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Literature summary for 1.5.1.3 extracted from

  • Khabnadideh, S.; Pez, D.; Musso, A.; Brun, R.; Perez, L.M.; Gonzalez-Pacanowska, D.; Gilbert, I.H.
    Design, synthesis and evaluation of 2,4-diaminoquinazolines as inhibitors of trypanosomal and leishmanial dihydrofolate reductase (2005), Bioorg. Med. Chem., 13, 2637-2649.
    View publication on PubMed
Search for more literature for 1.5.1.3

Inhibitors

Inhibitors Comment Organism Structure
4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]phenol 50% inhibition at 0.00165 mM Homo sapiens
4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]phenol 50% inhibition at 0.0799 mM Leishmania donovani
4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]phenol 50% inhibition at 0.000034 mM Leishmania major
4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]phenol 50% inhibition at 0.000054 mM Trypanosoma brucei rhodesiense
4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]phenol 50% inhibition at 0.000078 mM Trypanosoma cruzi
6-(2-[4-(benzyloxy)phenyl]ethyl)quinazoline-2,4-diamine 50% inhibition at 0.00185 mM Homo sapiens
6-(2-[4-(benzyloxy)phenyl]ethyl)quinazoline-2,4-diamine 50% inhibition at 0.0138 mM Leishmania donovani
6-(2-[4-(benzyloxy)phenyl]ethyl)quinazoline-2,4-diamine 50% inhibition at 0.00012 mM Leishmania major
6-(2-[4-(benzyloxy)phenyl]ethyl)quinazoline-2,4-diamine 50% inhibition at 0.0001 mM Trypanosoma brucei rhodesiense
6-(2-[4-(benzyloxy)phenyl]ethyl)quinazoline-2,4-diamine 50% inhibition at 0.000059 mM Trypanosoma cruzi
6-[2-(4-butoxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.00204 mM Homo sapiens
6-[2-(4-butoxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.0017 mM Leishmania donovani
6-[2-(4-butoxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.000044 mM Leishmania major
6-[2-(4-butoxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.00023mM Trypanosoma brucei rhodesiense
6-[2-(4-butoxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.000042 mM Trypanosoma cruzi
6-[2-(4-ethoxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.00234 mM Homo sapiens
6-[2-(4-ethoxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.002 mM Leishmania donovani
6-[2-(4-ethoxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.00018 mM Leishmania major
6-[2-(4-ethoxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.000081 mM Trypanosoma brucei rhodesiense
6-[2-(4-ethoxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.000041 mM Trypanosoma cruzi
6-[2-(4-hexoxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.00347 mM Homo sapiens
6-[2-(4-hexoxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.0021 mM Leishmania donovani
6-[2-(4-hexoxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.000177 mM Leishmania major
6-[2-(4-hexoxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.000095 mM Trypanosoma brucei rhodesiense
6-[2-(4-hexoxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.00011 mM Trypanosoma cruzi
6-[2-(4-octyloxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.01289 mM Homo sapiens
6-[2-(4-octyloxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.002 mM Leishmania donovani
6-[2-(4-octyloxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.000123 mM Leishmania major
6-[2-(4-octyloxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.00035 mM Trypanosoma brucei rhodesiense
6-[2-(4-octyloxyphenyl)ethyl]quinazoline-2,4-diamine 50% inhibition at 0.00022 mM Trypanosoma cruzi

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Leishmania donovani
-
-
-
Leishmania major
-
-
-
Trypanosoma brucei rhodesiense
-
-
-
Trypanosoma cruzi
-
-
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000014
-
 4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]phenol pH 7.0, 25°C Leishmania major
0.0000019
-
 6-[2-(4-butoxyphenyl)ethyl]quinazoline-2,4-diamine pH 7.0, 25°C Leishmania major
0.0000052
-
 6-(2-[4-(benzyloxy)phenyl]ethyl)quinazoline-2,4-diamine pH 7.0, 25°C Leishmania major
0.0000053
-
 6-[2-(4-octyloxyphenyl)ethyl]quinazoline-2,4-diamine pH 7.0, 25°C Leishmania major
0.0000076
-
 6-[2-(4-hexoxyphenyl)ethyl]quinazoline-2,4-diamine pH 7.0, 25°C Leishmania major
0.0000078
-
 6-[2-(4-ethoxyphenyl)ethyl]quinazoline-2,4-diamine pH 7.0, 25°C Leishmania major
0.000034
-
 4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]phenol pH 7.0, 25°C Homo sapiens
0.000038
-
 6-(2-[4-(benzyloxy)phenyl]ethyl)quinazoline-2,4-diamine pH 7.0, 25°C Homo sapiens
0.000042
-
 6-[2-(4-butoxyphenyl)ethyl]quinazoline-2,4-diamine pH 7.0, 25°C Homo sapiens
0.000048
-
 6-[2-(4-ethoxyphenyl)ethyl]quinazoline-2,4-diamine pH 7.0, 25°C Homo sapiens
0.000072
-
 6-[2-(4-hexoxyphenyl)ethyl]quinazoline-2,4-diamine pH 7.0, 25°C Homo sapiens
0.000269
-
 6-[2-(4-octyloxyphenyl)ethyl]quinazoline-2,4-diamine pH 7.0, 25°C Homo sapiens