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Literature summary for 1.13.11.52 extracted from

  • Balti, M.; Plas, A.; Meinguet, C.; Haufroid, M.; Themans, Q.; Efrit, M.L.; Wouters, J.; Lanners, S.
    Synthesis of 4- and 5-arylthiazolinethiones as inhibitors of indoleamine 2,3-dioxygenase (2017), Bioorg. Med. Chem. Lett., 27, 3607-3610 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-(2-sulfanylidene-2,3-dihydro-1,3-thiazol-4-yl)benzoic acid 0.1 mM, 8% inhibition Homo sapiens
2-bromo-4-phenyl-1,3-thiazole 0.1 mM, 12% inhibition Homo sapiens
2-chloro-4-phenyl-1,3-thiazole 0.1 mM, 0.5% inhibition Homo sapiens
4-(2-fluorophenyl)-1,3-thiazole-2(3H)-thione 0.1 mM, 77% inhibition Homo sapiens
4-(2-methoxyphenyl)-1,3-thiazole-2(3H)-thione 0.1 mM, 53% inhibition Homo sapiens
4-(2-sulfanylidene-2,3-dihydro-1,3-thiazol-4-yl)benzonitrile 0.1 mM, 8% inhibition Homo sapiens
4-(3-bromophenyl)-1,3-thiazole-2(3H)-thione 0.1 mM, 81% inhibition Homo sapiens
4-(3-chlorophenyl)-1,3-thiazole-2(3H)-thione 0.1 mM, 40% inhibition Homo sapiens
4-(3-fluorophenyl)-1,3-thiazole-2(3H)-thione 0.1 mM, 28% inhibition Homo sapiens
4-(4-bromophenyl)-1,3-thiazole-2(3H)-thione 0.1 mM, 100% inhibition Homo sapiens
4-(4-chlorophenyl)-1,3-thiazole-2(3H)-thione 0.1 mM, 95% inhibition Homo sapiens
4-(4-fluorophenyl)-1,3-thiazole-2(3H)-thione 0.1 mM, 72% inhibition Homo sapiens
4-(4-methoxyphenyl)-1,3-thiazole-2(3H)-thione 0.1 mM, 68% inhibition Homo sapiens
4-(4-methylphenyl)-1,3-thiazole-2(3H)-thione 0.1 mM, 90% inhibition Homo sapiens
4-(pyridin-3-yl)-1,3-thiazole-2(3H)-thione 0.1 mM, 48% inhibition Homo sapiens
4-(pyridin-4-yl)-1,3-thiazole-2(3H)-thione 0.1 mM, 21% inhibition Homo sapiens
4-phenyl-1,3-thiazol-2(3H)-one 0.1 mM, 15% inhibition Homo sapiens
4-phenyl-1,3-thiazol-2-amine 0.1 mM, 13% inhibition Homo sapiens
4-phenyl-1,3-thiazole-2(3H)-thione 0.1 mM, 76% inhibition Homo sapiens
4-[3-(hydroxymethyl)phenyl]-1,3-thiazole-2(3H)-thione 0.1 mM, 16% inhibition Homo sapiens
4-[4-(trifluoromethyl)phenyl]-1,3-thiazole-2(3H)-thione 0.1 mM, 37% inhibition Homo sapiens
5-(2-fluorophenyl)-1,3-thiazole-2(3H)-thione 0.1 mM, 29% inhibition Homo sapiens
5-(2-methoxyphenyl)-1,3-thiazole-2(3H)-thione 0.1 mM, 12% inhibition Homo sapiens
5-(3-bromophenyl)-1,3-thiazole-2(3H)-thione 0.1 mM, 48% inhibition Homo sapiens
5-(4-methylphenyl)-1,3-thiazole-2(3H)-thione 0.1 mM, 15% inhibition Homo sapiens
5-phenyl-1,3-thiazole-2(3H)-thione 0.1 mM, 16% inhibition Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
L-tryptophan + O2 Homo sapiens
-
N-formyl-L-kynurenine
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P14902
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-tryptophan + O2
-
Homo sapiens N-formyl-L-kynurenine
-
?

Synonyms

Synonyms Comment Organism
IDO1
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0026
-
pH 6.5, 22°C Homo sapiens 4-(4-chlorophenyl)-1,3-thiazole-2(3H)-thione
0.0034
-
pH 6.5, 22°C Homo sapiens 4-(4-bromophenyl)-1,3-thiazole-2(3H)-thione
0.0059
-
pH 6.5, 22°C Homo sapiens 4-(4-methylphenyl)-1,3-thiazole-2(3H)-thione
0.024
-
pH 6.5, 22°C Homo sapiens 4-phenyl-1,3-thiazole-2(3H)-thione