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Literature summary for 1.5.1.3 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

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

Organism

Organism UniProt Comment Textmining
Homo sapiens P00374
-
-
Trypanosoma cruzi Q27793
-
-

Synonyms

Synonyms Comment Organism
DHFR
-
Homo sapiens
DHFR
-
Trypanosoma cruzi
dihydrofolate reductase
-
Homo sapiens
dihydrofolate reductase
-
Trypanosoma cruzi

Temperature Optimum [°C]

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

pH Optimum

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

Ki Value [mM]

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

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