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Literature summary for 3.4.23.39 extracted from

  • Corminboeuf, O.; Dunet, G.; Hafsi, M.; Grimont, J.; Grisostomi, C.; Meyer, S.; Binkert, C.; Bur, D.; Jones, A.; Prade, L.; Brun, R.; Boss, C.
    Inhibitors of plasmepsin II-potential antimalarial agents (2006), Bioorg. Med. Chem. Lett., 16, 6194-6199.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)-N,N-dimethylbiphenyl-4-carboxamide IC50: 77 nM Plasmodium falciparum
methyl [4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-yl]acetate IC50: 183 nM Plasmodium falciparum
N-((4'-[2-(benzylamino)-2-oxoethyl]biphenyl-4-yl)methyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide IC50: 46 nM Plasmodium falciparum
N-(4-[5-(1,3-benzodioxol-5-yl)pyridin-2-yl]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide IC50: 1912 nM Plasmodium falciparum
N-(4-[6-(1,3-benzodioxol-5-yl)pyridin-3-yl]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide IC50: 437 nM Plasmodium falciparum
N-(4-[benzyl(methyl)amino]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide IC50: 289 nM Plasmodium falciparum
N-(biphenyl-4-ylmethyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide IC50: 143 nM Plasmodium falciparum
N-benzyl-4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-carboxamide IC50: 72 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-piperidin-1-ylbenzyl)benzamide IC50: 369 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-2-ylbenzyl)benzamide IC50: 380 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-3-ylbenzyl)benzamide IC50: 374 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-4-ylbenzyl)benzamide IC50: 212 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyrimidin-5-ylbenzyl)benzamide IC50: 531 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-thiomorpholin-4-ylbenzyl)benzamide IC50: 188 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-4-pentyl-N-([4'-(thiomorpholin-4-ylcarbonyl)biphenyl-4-yl]methyl)benzamide IC50: 56 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(1H-pyrrol-1-yl)benzyl]benzamide IC50: 240 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(4-phenylpiperazin-1-yl)benzyl]benzamide IC50: 200 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(5-phenylpyridin-2-yl)benzyl]benzamide IC50: 2345 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(5-pyrimidin-5-ylpyridin-2-yl)benzyl]benzamide IC50: 8530 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(6-phenylpyridin-3-yl)benzyl]benzamide IC50: 589 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(6-pyrimidin-5-ylpyridin-3-yl)benzyl]benzamide IC50: 2229 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(phenylamino)benzyl]benzamide IC50: 224 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(pyridin-4-ylamino)benzyl]benzamide IC50: 1816 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-N-(4-[methyl(phenyl)amino]benzyl)-4-pentylbenzamide IC50: 574 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-N-(4-[methyl(pyridin-4-yl)amino]benzyl)-4-pentylbenzamide IC50: 3015 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-N-([4'-(2-hydroxyethoxy)biphenyl-4-yl]methyl)-4-pentylbenzamide IC50: 511 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-N-([4'-(2-morpholin-4-yl-2-oxoethyl)biphenyl-4-yl]methyl)-4-pentylbenzamide IC50: 74 nM; IC50: 91 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-N-[4-(1H-indol-1-yl)benzyl]-4-pentylbenzamide IC50: 670 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-N-[4-(4-methylpiperazin-1-yl)benzyl]-4-pentylbenzamide IC50: 2547 nM Plasmodium falciparum
N-[2-(dibutylamino)ethyl]-N-[4-(diethylamino)benzyl]-4-pentylbenzamide IC50: 1491 nM Plasmodium falciparum
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]-2-methoxypyridine-4-carboxamide IC50: 154 nM Plasmodium falciparum
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]piperidine-3-carboxamide IC50: 202 nM Plasmodium falciparum
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]piperidine-4-carboxamide IC50: 464 nM Plasmodium falciparum
N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]pyrazine-2-carboxamide IC50: 243 nM Plasmodium falciparum
N-[4-(1,3-benzodioxol-5-yl)benzyl]-4-pentyl-N-(2-piperidin-1-ylethyl)benzamide IC50: 334 nM Plasmodium falciparum
N-[4-(1,3-benzodioxol-5-yl)benzyl]-4-pentyl-N-(2-[4-(3-phenylpropyl)piperidin-1-yl]ethyl)benzamide IC50: 165 nM Plasmodium falciparum
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-([2-(diethylamino)ethyl](ethyl)amino)ethyl)-4-pentylbenzamide IC50: 439 nM Plasmodium falciparum
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-morpholin-4-ylethyl)-4-pentylbenzamide IC50: 2897 nM Plasmodium falciparum
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-[benzyl(2-hydroxyethyl)amino]ethyl)-4-pentylbenzamide IC50: 334 nM Plasmodium falciparum
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-[bis(1-methylethyl)amino]ethyl)-4-pentylbenzamide IC50: 1501 nM Plasmodium falciparum
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(4-benzylpiperidin-1-yl)ethyl]-4-pentylbenzamide IC50: 190 nM Plasmodium falciparum
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide IC50: 101 nM Plasmodium falciparum
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(diethylamino)ethyl]-4-pentylbenzamide IC50: 1519 nM Plasmodium falciparum
N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dipropylamino)ethyl]-4-pentylbenzamide IC50: 531 nM Plasmodium falciparum
N-[4-(2,2'-bipyridin-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide IC50: 587 nM; IC50: 736 nM Plasmodium falciparum
N-[4-(2,4'-bipyridin-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide IC50: 642 nM Plasmodium falciparum
N-[4-(3,3'-bipyridin-6-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide IC50: 5266 nM Plasmodium falciparum
N-[4-(3,4'-bipyridin-6-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide IC50: 4553 nM Plasmodium falciparum
N-[4-(4-benzylpiperazin-1-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide IC50: 646 nM Plasmodium falciparum
N-[4-(benzylamino)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide IC50: 429 nM Plasmodium falciparum
[4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-yl]acetic acid IC50: 463 nM Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000046
-
IC50: 46 nM Plasmodium falciparum N-((4'-[2-(benzylamino)-2-oxoethyl]biphenyl-4-yl)methyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
0.000056
-
IC50: 56 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-4-pentyl-N-([4'-(thiomorpholin-4-ylcarbonyl)biphenyl-4-yl]methyl)benzamide
0.000072
-
IC50: 72 nM Plasmodium falciparum N-benzyl-4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-carboxamide
0.000074
-
IC50: 74 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-N-([4'-(2-morpholin-4-yl-2-oxoethyl)biphenyl-4-yl]methyl)-4-pentylbenzamide
0.000077
-
IC50: 77 nM Plasmodium falciparum 4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)-N,N-dimethylbiphenyl-4-carboxamide
0.000091
-
IC50: 91 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-N-([4'-(2-morpholin-4-yl-2-oxoethyl)biphenyl-4-yl]methyl)-4-pentylbenzamide
0.000101
-
IC50: 101 nM Plasmodium falciparum N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
0.000143
-
IC50: 143 nM Plasmodium falciparum N-(biphenyl-4-ylmethyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
0.000154
-
IC50: 154 nM Plasmodium falciparum N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]-2-methoxypyridine-4-carboxamide
0.000165
-
IC50: 165 nM Plasmodium falciparum N-[4-(1,3-benzodioxol-5-yl)benzyl]-4-pentyl-N-(2-[4-(3-phenylpropyl)piperidin-1-yl]ethyl)benzamide
0.000183
-
IC50: 183 nM Plasmodium falciparum methyl [4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-yl]acetate
0.000188
-
IC50: 188 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-thiomorpholin-4-ylbenzyl)benzamide
0.00019
-
IC50: 190 nM Plasmodium falciparum N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(4-benzylpiperidin-1-yl)ethyl]-4-pentylbenzamide
0.0002
-
IC50: 200 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(4-phenylpiperazin-1-yl)benzyl]benzamide
0.000202
-
IC50: 202 nM Plasmodium falciparum N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]piperidine-3-carboxamide
0.000212
-
IC50: 212 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-4-ylbenzyl)benzamide
0.000224
-
IC50: 224 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(phenylamino)benzyl]benzamide
0.00024
-
IC50: 240 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(1H-pyrrol-1-yl)benzyl]benzamide
0.000243
-
IC50: 243 nM Plasmodium falciparum N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]pyrazine-2-carboxamide
0.000289
-
IC50: 289 nM Plasmodium falciparum N-(4-[benzyl(methyl)amino]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
0.000334
-
IC50: 334 nM Plasmodium falciparum N-[4-(1,3-benzodioxol-5-yl)benzyl]-4-pentyl-N-(2-piperidin-1-ylethyl)benzamide
0.000334
-
IC50: 334 nM Plasmodium falciparum N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-[benzyl(2-hydroxyethyl)amino]ethyl)-4-pentylbenzamide
0.000369
-
IC50: 369 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-piperidin-1-ylbenzyl)benzamide
0.000374
-
IC50: 374 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-3-ylbenzyl)benzamide
0.00038
-
IC50: 380 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyridin-2-ylbenzyl)benzamide
0.000429
-
IC50: 429 nM Plasmodium falciparum N-[4-(benzylamino)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
0.000437
-
IC50: 437 nM Plasmodium falciparum N-(4-[6-(1,3-benzodioxol-5-yl)pyridin-3-yl]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
0.000439
-
IC50: 439 nM Plasmodium falciparum N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-([2-(diethylamino)ethyl](ethyl)amino)ethyl)-4-pentylbenzamide
0.000463
-
IC50: 463 nM Plasmodium falciparum [4'-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)biphenyl-4-yl]acetic acid
0.000464
-
IC50: 464 nM Plasmodium falciparum N-[4-(([2-(dibutylamino)ethyl][(4-pentylphenyl)carbonyl]amino)methyl)phenyl]piperidine-4-carboxamide
0.000511
-
IC50: 511 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-N-([4'-(2-hydroxyethoxy)biphenyl-4-yl]methyl)-4-pentylbenzamide
0.000531
-
IC50: 531 nM Plasmodium falciparum N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(dipropylamino)ethyl]-4-pentylbenzamide
0.000531
-
IC50: 531 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-4-pentyl-N-(4-pyrimidin-5-ylbenzyl)benzamide
0.000574
-
IC50: 574 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-N-(4-[methyl(phenyl)amino]benzyl)-4-pentylbenzamide
0.000587
-
IC50: 587 nM Plasmodium falciparum N-[4-(2,2'-bipyridin-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
0.000589
-
IC50: 589 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(6-phenylpyridin-3-yl)benzyl]benzamide
0.000642
-
IC50: 642 nM Plasmodium falciparum N-[4-(2,4'-bipyridin-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
0.000646
-
IC50: 646 nM Plasmodium falciparum N-[4-(4-benzylpiperazin-1-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
0.00067
-
IC50: 670 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-N-[4-(1H-indol-1-yl)benzyl]-4-pentylbenzamide
0.000736
-
IC50: 736 nM Plasmodium falciparum N-[4-(2,2'-bipyridin-5-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
0.001491
-
IC50: 1491 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-N-[4-(diethylamino)benzyl]-4-pentylbenzamide
0.001501
-
IC50: 1501 nM Plasmodium falciparum N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-[bis(1-methylethyl)amino]ethyl)-4-pentylbenzamide
0.001519
-
IC50: 1519 nM Plasmodium falciparum N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-[2-(diethylamino)ethyl]-4-pentylbenzamide
0.001816
-
IC50: 1816 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(pyridin-4-ylamino)benzyl]benzamide
0.001912
-
IC50: 1912 nM Plasmodium falciparum N-(4-[5-(1,3-benzodioxol-5-yl)pyridin-2-yl]benzyl)-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
0.002229
-
IC50: 2229 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(6-pyrimidin-5-ylpyridin-3-yl)benzyl]benzamide
0.002345
-
IC50: 2345 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(5-phenylpyridin-2-yl)benzyl]benzamide
0.002547
-
IC50: 2547 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-N-[4-(4-methylpiperazin-1-yl)benzyl]-4-pentylbenzamide
0.002897
-
IC50: 2897 nM Plasmodium falciparum N-[4-(1,3-benzodioxol-5-yl)benzyl]-N-(2-morpholin-4-ylethyl)-4-pentylbenzamide
0.003015
-
IC50: 3015 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-N-(4-[methyl(pyridin-4-yl)amino]benzyl)-4-pentylbenzamide
0.004553
-
IC50: 4553 nM Plasmodium falciparum N-[4-(3,4'-bipyridin-6-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
0.005266
-
IC50: 5266 nM Plasmodium falciparum N-[4-(3,3'-bipyridin-6-yl)benzyl]-N-[2-(dibutylamino)ethyl]-4-pentylbenzamide
0.00853
-
IC50: 8530 nM Plasmodium falciparum N-[2-(dibutylamino)ethyl]-4-pentyl-N-[4-(5-pyrimidin-5-ylpyridin-2-yl)benzyl]benzamide