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Literature summary for 1.5.1.3 extracted from

  • Kamchonwongpaisan, S.; Vanichtanankul, J.; Tarnchompoo, B.; Yuvaniyama, J.; Taweechai, S.; Yuthavong, Y.
    Stoichiometric selection of tight-binding inhibitors by wild-type and mutant forms of malarial (Plasmodium falciparum) dihydrofolate reductase (2005), Anal. Chem., 77, 1222-1227.
    View publication on PubMed

Application

Application Comment Organism
biotechnology method for screening combinatorial or other libraries of enzyme based on affinities of the inhibitors with the enzyme Homo sapiens
biotechnology method for screening combinatorial or other libraries of Plasmodium falciparum enzyme based on affinities of the inhibitors with the enzyme Plasmodium falciparum

Protein Variants

Protein Variants Comment Organism
C59R/S108N mutant with increased resistance to anitfolate antimalarials, use for screening inhibitors Plasmodium falciparum
N51I/C59R/S108N/I164L mutant with increased resistance to anitfolate antimalarials, use for screening inhibitors Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
5-(3,4-dichlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
Homo sapiens
5-(3,4-dichlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
Plasmodium falciparum
5-(3-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
Homo sapiens
5-(3-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
Plasmodium falciparum
5-(4-bromophenyl)-6-ethylpyrimidine-2,4-diamine
-
Homo sapiens
5-(4-bromophenyl)-6-ethylpyrimidine-2,4-diamine
-
Plasmodium falciparum
5-(4-chlorophenyl)-6-(4-methoxyphenyl)pyrimidine-2,4-diamine
-
Homo sapiens
5-(4-chlorophenyl)-6-(4-methoxyphenyl)pyrimidine-2,4-diamine
-
Plasmodium falciparum
5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
Homo sapiens
5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine
-
Plasmodium falciparum
5-(4-chlorophenyl)-6-isobutylpyrimidine-2,4-diamine
-
Homo sapiens
5-(4-chlorophenyl)-6-isobutylpyrimidine-2,4-diamine
-
Plasmodium falciparum
5-(4-chlorophenyl)-6-isopropylpyrimidine-2,4-diamine
-
Homo sapiens
5-(4-chlorophenyl)-6-isopropylpyrimidine-2,4-diamine
-
Plasmodium falciparum
5-(4-chlorophenyl)-6-phenylpyrimidine-2,4-diamine very high Ki-value Homo sapiens
5-(4-chlorophenyl)-6-phenylpyrimidine-2,4-diamine
-
Plasmodium falciparum
5-(4-chlorophenyl)-6-propylpyrimidine-2,4-diamine
-
Homo sapiens
5-(4-chlorophenyl)-6-propylpyrimidine-2,4-diamine
-
Plasmodium falciparum
6-ethyl-5-(4-methoxyphenyl)pyrimidine-2,4-diamine
-
Homo sapiens
6-ethyl-5-(4-methoxyphenyl)pyrimidine-2,4-diamine
-
Plasmodium falciparum
methyl 4-(2,6-diamino-5-phenylpyrimidin-4-yl)butanoate
-
Homo sapiens
methyl 4-(2,6-diamino-5-phenylpyrimidin-4-yl)butanoate
-
Plasmodium falciparum
methyl 4-[2,6-diamino-5-(3-chlorophenyl)pyrimidin-4-yl]butanoate
-
Homo sapiens
methyl 4-[2,6-diamino-5-(3-chlorophenyl)pyrimidin-4-yl]butanoate
-
Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Plasmodium falciparum
-
-
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000003
-
5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Plasmodium falciparum
0.0000003
-
5-(4-bromophenyl)-6-ethylpyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Plasmodium falciparum
0.0000003
-
5-(4-chlorophenyl)-6-isopropylpyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Plasmodium falciparum
0.0000003
-
5-(3,4-dichlorophenyl)-6-ethylpyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Homo sapiens
0.0000003
-
5-(4-chlorophenyl)-6-isobutylpyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Plasmodium falciparum
0.0000005
-
methyl 4-[2,6-diamino-5-(3-chlorophenyl)pyrimidin-4-yl]butanoate wild-type, pH 7.0, 25°C Plasmodium falciparum
0.0000005
-
5-(4-chlorophenyl)-6-propylpyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Plasmodium falciparum
0.0000006
-
methyl 4-(2,6-diamino-5-phenylpyrimidin-4-yl)butanoate wild-type, pH 7.0, 25°C Plasmodium falciparum
0.0000008
-
5-(3-chlorophenyl)-6-ethylpyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Plasmodium falciparum
0.0000009
-
6-ethyl-5-(4-methoxyphenyl)pyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Plasmodium falciparum
0.000001
-
5-(3,4-dichlorophenyl)-6-ethylpyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Plasmodium falciparum
0.0000014
-
5-(3-chlorophenyl)-6-ethylpyrimidine-2,4-diamine mutant C59R/S108N, pH 7.0, 25°C Plasmodium falciparum
0.0000016
-
5-(3-chlorophenyl)-6-ethylpyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Homo sapiens
0.0000025
-
methyl 4-[2,6-diamino-5-(3-chlorophenyl)pyrimidin-4-yl]butanoate wild-type, pH 7.0, 25°C Homo sapiens
0.0000027
-
methyl 4-[2,6-diamino-5-(3-chlorophenyl)pyrimidin-4-yl]butanoate mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C Plasmodium falciparum
0.0000028
-
methyl 4-[2,6-diamino-5-(3-chlorophenyl)pyrimidin-4-yl]butanoate mutant C59R/S108N, pH 7.0, 25°C Plasmodium falciparum
0.0000029
-
5-(4-chlorophenyl)-6-phenylpyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Plasmodium falciparum
0.0000031
-
6-ethyl-5-(4-methoxyphenyl)pyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Homo sapiens
0.0000033
-
5-(3-chlorophenyl)-6-ethylpyrimidine-2,4-diamine mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C Plasmodium falciparum
0.0000043
-
5-(4-chlorophenyl)-6-(4-methoxyphenyl)pyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Plasmodium falciparum
0.0000055
-
methyl 4-(2,6-diamino-5-phenylpyrimidin-4-yl)butanoate mutant C59R/S108N, pH 7.0, 25°C Plasmodium falciparum
0.0000087
-
methyl 4-(2,6-diamino-5-phenylpyrimidin-4-yl)butanoate wild-type, pH 7.0, 25°C Homo sapiens
0.0000126
-
5-(3,4-dichlorophenyl)-6-ethylpyrimidine-2,4-diamine mutant C59R/S108N, pH 7.0, 25°C Plasmodium falciparum
0.0000153
-
5-(4-bromophenyl)-6-ethylpyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Homo sapiens
0.0000241
-
methyl 4-(2,6-diamino-5-phenylpyrimidin-4-yl)butanoate mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C Plasmodium falciparum
0.0000282
-
5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Homo sapiens
0.0000362
-
5-(4-chlorophenyl)-6-isopropylpyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Homo sapiens
0.0000443
-
5-(4-bromophenyl)-6-ethylpyrimidine-2,4-diamine mutant C59R/S108N, pH 7.0, 25°C Plasmodium falciparum
0.0000494
-
5-(4-chlorophenyl)-6-propylpyrimidine-2,4-diamine mutant C59R/S108N, pH 7.0, 25°C Plasmodium falciparum
0.0000519
-
5-(4-chlorophenyl)-6-propylpyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Homo sapiens
0.0000534
-
5-(3,4-dichlorophenyl)-6-ethylpyrimidine-2,4-diamine mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C Plasmodium falciparum
0.0000539
-
5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine mutant C59R/S108N, pH 7.0, 25°C Plasmodium falciparum
0.000086
-
6-ethyl-5-(4-methoxyphenyl)pyrimidine-2,4-diamine mutant C59R/S108N, pH 7.0, 25°C Plasmodium falciparum
0.000099
-
5-(4-chlorophenyl)-6-isobutylpyrimidine-2,4-diamine mutant C59R/S108N, pH 7.0, 25°C Plasmodium falciparum
0.000113
-
5-(4-chlorophenyl)-6-isopropylpyrimidine-2,4-diamine mutant C59R/S108N, pH 7.0, 25°C Plasmodium falciparum
0.0001291
-
5-(4-chlorophenyl)-6-isobutylpyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Homo sapiens
0.0002473
-
5-(4-chlorophenyl)-6-(4-methoxyphenyl)pyrimidine-2,4-diamine wild-type, pH 7.0, 25°C Homo sapiens
0.000303
-
5-(4-bromophenyl)-6-ethylpyrimidine-2,4-diamine mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C Plasmodium falciparum
0.000359
-
5-(4-chlorophenyl)-6-propylpyrimidine-2,4-diamine mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C Plasmodium falciparum
0.000385
-
5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C Plasmodium falciparum
0.000541
-
5-(4-chlorophenyl)-6-isopropylpyrimidine-2,4-diamine mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C Plasmodium falciparum
0.0006
-
5-(4-chlorophenyl)-6-phenylpyrimidine-2,4-diamine mutant C59R/S108N, pH 7.0, 25°C Plasmodium falciparum
0.000617
-
6-ethyl-5-(4-methoxyphenyl)pyrimidine-2,4-diamine mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C Plasmodium falciparum
0.000742
-
5-(4-chlorophenyl)-6-(4-methoxyphenyl)pyrimidine-2,4-diamine mutant C59R/S108N, pH 7.0, 25°C Plasmodium falciparum
0.000798
-
5-(4-chlorophenyl)-6-isobutylpyrimidine-2,4-diamine mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C Plasmodium falciparum
0.001576
-
5-(4-chlorophenyl)-6-(4-methoxyphenyl)pyrimidine-2,4-diamine mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C Plasmodium falciparum
0.003461
-
5-(4-chlorophenyl)-6-phenylpyrimidine-2,4-diamine mutant N51I/C59R/S108N/I164L, pH 7.0, 25°C Plasmodium falciparum