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3.4.23.38: plasmepsin I

This is an abbreviated version!
For detailed information about plasmepsin I, go to the full flat file.

Word Map on EC 3.4.23.38

Reaction

hydrolysis of the -Phe33-/-Leu- bond in the alpha-chain of hemoglobin, leading to denaturation of the molecule =

Synonyms

AH I, aspartic hemoglobinase I, malaria aspartic hemoglobinase, PFAPG, PfPM1, plasmepsin 1, plasmepsin I, plasmepsin-I, PLm I, PM I, PM-I, PMI

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.23 Aspartic endopeptidases
                3.4.23.38 plasmepsin I

KI Value

KI Value on EC 3.4.23.38 - plasmepsin I

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Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00025
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-ylethyl)-butyramide
-
-
0.0013
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide
-
-
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
-
-
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
-
-
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
-
-
0.000006
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(1,3-benzodioxol-5-yl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
0.000008
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(4-acetylphenyl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N,N'-bis[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]hexanediamide
-
-
0.000038
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-(4-acetylphenyl)prop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
0.000009
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxo-6-[2-(3-phenylpropanoyl)hydrazino]hexanamide
-
-
0.000198
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-6-[2-[(4-tert-butylphenyl)carbonyl]hydrazino]-3,4-dihydroxy-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-oxohexanamide
-
-
0.001837
(2R,3R,4R,5R)-2,5-bis[[(2E)-3-bromoprop-2-en-1-yl]oxy]-N'1,N'6-bis[(4-tert-butylphenyl)carbonyl]-3,4-dihydroxyhexanedihydrazide
-
-
0.00016 - 0.000163
(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
0.0000084
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(2,4-dimethoxy-3,5-pyrimidin)-2-propenyl-oxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.000023
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(2,5-dimethyl-3,4-oxazol)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000005
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(3,4-methylenedioxyphenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000013
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(3-thienyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000008
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-acetylphenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
the best dual inhibitor for EC 3.4.23.38 and EC 3.4.23.39
0.0000025
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-fluorophenyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000058
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-(4-tolyl)-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.000027
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-bromo-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000014
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-3-phenyl-2-propenyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000072
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-5-phenyl-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.000037
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-5-trimethylsilyl-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.000037
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E)-pent-2-en-4-ynyl]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000037
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E,4E)-5-(methoxycarbonyl)-pent-2,4-dienyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.0000044
(2R,3R,4R,5R)-N1,N6-bis[(1S,2R)-2-hydroxy-1-indanyl]-2,5-bis[(2E,4E)-5-phenyl-pentadienyloxy]-3,4-dihydroxyhexane-1,6-diamide
-
-
0.00082
(2S,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
-
0.00001
(2S,5S,14S,17S,18S)-N-(2-amino-2-oxoethyl)-17-benzyl-18-hydroxy-14-[[N-(3-methylbutanoyl)-L-valyl]amino]-2-(1-methylethyl)-3,8,15,20-tetraoxo-1,4,9,16-tetraazacycloicosane-5-carboxamide
-
-
0.000098
(2S,5S,6R)-3-aza-2-(p-bromobenzyl)-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.00053
(2S,5S,6R)-3-aza-2-[m-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.0011
(2S,5S,6R)-3-aza-2-[m-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000063
(2S,5S,6R)-3-aza-2-[p-(m-aminophenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000115
(2S,5S,6R)-3-aza-2-[p-(p-methylphenyl)benzyl]-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.0013
(2S,5S,6R)-3-aza-5-hydroxy-2-[m-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000438
(2S,5S,6R)-3-aza-5-hydroxy-2-[p-(o-methoxyphenyl)-benzyl]-7-phenyl-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.001
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(m-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000068
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-2-(p-phenylbenzyl)-6-[(picolyl-L-valinyl)amino]heptanoyl amide
-
-
0.000469
(2S,5S,6R)-3-aza-5-hydroxy-7-phenyl-6-[(picolyl-L-valinyl)amino]-2-(m-(trifluoromethanesulfonyloxy)benzyl)-heptanoyl amide
-
-
0.024
(3S,4S)-5-(4-bromobenzyloxy)-3-hydroxy-4-(2-thiophen-2-ylacetylamino)pentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
0.04
(3S,4S)-5-(4-bromobenzyloxy)-4-(3,3-diphenylpropionylamino)-3-hydroxypentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
0.057
(3S,4S)-5-(4-bromobenzyloxy)-4-diphenylacetylamino-3-hydroxypentanoic acid [(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethyl]amide
-
-
0.000727
(3S,4S)-N-butyl-3-hydroxy-6-methyl-4-((2S,3S)-3-methyl-2-(2-(naphthalen-2-yloxy)acetamido)pentanamido)heptanamide
-
-
0.00028
(4R)-3-[(2S,3S)-3-[[(2,6-dimethylphenoxy)acetyl]amino]-2-hydroxy-4-phenylbutanoyl]-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.00091
(4R)-N-tert-butyl-3-[(2S,3S)-2-hydroxy-3-([N-[(isoquinolin-5-yloxy)acetyl]-S-methyl-L-cysteinyl]amino)-4-phenylbutanoyl]-1,3-thiazolidine-4-carboxamide
-
-
0.002046
(5S)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]-5-(p-phenylbenzyl)imidazolidine-2,4-dione
-
-
0.0019
(5S)-5-(p-bromobenzyl)-1-[(2S,3R)-2-hydroxy-4-phenyl-3-[(picolyl-L-valinyl)amino]butyl]imidazoline-2,4-dione
-
-
0.059
(S)-2,3-dihydro-1H-indole-2-carboxylic acid ((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxy-propyl)amide
-
-
0.000017
(S)-propyl 6-(tert-butoxycarbonylamino)-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000011
(S)-propyl 6-amino-2-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)hexanoate
-
-
0.00000001
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
-
-
0.000163
2,5-Bis-allyloxy-3,4-dihydroxy-hexanedioic acid bis-[(2-hydroxy-indan-1-yl)-amide]
-
-
0.000025
2,5-Bis-benzyloxy-3,4-dihydroxy-hexanedioic acid bis-[(2-hydroxy-indan-1-yl)-amide]
-
-
0.0000048
4-(1,3-benzodioxol-5-yl)-Nalpha-[(2S,3S)-2-hydroxy-3-([N-[3-(1H-indol-3-yl)propanoyl]-L-valyl]amino)-4-phenylbutyl]-L-phenylalaninamide
-
-
0.000013
4-(1-benzofuran-2-yl)-Nalpha-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
0.029
benzo[1,3]dioxole-5-carboxylic acid ((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-amide
-
-
0.00025
benzyl 2-benzyl-2-[(2S,3R)-3-[(4-bromobenzyl)oxy]-2-hydroxy-4-oxo-4-[(2-piperidin-1-ylethyl)amino]butyl]hydrazinecarboxylate
-
-
0.000009
benzyl 3-benzyl-4-([2-[(1-formyl-3-methylbutyl)amino]-2-oxo-1-phenylethyl]amino)-4-oxobutanoate
-
-
0.0000027
benzyl [(1S,4S,5R,6R,7S,10S)-4,7-bis[(4-cyanophenoxy)methyl]-5,6-dihydroxy-1,10-bis(1-methylethyl)-2,9,12-trioxo-14-phenyl-13-oxa-3,8,11-triazatetradec-1-yl]carbamate
-
-
0.0000005 - 0.0000007
Iva-Val-Val-Sta-Ala-Sta
0.042
KPFEL-PSI(CH2-NH)-AWT
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.000043
KPFSL-PSI(CH2-NH)-LQF
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.0055
KPLEF-PSI(CH2-NH)-FRV
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.038
KPLEF-PSI(CH2-NH)-YRV
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.000073
KPnorLSnorL-PSI(CH2-NH)-LQI
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.031
KPVEF-PSI(CH2-NH)-RQT
pH 4.5, 37°C, recombinant truncated proPfPM1 K110pN mutant
0.0003
N'1-[(E)-(2,3-dihydroxyphenyl)methylidene]-N'3-[(Z)-(2,3-dihydroxyphenyl)methylidene]benzene-1,3-dicarbohydrazide
0.0000033
N-((1S,2S)-1-(4-benzo[1,3]dioxol-5-yl-benzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
0.619
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-[2-(3-methoxyphenyl)ethylcarbamoyl]propyl)-2,4,6-trifluorobenzamide
-
-
0.0034
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-2,4,6-trifluorobenzamide
-
-
0.032
N-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropyl)-3,4-dichlorobenzamide
-
-
0.000116
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethylcarbamoyl]-propyl)-2,4,6-trifluorobenzamide
-
-
0.0000059
N-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propyl)-2,4,6-trifluorobenzamide
-
-
0.000221
N-((1S,2S)-2-hydroxy-3-[2-(3-methoxy-phenyl)-ethyl-carbamoyl]-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl)-2,4,6-trifluorobenzamide
-
-
0.000033
N-((2S)-1-((2S)-6-amino-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxohexan-2-ylamino)-1-oxopropan-2-yl)-4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
0.000001
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-1-oxopropan-2-ylcarbamoyl)phenoxy)benzamide
-
-
0.000074
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-1-oxopropan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000058
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
-
0.000765
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-((2S)-1-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamide
-
not cytotoxic against human fibroblasts at 0.100 mM and are highly selective for plasmepsins vs human cathepsin D
0.000081
N-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-yl)-4-(4-(4-(6-methoxyquinolin-8-ylamino)pentylcarbamoyl)phenoxy)benzamide
-
-
0.000031
N-[(1S)-1-([(1S,2S)-3-[(2-amino-2-oxoethyl)(benzyl)amino]-1-benzyl-2-hydroxypropyl]carbamoyl)-2-methylpropyl]pyridine-2-carboxamide
-
-
0.0000004
N-[(1S)-1-[[(1S,2S)-1-([[4-(1,3-benzodioxol-5-yl)benzyl]oxy]methyl)-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.000016
N-[(1S)-1-[[(1S,2S)-1-benzyl-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.0000005
N-[(1S)-1-[[(1S,2S)-1-[[(4-bromobenzyl)oxy]methyl]-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.000115
N-[(1S)-1-[[(1S,2S)-3-([(1S)-2-amino-1-[(4'-methylbiphenyl-4-yl)methyl]-2-oxoethyl]amino)-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.001
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-3-ylmethyl)-2-oxoethyl]amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.00022
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-4-ylmethyl)-2-oxoethyl](benzyl)amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.000068
N-[(1S)-1-[[(1S,2S)-3-[[(1S)-2-amino-1-(biphenyl-4-ylmethyl)-2-oxoethyl]amino]-1-benzyl-2-hydroxypropyl]carbamoyl]-2-methylpropyl]pyridine-2-carboxamide
-
-
0.822
N-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-cyclohexylcarbamoyl-2-hydroxypropyl]-2,4,6-trifluorobenzamide
-
-
0.000188
N-[(1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-cyclo-hexylcarbamoyl-2-hydroxypropyl]-2,4,6-trifluorobenzamide
-
-
0.0000034
N-[(1S,2S)-1-[[(4-bromobenzyl)oxy]methyl]-4-[[(1S)-2-[[(1S)-1-carbamoyl-3-methylbutyl]amino]-1-methyl-2-oxoethyl]amino]-2-hydroxy-4-oxobutyl]-2,4,6-trifluorobenzamide
-
-
0.000278
N-[(1S,2S)-3-cyclohexylcarbamoyl-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl]-2,4,6-trifluorobenzamide
-
-
0.0000021
N-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butyl-carbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl]-2,4,6-trifluorobenzamide
-
-
0.000022
N-[(3S)-3-[(2S,5S,14S)-14-[(3,3-dimethylbutanoyl)amino]-2-(1-methylethyl)-3,11,15-trioxo-1,4,10-triazacyclopentadecan-5-yl]-3-hydroxypropanoyl]-L-valyl-L-leucylglycinamide
-
-
0.000027
N-[(3S,4S)-3-hydroxy-6-phenyl-4-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]hexanoyl]-L-alanyl-L-leucinamide
-
-
0.0000026
N-[1-Benzyl-3-(2-biphenyl-4-yl-1-carbamoyl-ethylamino)-2-hydroxy-propyl]-2-(3-1H-indol-3-yl-propionylamino)-3-methyl-butyramide
-
-
0.0029
N2-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-leucinamide
-
-
0.0021
Nalpha-[(2S,3S)-2-hydroxy-4-phenyl-3-[[N-(pyridin-2-ylcarbonyl)-L-valyl]amino]butyl]-L-phenylalaninamide
-
-
0.000000565
pepstatin
-
pH 5.0, 37°C
0.0000000117 - 0.0000014
pepstatin A
0.0064
pyridine-2-carboxylic acid ((R)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
0.000001
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(3-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)-ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methyl-propyl)-amide
-
-
0.0000004
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-benzo-[1,3]dioxol-5-yl-benzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)-amide
-
-
0.0067
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(2-(3-methoxyphenyl)ethylcarbamoyl)propylcarbamoyl)-2-methylpropyl)amide
-
-
0.049
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-methoxypropylcarbamoyl)propylcarbamoyl)-2-methylpropyl)amide
-
-
0.0005
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(4-bromobenzyloxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
0.0000007
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(biphenyl-3-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propylcar-bamoyl)-2-methyl-propyl)-amide
-
-
0.0000003
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-propylcarbamoyl)-2-methyl-propyl)-amide
-
-
0.0054
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-1-benzyloxymethyl-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl)-2-methylpropyl)amide
-
-
0.027
pyridine-2-carboxylic acid ((S)-1-((1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methylbutylcarbamoyl)ethylcarbamoyl]-2-hydroxy-1-phenethylpropylcarbamoyl)-2-methylpropyl)amide
-
-
0.0000027
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-benzo-[1,3]dioxol-5-yl-benzyloxymethyl)-3-butylcarbamoyl-2-hydroxy-propylcarbamoyl]-2-methyl-propyl)-amide
-
-
0.0089
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(2-phenylaminoethyl-carbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
0.0054
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-2-hydroxy-3-(3-phenylpropylcarbamoyl)propylcarbamoyl]-2-methylpropyl)amide
-
-
0.053
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-(4-cyanobenzylcarbamoyl)-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
0.0039
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-(cyclohexylmethylcarbamoyl)-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
0.0081
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-butylcarbamoyl-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
0.0041
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(4-bromobenzyloxymethyl)-3-cyclohexylcarbamoyl-2-hydroxypropylcarbamoyl]-2-methylpropyl)amide
-
-
0.0000019
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-1-(biphenyl-4-ylmethoxymethyl)-3-butylcarbamoyl-2-hydroxy-propylcarbamoyl]-2-methylpropyl)-amide
-
-
0.000001
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-butylcarbamoyl-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propylcarbamoyl]-2-methyl-propyl)-amide
-
-
0.0000004
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(3-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
0.0000003
pyridine-2-carboxylic acid ((S)-1-[(1S,2S)-3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-hydroxy-1-(4-thiophen-3-yl-benzyloxymethyl)-propyl-carbamoyl]-2-methyl-propyl)-amide
-
-
0.0000014 - 0.000009
Ro40-4388
0.000006 - 0.000008
Ro40-5576
0.00023
tert-butyl (5S)-5-((S)-2-(4-(4-((2S,3S)-1-((3S,4S)-1-(butylamino)-3-hydroxy-6-methyl-1-oxoheptan-4-ylamino)-3-methyl-1-oxopentan-2-ylcarbamoyl)phenoxy)benzamido)-4-methylpentanamido)-6-(4-(6-methoxyquinolin-8-ylamino)pentylamino)-6-oxohexylcarbamate
-
-
additional information
additional information
-
Ki-value for Ro17-7109 is above 0.05 mM
-