 2010 Aug 15;20(16):4836-9. Epub 2010 Jun 25.Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 528767 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52. Epub 2007 Mar 21.Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. | ||||
| Ref 528767 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52. Epub 2007 Mar 21.Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. | ||||
| Ref 528767 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52. Epub 2007 Mar 21.Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 534798 | Bioorg Med Chem Lett. 1998 Sep 8;8(17):2315-20.Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library. | ||||
| Ref 528767 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52. Epub 2007 Mar 21.Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 531036 | Bioorg Med Chem Lett. 2010 Aug 15;20(16):4836-9. Epub 2010 Jun 25.Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. | ||||
| Ref 528767 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52. Epub 2007 Mar 21.Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 531036 | Bioorg Med Chem Lett. 2010 Aug 15;20(16):4836-9. Epub 2010 Jun 25.Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 528767 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52. Epub 2007 Mar 21.Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 531036 | Bioorg Med Chem Lett. 2010 Aug 15;20(16):4836-9. Epub 2010 Jun 25.Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 534798 | Bioorg Med Chem Lett. 1998 Sep 8;8(17):2315-20.Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library. | ||||
| Ref 528767 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52. Epub 2007 Mar 21.Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. | ||||
| Ref 531036 | Bioorg Med Chem Lett. 2010 Aug 15;20(16):4836-9. Epub 2010 Jun 25.Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 531036 | Bioorg Med Chem Lett. 2010 Aug 15;20(16):4836-9. Epub 2010 Jun 25.Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. | ||||
| Ref 531036 | Bioorg Med Chem Lett. 2010 Aug 15;20(16):4836-9. Epub 2010 Jun 25.Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. | ||||
| Ref 531036 | Bioorg Med Chem Lett. 2010 Aug 15;20(16):4836-9. Epub 2010 Jun 25.Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 528767 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52. Epub 2007 Mar 21.Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. | ||||
| Ref 531036 | Bioorg Med Chem Lett. 2010 Aug 15;20(16):4836-9. Epub 2010 Jun 25.Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 528767 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52. Epub 2007 Mar 21.Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. | ||||
| Ref 531036 | Bioorg Med Chem Lett. 2010 Aug 15;20(16):4836-9. Epub 2010 Jun 25.Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. | ||||
| Ref 528767 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52. Epub 2007 Mar 21.Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. | ||||
| Ref 528767 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52. Epub 2007 Mar 21.Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. | ||||
| Ref 528767 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52. Epub 2007 Mar 21.Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. | ||||
| Ref 534798 | Bioorg Med Chem Lett. 1998 Sep 8;8(17):2315-20.Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
| Ref 529771 | Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. | ||||
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