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Literature summary for 1.8.1.9 extracted from

  • Andricopulo, A.D.; Akoachere, M.B.; Krogh, R.; Nickel, C.; McLeish, M.J.; Kenyon, G.L.; Arscott, L.D.; Williams, C.H.; Davioud-Charvet, E.; Becker, K.
    Specific inhibitors of Plasmodium falciparum thioredoxin reductase as potential antimalarial agents (2006), Bioorg. Med. Chem. Lett., 16, 2283-2292.
    View publication on PubMed
Search for more literature for 1.8.1.9

Application

Application Comment Organism
medicine potential drug target for malaria chemotherapy Homo sapiens
medicine potential drug target for malaria chemotherapy Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
1,1'-sulfanediylbis(2,4-dinitrobenzene) IC50: 0.004 mM Homo sapiens
1,1'-sulfanediylbis(2,4-dinitrobenzene) IC50: 0.0005 mM Plasmodium falciparum
1,1'-sulfanediylbis[2-nitro-4-(trifluoromethyl)benzene] IC50: 0.15 mM Homo sapiens
1,1'-sulfanediylbis[2-nitro-4-(trifluoromethyl)benzene] IC50: 0.02 mM Plasmodium falciparum
1,3-dinitro-5-(trifluoromethyl)benzene IC50: 0.2 mM Homo sapiens
1,3-dinitro-5-(trifluoromethyl)benzene IC50: 0.03 mM Plasmodium falciparum
2-chloro-1,3-dinitro-5-(trifluoromethyl)benzene IC50: 0.1 mM Homo sapiens
2-chloro-1,3-dinitro-5-(trifluoromethyl)benzene IC50: 0.008 mM Plasmodium falciparum
4,5-dinitro-1,3-benzodioxole IC50: 0.08 mM Homo sapiens
4,5-dinitro-1,3-benzodioxole IC50: 0.01 mM Plasmodium falciparum
4,6-dinitro-2,1,3-benzothiadiazole IC50: 0.002 mM Homo sapiens
4,6-dinitro-2,1,3-benzothiadiazole IC50: 0.01 mM Plasmodium falciparum
4-nitro-2,1,3-benzothiadiazole IC50: 0.05 mM Homo sapiens
4-nitro-2,1,3-benzothiadiazole IC50: 0.002 mM Plasmodium falciparum
5-nitro-1,3-benzodioxole IC50: 0.2 mM Homo sapiens
5-nitro-1,3-benzodioxole 0.1 mM, 10% inhibition Plasmodium falciparum
5-nitro-2,1,3-benzothiadiazole IC50: 0.09 mM Homo sapiens
5-nitro-2,1,3-benzothiadiazole IC50: 0.01 mM Plasmodium falciparum
6,7-dinitroquinoxaline IC50: 0.14 mM Homo sapiens
6,7-dinitroquinoxaline IC50: 0.002 mM Plasmodium falciparum
6-nitroquinoxaline IC50: 0.2 mM Homo sapiens
6-nitroquinoxaline IC50: 0.04 mM Plasmodium falciparum

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
55000
-
 2 * 55000 Homo sapiens
55000
-
 2 * 55000 Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Plasmodium falciparum
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
thioredoxin + NADP+
-
 Homo sapiens thioredoxin disulfide + NADPH
-
 ?
thioredoxin + NADP+
-
 Plasmodium falciparum thioredoxin disulfide + NADPH
-
 ?

Subunits

Subunits Comment Organism
homodimer 2 * 55000 Homo sapiens
homodimer 2 * 55000 Plasmodium falciparum

Synonyms

Synonyms Comment Organism
thioredoxin reductase
-
 Homo sapiens
thioredoxin reductase
-
 Plasmodium falciparum
TrxR
-
 Homo sapiens
TrxR
-
 Plasmodium falciparum

Cofactor

Cofactor Comment Organism Structure
FAD
-
 Homo sapiens
FAD
-
 Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0005
-
 IC50: 0.0005 mM Plasmodium falciparum 1,1'-sulfanediylbis(2,4-dinitrobenzene)
0.002
-
 IC50: 0.002 mM Plasmodium falciparum 4-nitro-2,1,3-benzothiadiazole
0.002
-
 IC50: 0.002 mM Plasmodium falciparum 6,7-dinitroquinoxaline
0.002
-
 IC50: 0.002 mM Homo sapiens 4,6-dinitro-2,1,3-benzothiadiazole
0.004
-
 IC50: 0.004 mM Homo sapiens 1,1'-sulfanediylbis(2,4-dinitrobenzene)
0.008
-
 IC50: 0.008 mM Plasmodium falciparum 2-chloro-1,3-dinitro-5-(trifluoromethyl)benzene
0.01
-
 IC50: 0.01 mM Plasmodium falciparum 5-nitro-2,1,3-benzothiadiazole
0.01
-
 IC50: 0.01 mM Plasmodium falciparum 4,6-dinitro-2,1,3-benzothiadiazole
0.01
-
 IC50: 0.01 mM Plasmodium falciparum 4,5-dinitro-1,3-benzodioxole
0.02
-
 IC50: 0.02 mM Plasmodium falciparum 1,1'-sulfanediylbis[2-nitro-4-(trifluoromethyl)benzene]
0.03
-
 IC50: 0.03 mM Plasmodium falciparum 1,3-dinitro-5-(trifluoromethyl)benzene
0.04
-
 IC50: 0.04 mM Plasmodium falciparum 6-nitroquinoxaline
0.05
-
 IC50: 0.05 mM Homo sapiens 4-nitro-2,1,3-benzothiadiazole
0.08
-
 IC50: 0.08 mM Homo sapiens 4,5-dinitro-1,3-benzodioxole
0.09
-
 IC50: 0.09 mM Homo sapiens 5-nitro-2,1,3-benzothiadiazole
0.1
-
 IC50: 0.1 mM Homo sapiens 2-chloro-1,3-dinitro-5-(trifluoromethyl)benzene
0.14
-
 IC50: 0.14 mM Homo sapiens 6,7-dinitroquinoxaline
0.15
-
 IC50: 0.15 mM Homo sapiens 1,1'-sulfanediylbis[2-nitro-4-(trifluoromethyl)benzene]
0.2
-
 IC50: 0.2 mM Homo sapiens 1,3-dinitro-5-(trifluoromethyl)benzene
0.2
-
 IC50: 0.2 mM Homo sapiens 6-nitroquinoxaline
0.2
-
 IC50: 0.2 mM Homo sapiens 5-nitro-1,3-benzodioxole