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Literature summary extracted from

  • Schormann, N.; Velu, S.E.; Murugesan, S.; Senkovich, O.; Walker, K.; Chenna, B.C.; Shinkre, B.; Desai, A.; Chattopadhyay, D.
    Synthesis and characterization of potent inhibitors of Trypanosoma cruzi dihydrofolate reductase (2010), Bioorg. Med. Chem., 18, 4056-4066.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.5.1.3 4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoic acid
-
 Homo sapiens
1.5.1.3 4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoic acid
-
 Trypanosoma cruzi
1.5.1.3 5-(5-[[(2,4-diamino-6-quinazolinyl)methyl](propyl)amino]-2-methoxyphenoxy) pentanoate
-
 Homo sapiens
1.5.1.3 5-(5-[[(2,4-diamino-6-quinazolinyl)methyl](propyl)amino]-2-methoxyphenoxy) pentanoate
-
 Trypanosoma cruzi
1.5.1.3 6-[(3,4-dimethoxyanilino)methyl]-2,4-quinazolinediamine
-
 Homo sapiens
1.5.1.3 6-[(3,4-dimethoxyanilino)methyl]-2,4-quinazolinediamine
-
 Trypanosoma cruzi
1.5.1.3 ethyl 4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoate
-
 Homo sapiens
1.5.1.3 ethyl 4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoate
-
 Trypanosoma cruzi
1.5.1.3 methyl 4-[(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) methyl]benzene carboxylate
-
 Homo sapiens
1.5.1.3 methyl 4-[(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) methyl]benzene carboxylate
-
 Trypanosoma cruzi
1.5.1.3 methyl 5-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) pentanoate
-
 Homo sapiens
1.5.1.3 methyl 5-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) pentanoate
-
 Trypanosoma cruzi

Organism

EC Number Organism UniProt Comment Textmining
1.5.1.3 Homo sapiens P00374
-
-
1.5.1.3 Trypanosoma cruzi Q27793
-
-

Synonyms

EC Number Synonyms Comment Organism
1.5.1.3 DHFR
-
 Homo sapiens
1.5.1.3 DHFR
-
 Trypanosoma cruzi
1.5.1.3 dihydrofolate reductase
-
 Homo sapiens
1.5.1.3 dihydrofolate reductase
-
 Trypanosoma cruzi

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.5.1.3 22.6
-
 assay at Homo sapiens
1.5.1.3 22.6
-
 assay at Trypanosoma cruzi

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.5.1.3 7
-
 assay at Trypanosoma cruzi
1.5.1.3 7.3
-
 assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.5.1.3 0.0000013
-
 ethyl 4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoate pH 7, 22.6°C Trypanosoma cruzi
1.5.1.3 0.0000016
-
 6-[(3,4-dimethoxyanilino)methyl]-2,4-quinazolinediamine pH 7, 22.6°C Trypanosoma cruzi
1.5.1.3 0.0000016
-
 methyl 5-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) pentanoate pH 7, 22.6°C Trypanosoma cruzi
1.5.1.3 0.0000033
-
 methyl 4-[(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) methyl]benzene carboxylate pH 7, 22.6°C Trypanosoma cruzi
1.5.1.3 0.0000036
-
 4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoic acid pH 7, 22.6°C Trypanosoma cruzi
1.5.1.3 0.0000096
-
 ethyl 4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoate pH 7.3, 22.6°C Homo sapiens
1.5.1.3 0.0000118
-
 6-[(3,4-dimethoxyanilino)methyl]-2,4-quinazolinediamine pH 7.3, 22.6°C Homo sapiens
1.5.1.3 0.000013
-
 methyl 5-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) pentanoate pH 7.3, 22.6°C Homo sapiens
1.5.1.3 0.000024
-
 5-(5-[[(2,4-diamino-6-quinazolinyl)methyl](propyl)amino]-2-methoxyphenoxy) pentanoate pH 7, 22.6°C Trypanosoma cruzi
1.5.1.3 0.000024
-
 methyl 4-[(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) methyl]benzene carboxylate pH 7.3, 22.6°C Homo sapiens
1.5.1.3 0.000049
-
 4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoic acid pH 7.3, 22.6°C Homo sapiens
1.5.1.3 0.000188
-
 5-(5-[[(2,4-diamino-6-quinazolinyl)methyl](propyl)amino]-2-methoxyphenoxy) pentanoate pH 7.3, 22.6°C Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.5.1.3 0.0000238
-
 pH 7, 22.6°C Trypanosoma cruzi ethyl 4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoate
1.5.1.3 0.000027
-
 pH 7, 22.6°C Trypanosoma cruzi methyl 5-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) pentanoate
1.5.1.3 0.0000271
-
 pH 7, 22.6°C Trypanosoma cruzi 6-[(3,4-dimethoxyanilino)methyl]-2,4-quinazolinediamine
1.5.1.3 0.0000575
-
 pH 7, 22.6°C Trypanosoma cruzi methyl 4-[(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) methyl]benzene carboxylate
1.5.1.3 0.000061
-
 pH 7, 22.6°C Trypanosoma cruzi 4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoic acid
1.5.1.3 0.0000683
-
 pH 7.3, 22.6°C Homo sapiens ethyl 4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoate
1.5.1.3 0.0000855
-
 pH 7.3, 22.6°C Homo sapiens 6-[(3,4-dimethoxyanilino)methyl]-2,4-quinazolinediamine
1.5.1.3 0.0000935
-
 pH 7.3, 22.6°C Homo sapiens methyl 5-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) pentanoate
1.5.1.3 0.000174
-
 pH 7.3, 22.6°C Homo sapiens methyl 4-[(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) methyl]benzene carboxylate
1.5.1.3 0.000356
-
 pH 7.3, 22.6°C Homo sapiens 4-(5-[(2,4-diamino-6-quinazolinyl)methyl]amino-2-methoxyphenoxy) butanoic acid
1.5.1.3 0.000422
-
 pH 7, 22.6°C Trypanosoma cruzi 5-(5-[[(2,4-diamino-6-quinazolinyl)methyl](propyl)amino]-2-methoxyphenoxy) pentanoate
1.5.1.3 0.001338
-
 pH 7.3, 22.6°C Homo sapiens 5-(5-[[(2,4-diamino-6-quinazolinyl)methyl](propyl)amino]-2-methoxyphenoxy) pentanoate