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Literature summary for 3.4.11.18 extracted from

  • Chen, X.; Chong, C.R.; Shi, L.; Yoshimoto, T.; Sullivan, D.J.; Liu, J.O.
    Inhibitors of Plasmodium falciparum methionine aminopeptidase 1b possess antimalarial activity (2006), Proc. Natl. Acad. Sci. USA, 103, 14548-14553.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(2-sulfanylmorpholin-4-yl)ethanone
-
Plasmodium falciparum
1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(2-sulfanylphenyl)ethanone
-
Plasmodium falciparum
1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(4-fluoro-2-sulfanylphenyl)ethanone
-
Plasmodium falciparum
1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(4-methoxy-2-sulfanylphenyl)ethanone
-
Plasmodium falciparum
1-[2-pyridin-2-yl-6-(trifluoromethyl)-3,4-dihydropyrimidin-4-yl]propane-2-thiol
-
Plasmodium falciparum
2-pyridin-2-yl-4-(trifluoromethyl)-6-[2-(trifluoromethyl)benzyl]-1,6-dihydropyrimidine
-
Plasmodium falciparum
4-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)morpholine
-
Plasmodium falciparum
4-(5-methoxy-2-phenyl-3,4-dihydropyrimidin-4-yl)morpholine
-
Plasmodium falciparum
4-(5-methoxy-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)morpholine
-
Plasmodium falciparum
5-chloro-4,6-dimethyl-2-pyridin-2-yl-1,6-dihydropyrimidine
-
Plasmodium falciparum
5-chloro-4-methyl-2-pyridin-2-yl-6-pyrrolidin-1-yl-1,6-dihydropyrimidine
-
Plasmodium falciparum
5-chloro-4-methyl-6-(4-methylbenzyl)-2-pyridin-2-yl-1,6-dihydropyrimidine
-
Plasmodium falciparum
5-chloro-6-(2-ethylphenyl)-4-methyl-2-pyridin-2-yl-1,6-dihydropyrimidine highly selective inhibitor Plasmodium falciparum
5-methoxy-2-phenyl-6-pyrrolidin-1-yl-1,6-dihydropyrimidine
-
Plasmodium falciparum
5-methoxy-2-pyridin-2-yl-3,4-dihydropyrimidin-4-ol
-
Plasmodium falciparum
5-methoxy-2-pyridin-2-yl-6-pyrrolidin-1-yl-1,6-dihydropyrimidine
-
Plasmodium falciparum
5-methoxy-6,6-dimethyl-2-pyridin-2-yl-1,6-dihydropyrimidine
-
Plasmodium falciparum
5-methoxy-6-methyl-2-phenyl-1,6-dihydropyrimidine
-
Plasmodium falciparum
5-methoxy-6-methyl-6-phenyl-2-pyridin-2-yl-1,6-dihydropyrimidine
-
Plasmodium falciparum
5-methoxy-6-[(4-methoxyphenyl)sulfanyl]-2-pyridin-2-yl-1,6-dihydropyrimidine
-
Plasmodium falciparum
6-(2-chlorobenzyl)-2-pyridin-2-yl-4-(trifluoromethyl)-1,6-dihydropyrimidine
-
Plasmodium falciparum
6-(benzylsulfanyl)-5-chloro-4-methyl-2-pyridin-2-yl-1,6-dihydropyrimidine
-
Plasmodium falciparum
6-(phenylsulfanyl)-2-pyridin-2-yl-4-(trifluoromethyl)-1,6-dihydropyrimidine
-
Plasmodium falciparum
6-benzyl-2-pyridin-2-yl-4-(trifluoromethyl)-1,6-dihydropyrimidine
-
Plasmodium falciparum
6-benzyl-5-chloro-4-methyl-2-pyridin-3-yl-1,6-dihydropyrimidine
-
Plasmodium falciparum
6-[(2,4-dichlorophenyl)sulfanyl]-5-methoxy-2-pyridin-2-yl-1,6-dihydropyrimidine
-
Plasmodium falciparum
6-[(4-methoxyphenyl)sulfanyl]-2-pyridin-2-yl-4-(trifluoromethyl)-1,6-dihydropyrimidine
-
Plasmodium falciparum
N-(2-aminoethyl)-N'-[5-chloro-6-methyl-2-pyridin-2-yl-4-[5-(trifluoromethyl)pyridin-2-yl]-3,4-dihydropyrimidin-4-yl]ethane-1,2-diamine
-
Plasmodium falciparum
N-(2-aminoethyl)-N'-[5-chloro-6-methyl-2-pyridin-3-yl-4-[5-(trifluoromethyl)pyridin-2-yl]-3,4-dihydropyrimidin-4-yl]ethane-1,2-diamine
-
Plasmodium falciparum
N-(2-aminoethyl)-N'-[5-chloro-6-methyl-2-pyridin-4-yl-4-[5-(trifluoromethyl)pyridin-2-yl]-3,4-dihydropyrimidin-4-yl]ethane-1,2-diamine
-
Plasmodium falciparum

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.3273
-
Met-peptide
-
Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
strains 3D7 and Dd2
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Met-peptide + H2O
-
Plasmodium falciparum Met + peptide
-
?

Synonyms

Synonyms Comment Organism
MetAP1b
-
Plasmodium falciparum
methionine aminopeptidase 1b
-
Plasmodium falciparum

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.232
-
Met-peptide
-
Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000112
-
-
Plasmodium falciparum 5-chloro-6-(2-ethylphenyl)-4-methyl-2-pyridin-2-yl-1,6-dihydropyrimidine
0.000152
-
-
Plasmodium falciparum 4-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)morpholine
0.000158
-
-
Plasmodium falciparum 5-chloro-4-methyl-6-(4-methylbenzyl)-2-pyridin-2-yl-1,6-dihydropyrimidine
0.000199
-
-
Plasmodium falciparum N-(2-aminoethyl)-N'-[5-chloro-6-methyl-2-pyridin-2-yl-4-[5-(trifluoromethyl)pyridin-2-yl]-3,4-dihydropyrimidin-4-yl]ethane-1,2-diamine
0.000521
-
-
Plasmodium falciparum 5-chloro-4-methyl-2-pyridin-2-yl-6-pyrrolidin-1-yl-1,6-dihydropyrimidine
0.000843
-
-
Plasmodium falciparum 5-chloro-4,6-dimethyl-2-pyridin-2-yl-1,6-dihydropyrimidine
0.000938
-
-
Plasmodium falciparum 6-(benzylsulfanyl)-5-chloro-4-methyl-2-pyridin-2-yl-1,6-dihydropyrimidine
0.00102
-
-
Plasmodium falciparum 1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(4-methoxy-2-sulfanylphenyl)ethanone
0.00104
-
-
Plasmodium falciparum 6-[(2,4-dichlorophenyl)sulfanyl]-5-methoxy-2-pyridin-2-yl-1,6-dihydropyrimidine
0.00106
-
-
Plasmodium falciparum 6-(2-chlorobenzyl)-2-pyridin-2-yl-4-(trifluoromethyl)-1,6-dihydropyrimidine
0.00106
-
-
Plasmodium falciparum 6-benzyl-2-pyridin-2-yl-4-(trifluoromethyl)-1,6-dihydropyrimidine
0.00107
-
-
Plasmodium falciparum 2-pyridin-2-yl-4-(trifluoromethyl)-6-[2-(trifluoromethyl)benzyl]-1,6-dihydropyrimidine
0.00111
-
-
Plasmodium falciparum 6-(phenylsulfanyl)-2-pyridin-2-yl-4-(trifluoromethyl)-1,6-dihydropyrimidine
0.00113
-
-
Plasmodium falciparum 5-methoxy-6-[(4-methoxyphenyl)sulfanyl]-2-pyridin-2-yl-1,6-dihydropyrimidine
0.00118
-
-
Plasmodium falciparum 1-[2-pyridin-2-yl-6-(trifluoromethyl)-3,4-dihydropyrimidin-4-yl]propane-2-thiol
0.00123
-
-
Plasmodium falciparum 6-[(4-methoxyphenyl)sulfanyl]-2-pyridin-2-yl-4-(trifluoromethyl)-1,6-dihydropyrimidine
0.00124
-
-
Plasmodium falciparum 1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(4-fluoro-2-sulfanylphenyl)ethanone
0.00154
-
-
Plasmodium falciparum 1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(2-sulfanylphenyl)ethanone
0.0017
-
-
Plasmodium falciparum 5-methoxy-6,6-dimethyl-2-pyridin-2-yl-1,6-dihydropyrimidine
0.00217
-
-
Plasmodium falciparum 5-methoxy-6-methyl-6-phenyl-2-pyridin-2-yl-1,6-dihydropyrimidine
0.00312
-
-
Plasmodium falciparum 1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(2-sulfanylmorpholin-4-yl)ethanone
0.00513
-
-
Plasmodium falciparum 4-(5-methoxy-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)morpholine
0.00791
-
-
Plasmodium falciparum 5-methoxy-2-pyridin-2-yl-6-pyrrolidin-1-yl-1,6-dihydropyrimidine
0.1
-
IC50 above 0.1 mM Plasmodium falciparum 4-(5-methoxy-2-phenyl-3,4-dihydropyrimidin-4-yl)morpholine
0.1
-
IC50 above 0.1 mM Plasmodium falciparum 5-methoxy-2-phenyl-6-pyrrolidin-1-yl-1,6-dihydropyrimidine
0.1
-
IC50 above 0.1 mM Plasmodium falciparum 5-methoxy-2-pyridin-2-yl-3,4-dihydropyrimidin-4-ol
0.1
-
IC50 above 0.1 mM Plasmodium falciparum 5-methoxy-6-methyl-2-phenyl-1,6-dihydropyrimidine
0.1
-
IC50 above 0.1 mM Plasmodium falciparum 6-benzyl-5-chloro-4-methyl-2-pyridin-3-yl-1,6-dihydropyrimidine
0.1
-
IC50 above 0.1 mM Plasmodium falciparum N-(2-aminoethyl)-N'-[5-chloro-6-methyl-2-pyridin-3-yl-4-[5-(trifluoromethyl)pyridin-2-yl]-3,4-dihydropyrimidin-4-yl]ethane-1,2-diamine
0.1
-
IC50 above 0.1 mM Plasmodium falciparum N-(2-aminoethyl)-N'-[5-chloro-6-methyl-2-pyridin-4-yl-4-[5-(trifluoromethyl)pyridin-2-yl]-3,4-dihydropyrimidin-4-yl]ethane-1,2-diamine