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Literature summary for 1.13.11.11 extracted from

  • Pei, Z.; Mendonca, R.; Gazzard, L.; Pastor, R.; Goon, L.; Gustafson, A.; VanderPorten, E.; Hatzivassiliou, G.; Dement, K.; Cass, R.; Yuen, P.W.; Zhang, Y.; Wu, G.; Lin, X.; Liu, Y.; Sellers, B.D.
    Aminoisoxazoles as potent inhibitors of tryptophan 2,3-dioxygenase 2 (TDO2) (2018), ACS Med. Chem. Lett., 9, 417-421 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.13.11.11

Inhibitors

Inhibitors Comment Organism Structure
(4-phenyl-1,2-oxazol-5-yl)methanol
-
 Homo sapiens
3-methyl-4-phenyl-1,2-oxazol-5-amine
-
 Homo sapiens
4-(1H-pyrazol-1-yl)-1,2-oxazol-5-amine
-
 Homo sapiens
4-(3-chlorophenyl)-1,2-oxazol-5-amine
-
 Homo sapiens
4-(3-methoxyphenyl)-1,2-oxazol-5-amine
-
 Homo sapiens
4-(3-methyl-1H-pyrazol-1-yl)-1,2-oxazol-5-amine
-
 Homo sapiens
4-(4-chlorophenyl)-1,2-oxazol-5-amine
-
 Homo sapiens
4-(4-fluoro-1H-pyrazol-1-yl)-1,2-oxazol-5-amine
-
 Homo sapiens
4-(4-fluorophenyl)-1,2-oxazol-5-amine
-
 Homo sapiens
4-(4-methyl-1H-pyrazol-1-yl)-1,2-oxazol-5-amine
-
 Homo sapiens
4-(pyridin-2-yl)-1,2-oxazol-5-amine
-
 Homo sapiens
4-(pyridin-3-yl)-1,2-oxazol-5-amine
-
 Homo sapiens
4-(thiophen-2-yl)-1,2-oxazol-5-amine
-
 Homo sapiens
4-(thiophen-3-yl)-1,2-oxazol-5-amine
-
 Homo sapiens
4-cyclohexyl-1,2-oxazol-5-amine
-
 Homo sapiens
4-cyclopentyl-1,2-oxazol-5-amine
-
 Homo sapiens
4-phenyl-1,2-oxazol-5-amine
-
 Homo sapiens
4-phenyl-1,2-thiazol-5-amine
-
 Homo sapiens
5-phenyl-1,2,3-thiadiazol-4-amine potent tryptophan 2,3-dioxygenase 2 inhibitor with modest selectivity over indolamine 2,3-dioxygenase 1 and with improved human whole blood stability Homo sapiens
N-methyl-4-phenyl-1,2-oxazol-5-amine
-
 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 P48775
-
-

Source Tissue

Source Tissue Comment Organism Textmining
leiomyoma
-
 Homo sapiens
-

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
TDO2
-
 Homo sapiens
tryptophan 2,3-dioxygenase 2
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
heme heme-containing enzyme Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000028
-
 pH and temperature not specified in the publication Homo sapiens 4-(thiophen-3-yl)-1,2-oxazol-5-amine
0.000029
-
 pH and temperature not specified in the publication Homo sapiens 4-(thiophen-2-yl)-1,2-oxazol-5-amine
0.00014
-
 pH and temperature not specified in the publication Homo sapiens 4-phenyl-1,2-oxazol-5-amine
0.00019
-
 pH and temperature not specified in the publication Homo sapiens N-methyl-4-phenyl-1,2-oxazol-5-amine
0.00029
-
 pH and temperature not specified in the publication Homo sapiens 4-(1H-pyrazol-1-yl)-1,2-oxazol-5-amine
0.00034
-
 pH and temperature not specified in the publication Homo sapiens 4-(4-fluoro-1H-pyrazol-1-yl)-1,2-oxazol-5-amine
0.0005
-
 pH and temperature not specified in the publication Homo sapiens 4-(3-chlorophenyl)-1,2-oxazol-5-amine
0.00058
-
 pH and temperature not specified in the publication Homo sapiens 4-(4-fluorophenyl)-1,2-oxazol-5-amine
0.00064
-
 pH and temperature not specified in the publication Homo sapiens 4-cyclopentyl-1,2-oxazol-5-amine
0.00083
-
 pH and temperature not specified in the publication Homo sapiens 4-(4-chlorophenyl)-1,2-oxazol-5-amine
0.0016
-
 pH and temperature not specified in the publication Homo sapiens 4-(3-methyl-1H-pyrazol-1-yl)-1,2-oxazol-5-amine
0.0016
-
 pH and temperature not specified in the publication Homo sapiens 4-(4-methyl-1H-pyrazol-1-yl)-1,2-oxazol-5-amine
0.0017
-
 pH and temperature not specified in the publication Homo sapiens 4-(pyridin-2-yl)-1,2-oxazol-5-amine
0.0023
-
 pH and temperature not specified in the publication Homo sapiens 4-(pyridin-3-yl)-1,2-oxazol-5-amine
0.0031
-
 pH and temperature not specified in the publication Homo sapiens 4-(3-methoxyphenyl)-1,2-oxazol-5-amine
0.0044
-
 pH and temperature not specified in the publication Homo sapiens (4-phenyl-1,2-oxazol-5-yl)methanol
0.0078
-
 pH and temperature not specified in the publication Homo sapiens 4-cyclohexyl-1,2-oxazol-5-amine
0.018
-
 pH and temperature not specified in the publication Homo sapiens 4-phenyl-1,2-thiazol-5-amine
0.025
-
 pH and temperature not specified in the publication Homo sapiens 3-methyl-4-phenyl-1,2-oxazol-5-amine

General Information

General Information Comment Organism
drug target the enzyme (TDO2) catalyzes the conversion of tryptophan to the immunosuppressive metabolite kynurenine. TDO2 overexpression has been observed in a number of cancers. Therefore, TDO inhibition may be a useful therapeutic intervention for cancers Homo sapiens
physiological function the enzyme (TDO2) catalyzes the conversion of tryptophan to the immunosuppressive metabolite kynurenine Homo sapiens