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Literature summary extracted from

  • Ersmark, K.; Nervall, M.; Gutierrez-de-Teran, H.; Hamelink, E.; Janka, L.K.; Clemente, J.C.; Dunn, B.M.; Gogoll, A.; Samuelsson, B.; Qvist, J.; Hallberg, A.
    Macrocyclic inhibitors of the malarial aspartic proteases plasmepsin I, II, and IV (2006), Bioorg. Med. Chem., 14, 2197-2208.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.23.B14 (2R,3R,4R)-2-benzyloxy-3,4-dihydroxy-N-[(1S,2R)-2-hydroxyindan-1-yl]-4-[(2R)-3-oxo-1-oxa-4-aza-cyclotridec-2-yl]butyramide
-
 Plasmodium falciparum
3.4.23.B14 (2R,3R,4R)-2-benzyloxy-3,4-dihydroxy-N-[(1S,2R)-2-hydroxyindan-1-yl]-4-[(2R,11E)-3-oxo-1-oxa-4-aza-cyclo-tridec-11-en-2-yl]butyramide
-
 Plasmodium falciparum
3.4.23.B14 (2R,3R,4R,5R)-5-benzyloxy-3,4-dihydroxy-6-oxo-1-oxa-7-aza-cyclohexadec-2-carboxylic acid [(1S,2R)-2-hydroxyindan-1-yl]-amide
-
 Plasmodium falciparum
3.4.23.B14 (2R,3R,4R,5R,14E)-5-benzyloxy-3,4-dihydroxy-6-oxo-1-oxa-7-aza-cyclohexadec-14-ene-2-carboxylic acid [(1S,2R)-2-hydroxyindan-1-yl]-amide
-
 Plasmodium falciparum
3.4.23.38 (2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R)-3-oxo-1-oxa-4-azacyclotridecan-2-yl]butanamide
-
 Plasmodium falciparum
3.4.23.38 (2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R,11E)-3-oxo-1-oxa-4-azacyclotridec-11-en-2-yl]butanamide
-
 Plasmodium falciparum
3.4.23.38 (2R,3R,4R,5R)-2,5-bis(benzyloxy)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
-
 Plasmodium falciparum
3.4.23.38 (2R,3R,4R,5R)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-2,5-bis(prop-2-en-1-yloxy)hexanediamide
-
 Plasmodium falciparum
3.4.23.39 (2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R)-3-oxo-1-oxa-4-azacyclotridecan-2-yl]butanamide
-
 Plasmodium falciparum
3.4.23.39 (2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R,11E)-3-oxo-1-oxa-4-azacyclotridec-11-en-2-yl]butanamide
-
 Plasmodium falciparum
3.4.23.39 (2R,3R,4R,5R)-2,5-bis(benzyloxy)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
-
 Plasmodium falciparum
3.4.23.39 (2R,3R,4R,5R)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-2,5-bis(prop-2-en-1-yloxy)hexanediamide
-
 Plasmodium falciparum
3.4.23.39 (2R,3R,4R,5R,14E)-5-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-1-oxa-7-azacyclohexadec-14-ene-2-carboxamide
-
 Plasmodium falciparum

Organism

EC Number Organism UniProt Comment Textmining
3.4.23.B14 Plasmodium falciparum
-
-
-
3.4.23.38 Plasmodium falciparum
-
-
-
3.4.23.39 Plasmodium falciparum
-
-
-

Synonyms

EC Number Synonyms Comment Organism
3.4.23.38 PLm I
-
 Plasmodium falciparum
3.4.23.39 PLm II
-
 Plasmodium falciparum

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.23.B14 0.0002
-
 (2R,3R,4R)-2-benzyloxy-3,4-dihydroxy-N-[(1S,2R)-2-hydroxyindan-1-yl]-4-[(2R)-3-oxo-1-oxa-4-aza-cyclotridec-2-yl]butyramide
-
 Plasmodium falciparum
3.4.23.B14 0.002
-
 (2R,3R,4R,5R,14E)-5-benzyloxy-3,4-dihydroxy-6-oxo-1-oxa-7-aza-cyclohexadec-14-ene-2-carboxylic acid [(1S,2R)-2-hydroxyindan-1-yl]-amide
-
 Plasmodium falciparum
3.4.23.B14 0.0022
-
 (2R,3R,4R,5R)-5-benzyloxy-3,4-dihydroxy-6-oxo-1-oxa-7-aza-cyclohexadec-2-carboxylic acid [(1S,2R)-2-hydroxyindan-1-yl]-amide
-
 Plasmodium falciparum
3.4.23.B14 0.0068
-
 (2R,3R,4R)-2-benzyloxy-3,4-dihydroxy-N-[(1S,2R)-2-hydroxyindan-1-yl]-4-[(2R,11E)-3-oxo-1-oxa-4-aza-cyclo-tridec-11-en-2-yl]butyramide
-
 Plasmodium falciparum
3.4.23.38 0.000025
-
 (2R,3R,4R,5R)-2,5-bis(benzyloxy)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
-
 Plasmodium falciparum
3.4.23.38 0.00016
-
 (2R,3R,4R,5R)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-2,5-bis(prop-2-en-1-yloxy)hexanediamide
-
 Plasmodium falciparum
3.4.23.38 0.00018
-
 (2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R)-3-oxo-1-oxa-4-azacyclotridecan-2-yl]butanamide
-
 Plasmodium falciparum
3.4.23.38 0.0005
-
 (2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R,11E)-3-oxo-1-oxa-4-azacyclotridec-11-en-2-yl]butanamide
-
 Plasmodium falciparum
3.4.23.39 0.000085
-
 (2R,3R,4R,5R)-2,5-bis(benzyloxy)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
-
 Plasmodium falciparum
3.4.23.39 0.000096
-
 (2R,3R,4R,5R)-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-2,5-bis(prop-2-en-1-yloxy)hexanediamide
-
 Plasmodium falciparum
3.4.23.39 0.00012
-
 (2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R)-3-oxo-1-oxa-4-azacyclotridecan-2-yl]butanamide
-
 Plasmodium falciparum
3.4.23.39 0.00038
-
 (2R,3R,4R)-2-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-4-[(2R,11E)-3-oxo-1-oxa-4-azacyclotridec-11-en-2-yl]butanamide
-
 Plasmodium falciparum
3.4.23.39 0.0011
-
 (2R,3R,4R,5R,14E)-5-(benzyloxy)-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-1-oxa-7-azacyclohexadec-14-ene-2-carboxamide
-
 Plasmodium falciparum