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Literature summary for 1.13.11.52 extracted from

  • Griglio, A.; Torre, E.; Serafini, M.; Bianchi, A.; Schmid, R.; Coda Zabetta, G.; Massarotti, A.; Sorba, G.; Pirali, T.; Fallarini, S.
    A multicomponent approach in the discovery of indoleamine 2,3-dioxygenase 1 inhibitors Synthesis, biological investigation and docking studies (2018), Bioorg. Med. Chem. Lett., 28, 651-657 .
    View publication on PubMed
Search for more literature for 1.13.11.52

Inhibitors

Inhibitors Comment Organism Structure
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (2-chlorophenyl)acetate
-
 Homo sapiens
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (2-hydroxyphenyl)acetate 0.001 mM, 73% inhibition Homo sapiens
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (2-nitrophenyl)acetate
-
 Homo sapiens
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (3,4-dihydroxyphenyl)acetate
-
 Homo sapiens
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (3-chlorophenyl)acetate
-
 Homo sapiens
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (3-cyanophenyl)acetate
-
 Homo sapiens
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (3-hydroxyphenyl)acetate
-
 Homo sapiens
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (3-nitrophenyl)acetate
-
 Homo sapiens
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (4-chlorophenyl)acetate
-
 Homo sapiens
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (4-cyanophenyl)acetate 0.001 mM, 69% inhibition Homo sapiens
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (4-hydroxyphenyl)acetate 0.001 mM, 89% inhibition Homo sapiens
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (4-nitrophenyl)acetate
-
 Homo sapiens
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl phenylacetate 0.001 mM, 72% inhibition Homo sapiens
epacadostat pH and temperature not specified in the publication Homo sapiens
N-[2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl]-3-methoxy-N-methylbenzamide
-
 Homo sapiens
N-[2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl]-4-methoxy-N-methylbenzamide
-
 Homo sapiens
N-[2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl]-N-(4-cyanophenyl)acetamide
-
 Homo sapiens
N-[2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl]-N-methyl-4-nitrobenzamide
-
 Homo sapiens
N-[2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl]-N-methylacetamide
-
 Homo sapiens
N-[2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl]-N-phenylacetamide
-
 Homo sapiens
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-2-hydroxyacetamide
-
 Homo sapiens
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-4-oxobutanamide 0.001 mM, 97% inhibition Homo sapiens
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-(phenylacetyl)glycinamide
-
 Homo sapiens
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-methyl-N2-(phenylacetyl)glycinamide 0.001 mM, 62% inhibition Homo sapiens
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-methyl-N2-[(2-nitrophenyl)acetyl]glycinamide 0.001 mM, 67% inhibition Homo sapiens
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-methyl-N2-[(3-nitrophenyl)acetyl]glycinamide 0.001 mM, 65% inhibition Homo sapiens
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-methyl-N2-[(4-nitrophenyl)acetyl]glycinamide 0.001 mM, 66% inhibition Homo sapiens
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-[(2-chlorophenyl)acetyl]-N2-methylglycinamide
-
 Homo sapiens
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-[(3,4-dihydroxyphenyl)acetyl]-N2-methylglycinamide
-
 Homo sapiens
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-[(3-chlorophenyl)acetyl]-N2-methylglycinamide
-
 Homo sapiens
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-[(3-hydroxyphenyl)acetyl]-N2-methylglycinamide 0.001 mM, 63% inhibition Homo sapiens
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-[(4-chlorophenyl)acetyl]-N2-methylglycinamide
-
 Homo sapiens
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-[(4-cyanophenyl)acetyl]-N2-methylglycinamide
-
 Homo sapiens
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-[(4-hydroxyphenyl)acetyl]-N2-methylglycinamide
-
 Homo sapiens
N2-[(2S)-2-amino-2-phenylacetyl]-N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]glycinamide
-
 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
0.00001
-
 pH and temperature not specified in the publication Homo sapiens epacadostat
0.00008
-
 pH and temperature not specified in the publication Homo sapiens N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-4-oxobutanamide
0.0002
-
 pH and temperature not specified in the publication Homo sapiens 2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (4-hydroxyphenyl)acetate
0.00034
-
 pH and temperature not specified in the publication Homo sapiens 2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (4-cyanophenyl)acetate
0.00045
-
 pH and temperature not specified in the publication Homo sapiens N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-[(3-hydroxyphenyl)acetyl]-N2-methylglycinamide
0.00058
-
 pH and temperature not specified in the publication Homo sapiens 2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl phenylacetate
0.00063
-
 pH and temperature not specified in the publication Homo sapiens N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-methyl-N2-[(3-nitrophenyl)acetyl]glycinamide
0.00069
-
 pH and temperature not specified in the publication Homo sapiens N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-methyl-N2-(phenylacetyl)glycinamide
0.00073
-
 pH and temperature not specified in the publication Homo sapiens N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-methyl-N2-[(2-nitrophenyl)acetyl]glycinamide
0.00081
-
 pH and temperature not specified in the publication Homo sapiens N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-methyl-N2-[(4-nitrophenyl)acetyl]glycinamide
0.00087
-
 pH and temperature not specified in the publication Homo sapiens 2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (2-hydroxyphenyl)acetate

General Information

General Information Comment Organism
drug target the enzyme is an attractive target for cancer immunotherapy Homo sapiens
physiological function the enzyme plays a crucial role in immune tolerance Homo sapiens