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Literature summary for 3.4.23.39 extracted from

  • Haque, T.S.; Skillman, A.G.; Lee, C.E.; Habashita, H.; Gluzman, I.Y.; Ewing, T.J.; Goldberg, D.E.; Kuntz, I.D.; Ellman, J.A.
    Potent, low-molecular-weight non-peptide inhibitors of malarial aspartyl protease plasmepsin II (1999), J. Med. Chem., 42, 1428-1440.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-[3-(4-benzyloxy-3,5-dimethoxy-benzoylamino)-2-hydroxy-4-phenyl-butyl]-amide
-
Plasmodium falciparum
1-acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-[3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-amide
-
Plasmodium falciparum
1-acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-[3-[2-(3-chloro-phenylamino)-acetylamino]-2-hydroxy-4-phenyl-butyl]-amide
-
Plasmodium falciparum
1-Acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-{3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-amide
-
Plasmodium falciparum
1-Acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-{3-[2-(3-chloro-phenylamino)-acetylamino]-2-hydroxy-4-phenyl-butyl}-amide
-
Plasmodium falciparum
1-methyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-(3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl)-amide
-
Plasmodium falciparum
1-Methyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-{3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-amide
-
Plasmodium falciparum
1-Methyl-piperidine-4-carboxylic acid [3-(4-benzyloxy-3,5-dimethoxy-benzoylamino)-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
Plasmodium falciparum
1-methyl-piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
Plasmodium falciparum
1-Methyl-piperidine-4-carboxylic acid {3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-[2-(4-methoxy-phenyl)-ethyl]-amide
-
Plasmodium falciparum
17-Benzyl-14-[2-(3,3-dimethyl-butyrylamino)-3-methyl-butyrylamino]-18-hydroxy-2-isopropyl-3,8,15,20-tetraoxo-1,4,9,16tetraaza-cycloicosane-5-carboxylic acid carbamoylmethyl-amide
-
Plasmodium falciparum
additional information single-digit nanomolar, low-molecular-weight inhibitors Plasmodium falciparum
N-(2-benzo[1,3]dioxol-5-yl-ethyl)-N-[3-[2-(2,5-dimethyl-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-3-(dioxo-1,3-dihydro-isoindol-2-yl)-propionamide
-
Plasmodium falciparum
N-(2-benzo[1,3]dioxol-5-yl-ethyl)-N-[3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-3-(dioxo-1,3-dihydro-isoindol-2-yl)-propionamide
-
Plasmodium falciparum
N-(2-Benzo[1,3]dioxol-5-yl-ethyl)-N-{3-[2-(2,5-dimethyl-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-3-(dioxo-1,3-dihydro-isoindol-2-yl)-propionamide
-
Plasmodium falciparum
N-(2-Benzo[1,3]dioxol-5-yl-ethyl)-N-{3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-3-(dioxo-1,3-dihydro-isoindol-2-yl)-propionamide
-
Plasmodium falciparum
N-(3-{(2-Benzo[1,3]dioxol-5-yl-ethyl)-[3-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-propionyl]-amino}-1-benzyl-2-hydroxy-propyl)-4-benzyloxy-3,5-dimethoxy-benzamide
-
Plasmodium falciparum
N-[3-[(2-benzo[1,3]dioxol-5-yl-ethyl)-[3-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-propionyl]-amino]-1-benzyl-2-hydroxy-propyl]-4-benzyloxy-3,5-dimethoxy-benzamide
-
Plasmodium falciparum
Piperidine-4-carboxylic acid [3-(4-benzyloxy-3,5-dimethoxy-benzoylamino)-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
Plasmodium falciparum
piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
Plasmodium falciparum
Piperidine-4-carboxylic acid {3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl}-[2-(4-methoxy-phenyl)-ethyl]-amide
-
Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000002
-
1-methyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-(3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl)-amide
-
Plasmodium falciparum
0.000002
-
1-methyl-piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
Plasmodium falciparum
0.000003
-
1-acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-[3-[2-(3-chloro-phenylamino)-acetylamino]-2-hydroxy-4-phenyl-butyl]-amide
-
Plasmodium falciparum
0.000004
-
1-acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-[3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-amide
-
Plasmodium falciparum
0.0000041
-
1-Methyl-piperidine-4-carboxylic acid [3-(4-benzyloxy-3,5-dimethoxy-benzoylamino)-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
Plasmodium falciparum
0.0000043
-
piperidine-4-carboxylic acid [3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
Plasmodium falciparum
0.0000048
-
1-acetyl-piperidine-4-carboxylic acid (2-benzo[1,3]dioxol-5-yl-ethyl)-[3-(4-benzyloxy-3,5-dimethoxy-benzoylamino)-2-hydroxy-4-phenyl-butyl]-amide
-
Plasmodium falciparum
0.000009
-
Piperidine-4-carboxylic acid [3-(4-benzyloxy-3,5-dimethoxy-benzoylamino)-2-hydroxy-4-phenyl-butyl]-[2-(4-methoxy-phenyl)-ethyl]-amide
-
Plasmodium falciparum
0.0001
-
N-[3-[(2-benzo[1,3]dioxol-5-yl-ethyl)-[3-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-propionyl]-amino]-1-benzyl-2-hydroxy-propyl]-4-benzyloxy-3,5-dimethoxy-benzamide
-
Plasmodium falciparum
0.00022
-
N-(2-benzo[1,3]dioxol-5-yl-ethyl)-N-[3-[2-(3-chloro-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-3-(dioxo-1,3-dihydro-isoindol-2-yl)-propionamide
-
Plasmodium falciparum
0.0003
-
N-(2-benzo[1,3]dioxol-5-yl-ethyl)-N-[3-[2-(2,5-dimethyl-phenoxy)-acetylamino]-2-hydroxy-4-phenyl-butyl]-3-(dioxo-1,3-dihydro-isoindol-2-yl)-propionamide
-
Plasmodium falciparum
0.0015
-
17-Benzyl-14-[2-(3,3-dimethyl-butyrylamino)-3-methyl-butyrylamino]-18-hydroxy-2-isopropyl-3,8,15,20-tetraoxo-1,4,9,16tetraaza-cycloicosane-5-carboxylic acid carbamoylmethyl-amide
-
Plasmodium falciparum