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Literature summary for 1.5.1.3 extracted from

  • Zolli-Juran, M.; Cechetto, J.D.; Hartlen, R.; Daigle, D.M.; Brown, E.D.
    High throughput screening identifies novel inhibitors of Escherichia coli dihydrofolate reductase that are competitive with dihydrofolate (2003), Bioorg. Med. Chem. Lett., 13, 2493-2496.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1,6-bis-(4-fluoro-phenyl)-[1,3,5]triazine-2,4-diamine IC50: 0.011 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli
3-heptyl-4-hydroxy-1H-naphthalen-2-one IC50: 0.48 mM, 0.03 mM 7,8-dihydrofolate Escherichia coli
5-(3,4,5-trimethoxy-benzyl)-pyrimidine-2,4-diamine IC50: 18 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli
6,7-dimethyl-5,6,7,8-tetrahydro-quinazoline-2,4-diamine IC50: 790 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli
6-(4-trifluoromethyl-phenoxy)-quinazoline-2,4-diamine IC50: 660 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli
6-p-tolyloxy-quinazoline-2,4-diamine IC50: 190 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli
6-p-tolylsulfanyl-quinazoline-2,4-diamine IC50: 310 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli
7-methyl-5,6,7,8-tetrahydro-quinazoline-2,4-diamine IC50: 0.011 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli
N-(4-chloro-2-cyanophenyl)imidodicarbonimidic diamide IC50: 320 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli
[amino-(4-[[(amino-thioureido-methyl)-amino]-methyl]-2,5-dimethyl-benzylamino)-methyl]-thiourea IC50: 109 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7,8-dihydrofolate + NADPH
-
Escherichia coli 5,6,7,8-tetrahydrofolate + NADP+
-
?

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000000011
-
IC50: 0.011 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli 7-methyl-5,6,7,8-tetrahydro-quinazoline-2,4-diamine
0.000000011
-
IC50: 0.011 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli 1,6-bis-(4-fluoro-phenyl)-[1,3,5]triazine-2,4-diamine
0.000018
-
IC50: 18 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli 5-(3,4,5-trimethoxy-benzyl)-pyrimidine-2,4-diamine
0.000109
-
IC50: 109 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli [amino-(4-[[(amino-thioureido-methyl)-amino]-methyl]-2,5-dimethyl-benzylamino)-methyl]-thiourea
0.00019
-
IC50: 190 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli 6-p-tolyloxy-quinazoline-2,4-diamine
0.00031
-
IC50: 310 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli 6-p-tolylsulfanyl-quinazoline-2,4-diamine
0.00032
-
IC50: 320 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli N-(4-chloro-2-cyanophenyl)imidodicarbonimidic diamide
0.00066
-
IC50: 660 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli 6-(4-trifluoromethyl-phenoxy)-quinazoline-2,4-diamine
0.00079
-
IC50: 790 nM, 0.03 mM 7,8-dihydrofolate Escherichia coli 6,7-dimethyl-5,6,7,8-tetrahydro-quinazoline-2,4-diamine
0.48
-
IC50: 0.48 mM, 0.03 mM 7,8-dihydrofolate Escherichia coli 3-heptyl-4-hydroxy-1H-naphthalen-2-one