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Literature summary for 1.5.1.33 extracted from

  • Tulloch, L.B.; Martini, V.P.; Iulek, J.; Huggan, J.K.; Lee, J.H.; Gibson, C.L.; Smith, T.K.; Suckling, C.J.; Hunter, W.N.
    Structure-based design of pteridine reductase inhibitors targeting African sleeping sickness and the leishmaniases (2010), J. Med. Chem., 53, 221-229.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
recombinantly expressed Leishmania major
recombinantly expressed Trypanosoma brucei

Inhibitors

Inhibitors Comment Organism Structure
2-amino-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one
-
Leishmania major
2-amino-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one
-
Trypanosoma brucei
2-amino-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidine-4-thione
-
Leishmania major
2-amino-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidine-4-thione
-
Trypanosoma brucei
2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
Leishmania major
2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
Trypanosoma brucei
2-amino-4-oxo-6-phenyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
Leishmania major
2-amino-4-oxo-6-phenyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
Trypanosoma brucei
2-amino-5-(2-phenylethyl)-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one
-
Leishmania major
2-amino-5-(2-phenylethyl)-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one
-
Trypanosoma brucei
2-amino-6-(1,3-benzodioxol-5-yl)-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
Leishmania major
2-amino-6-(1,3-benzodioxol-5-yl)-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
Trypanosoma brucei
2-amino-6-(3-formylphenyl)-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
Leishmania major
2-amino-6-(3-formylphenyl)-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
Trypanosoma brucei
2-amino-6-(4-ethylphenyl)-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
Leishmania major
2-amino-6-(4-ethylphenyl)-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
Trypanosoma brucei
2-amino-6-(4-methoxyphenyl)-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
Leishmania major
2-amino-6-(4-methoxyphenyl)-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
Trypanosoma brucei
2-amino-6-bromo-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
Leishmania major
2-amino-6-bromo-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
Trypanosoma brucei
6,7-di(propan-2-yl)pteridine-2,4-diamine
-
Leishmania major
6,7-di(propan-2-yl)pteridine-2,4-diamine
-
Trypanosoma brucei
6-(benzylsulfanyl)pyrimidine-2,4-diamine
-
Leishmania major
6-(benzylsulfanyl)pyrimidine-2,4-diamine
-
Trypanosoma brucei
6-methyl-7-(propan-2-yl)pteridine-2,4-diamine
-
Leishmania major
6-methyl-7-(propan-2-yl)pteridine-2,4-diamine
-
Trypanosoma brucei
6-phenylpteridine-2,4,7-triamine
-
Leishmania major
6-phenylpteridine-2,4,7-triamine
-
Trypanosoma brucei
6-[(4-methoxybenzyl)sulfanyl]pyrimidine-2,4-diamine
-
Leishmania major
6-[(4-methoxybenzyl)sulfanyl]pyrimidine-2,4-diamine
-
Trypanosoma brucei
6-[(4-methylphenyl)sulfanyl]pyrimidine-2,4-diamine
-
Leishmania major
6-[(4-methylphenyl)sulfanyl]pyrimidine-2,4-diamine
-
Trypanosoma brucei
N4-cyclopropylpyrimidine-2,4,6-triamine
-
Leishmania major
N4-cyclopropylpyrimidine-2,4,6-triamine
-
Trypanosoma brucei
pyrimidine-2,4,6-triamine
-
Leishmania major
pyrimidine-2,4,6-triamine
-
Trypanosoma brucei

Organism

Organism UniProt Comment Textmining
Leishmania major
-
-
-
Trypanosoma brucei Q581W1
-
-

Synonyms

Synonyms Comment Organism
LmPTR1
-
Leishmania major
pteridine reductase 1
-
Leishmania major
pteridine reductase 1
-
Trypanosoma brucei
TbPTR1
-
Trypanosoma brucei

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Leishmania major
7.5
-
assay at Trypanosoma brucei

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00024
-
6,7-di(propan-2-yl)pteridine-2,4-diamine pH 7.5, temperature not specified in the publication Leishmania major
0.00029
-
2-amino-6-(3-formylphenyl)-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile pH 7.5, temperature not specified in the publication Trypanosoma brucei
0.00036
-
2-amino-6-(4-methoxyphenyl)-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile pH 7.5, temperature not specified in the publication Trypanosoma brucei
0.0004
-
2-amino-6-(1,3-benzodioxol-5-yl)-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile pH 7.5, temperature not specified in the publication Trypanosoma brucei
0.0005
-
2-amino-6-(4-ethylphenyl)-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile pH 7.5, temperature not specified in the publication Trypanosoma brucei
0.0006
-
6-(benzylsulfanyl)pyrimidine-2,4-diamine pH 7.5, temperature not specified in the publication Leishmania major
0.00071
-
2-amino-4-oxo-6-phenyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile pH 7.5, temperature not specified in the publication Trypanosoma brucei
0.00096
-
2-amino-5-(2-phenylethyl)-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one pH 7.5, temperature not specified in the publication Trypanosoma brucei
0.0012
-
6-phenylpteridine-2,4,7-triamine pH 7.5, temperature not specified in the publication Trypanosoma brucei
0.0012
-
6-methyl-7-(propan-2-yl)pteridine-2,4-diamine pH 7.5, temperature not specified in the publication Leishmania major
0.0026
-
2-amino-6-(1,3-benzodioxol-5-yl)-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile pH 7.5, temperature not specified in the publication Leishmania major
0.0027
-
6-[(4-methoxybenzyl)sulfanyl]pyrimidine-2,4-diamine pH 7.5, temperature not specified in the publication Leishmania major
0.0032
-
6-(benzylsulfanyl)pyrimidine-2,4-diamine pH 7.5, temperature not specified in the publication Trypanosoma brucei
0.0033
-
6,7-di(propan-2-yl)pteridine-2,4-diamine pH 7.5, temperature not specified in the publication Trypanosoma brucei
0.0034
-
6-phenylpteridine-2,4,7-triamine pH 7.5, temperature not specified in the publication Leishmania major
0.0034
-
2-amino-6-(4-methoxyphenyl)-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile pH 7.5, temperature not specified in the publication Leishmania major
0.0039
-
2-amino-6-bromo-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile pH 7.5, temperature not specified in the publication Trypanosoma brucei
0.0042
-
2-amino-6-(3-formylphenyl)-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile pH 7.5, temperature not specified in the publication Leishmania major
0.0054
-
6-[(4-methylphenyl)sulfanyl]pyrimidine-2,4-diamine pH 7.5, temperature not specified in the publication Trypanosoma brucei
0.0058
-
2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile pH 7.5, temperature not specified in the publication Trypanosoma brucei
0.0164
-
2-amino-6-(4-ethylphenyl)-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile pH 7.5, temperature not specified in the publication Leishmania major
0.018
-
6-[(4-methoxybenzyl)sulfanyl]pyrimidine-2,4-diamine pH 7.5, temperature not specified in the publication Trypanosoma brucei
0.027
-
2-amino-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one pH 7.5, temperature not specified in the publication, value above 0.027 Leishmania major
0.027
-
2-amino-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidine-4-thione pH 7.5, temperature not specified in the publication, value above 0.027 Leishmania major
0.027
-
2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile pH 7.5, temperature not specified in the publication, value above 0.027 Leishmania major
0.027
-
2-amino-5-(2-phenylethyl)-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one pH 7.5, temperature not specified in the publication, value above 0.027 Leishmania major
0.027
-
2-amino-6-bromo-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile pH 7.5, temperature not specified in the publication, value above 0.027 Leishmania major
0.027
-
2-amino-4-oxo-6-phenyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile pH 7.5, temperature not specified in the publication, value above 0.027 Leishmania major
0.027
-
pyrimidine-2,4,6-triamine pH 7.5, temperature not specified in the publication, value above 0.027 Leishmania major
0.027
-
N4-cyclopropylpyrimidine-2,4,6-triamine pH 7.5, temperature not specified in the publication, value above 0.027 Leishmania major
0.027
-
6-[(4-methylphenyl)sulfanyl]pyrimidine-2,4-diamine pH 7.5, temperature not specified in the publication, value above 0.027 Leishmania major
0.035
-
6-methyl-7-(propan-2-yl)pteridine-2,4-diamine pH 7.5, temperature not specified in the publication, value above 0.035 Trypanosoma brucei
0.035
-
2-amino-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one pH 7.5, temperature not specified in the publication, value above 0.035 Trypanosoma brucei
0.035
-
2-amino-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidine-4-thione pH 7.5, temperature not specified in the publication, value above 0.035 Trypanosoma brucei
0.035
-
pyrimidine-2,4,6-triamine pH 7.5, temperature not specified in the publication, value above 0.035 Trypanosoma brucei
0.035
-
N4-cyclopropylpyrimidine-2,4,6-triamine pH 7.5, temperature not specified in the publication, value above 0.035 Trypanosoma brucei