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Literature summary for 1.5.1.33 extracted from

  • Spinks, D.; Ong, H.B.; Mpamhanga, C.P.; Shanks, E.J.; Robinson, D.A.; Collie, I.T.; Read, K.D.; Frearson, J.A.; Wyatt, P.G.; Brenk, R.; Fairlamb, A.H.; Gilbert, I.H.
    Design, synthesis and biological evaluation of novel inhibitors of Trypanosoma brucei pteridine reductase 1 (2011), ChemMedChem, 6, 302-308.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(2-amino-2,3-dihydro-1H-benzimidazol-1-yl)(phenyl)methanone
-
Trypanosoma brucei
1-(2,5-dichlorobenzyl)-2,3-dihydro-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(2-chlorobenzyl)-2,3-dihydro-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(2-fluorobenzyl)-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(2-methylbenzyl)-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(2-phenylethyl)-2,3-dihydro-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(3,4-dichlorobenzyl)-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(3,4-dichlorobenzyl)-2,3-dihydro-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(3,4-dichlorobenzyl)-4-methoxy-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(3,4-dichlorobenzyl)-4-phenyl-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(3,4-dichlorobenzyl)-4-propoxy-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(3,4-dichlorobenzyl)-5,6-dimethyl-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(3,4-dichlorobenzyl)-7-methoxy-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(3,4-dichlorobenzyl)-7-phenyl-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(3,4-dichlorobenzyl)-7-propoxy-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(3,5-dichlorobenzyl)-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(3-chlorobenzyl)-2,3-dihydro-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(4-bromobenzyl)-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(4-chlorobenzyl)-2,3-dihydro-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(4-methylbenzyl)-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(4-tert-butylbenzyl)-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(naphthalen-1-ylmethyl)-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(naphthalen-2-ylmethyl)-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(pyridin-2-yl)-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-(pyridin-3-yl)-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-benzyl-2,3-dihydro-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-ethyl-2,3-dihydro-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1-[3-(trifluoromethyl)benzyl]-1H-benzimidazol-2-amine
-
Trypanosoma brucei
1H-benzimidazol-2-amine
-
Trypanosoma brucei
4-(benzyloxy)-1-(3,4-dichlorobenzyl)-1H-benzimidazol-2-amine
-
Trypanosoma brucei
4-chloro-1-(3,4-dichlorobenzyl)-1H-benzimidazol-2-amine
-
Trypanosoma brucei
7-(benzyloxy)-1-(3,4-dichlorobenzyl)-1H-benzimidazol-2-amine
-
Trypanosoma brucei
7-chloro-1-(3,4-dichlorobenzyl)-1H-benzimidazol-2-amine
-
Trypanosoma brucei

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
biopterin + 2 NADPH + 2 H+ Trypanosoma brucei
-
5,6,7,8-tetrahydrobiopterin + 2 NADP+
-
?

Organism

Organism UniProt Comment Textmining
Trypanosoma brucei
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
biopterin + 2 NADPH + 2 H+
-
Trypanosoma brucei 5,6,7,8-tetrahydrobiopterin + 2 NADP+
-
?

Synonyms

Synonyms Comment Organism
pteridine reductase 1
-
Trypanosoma brucei
PTR1
-
Trypanosoma brucei

Cofactor

Cofactor Comment Organism Structure
NADPH dependent on Trypanosoma brucei

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000007
-
1-(3,4-dichlorobenzyl)-7-phenyl-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.000047
-
1-(3,4-dichlorobenzyl)-7-propoxy-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.000098
-
7-(benzyloxy)-1-(3,4-dichlorobenzyl)-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.00031
-
1-(3,4-dichlorobenzyl)-4-propoxy-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.0004
-
1-(3,4-dichlorobenzyl)-2,3-dihydro-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.00046
-
1-(3,4-dichlorobenzyl)-4-methoxy-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.00051
-
7-chloro-1-(3,4-dichlorobenzyl)-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.00065
-
1-(3,4-dichlorobenzyl)-7-methoxy-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.0023
-
4-chloro-1-(3,4-dichlorobenzyl)-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.0028
-
1-(naphthalen-2-ylmethyl)-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.0031
-
1-(4-bromobenzyl)-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.0037
-
1-(2,5-dichlorobenzyl)-2,3-dihydro-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.0039
-
1-(3,4-dichlorobenzyl)-5,6-dimethyl-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.0042
-
1-(4-tert-butylbenzyl)-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.0054
-
1-(4-chlorobenzyl)-2,3-dihydro-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.0061
-
1-(naphthalen-1-ylmethyl)-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.0063
-
1-[3-(trifluoromethyl)benzyl]-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.0075
-
1-(3-chlorobenzyl)-2,3-dihydro-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.0088
-
1-(3,5-dichlorobenzyl)-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.01
-
1-(2-chlorobenzyl)-2,3-dihydro-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.015
-
1-(2-methylbenzyl)-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.015
-
1-(4-methylbenzyl)-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.016
-
1-benzyl-2,3-dihydro-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.016
-
4-(benzyloxy)-1-(3,4-dichlorobenzyl)-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.021
-
1-(2-fluorobenzyl)-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.024
-
1-(2-phenylethyl)-2,3-dihydro-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.053
-
1-(pyridin-2-yl)-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.054
-
1-(pyridin-3-yl)-1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei
0.06
-
(2-amino-2,3-dihydro-1H-benzimidazol-1-yl)(phenyl)methanone Ki above 0.06 mM, pH and temperature not specified in the publication Trypanosoma brucei
0.06
-
1-(3,4-dichlorobenzyl)-1H-benzimidazol-2-amine Ki above 0.06 mM, pH and temperature not specified in the publication Trypanosoma brucei
0.06
-
1-(3,4-dichlorobenzyl)-4-phenyl-1H-benzimidazol-2-amine Ki above 0.06 mM, pH and temperature not specified in the publication Trypanosoma brucei
0.2
-
1-ethyl-2,3-dihydro-1H-benzimidazol-2-amine Ki above 0.2 mM, pH and temperature not specified in the publication Trypanosoma brucei
0.228
-
1H-benzimidazol-2-amine pH and temperature not specified in the publication Trypanosoma brucei