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Literature summary for 1.13.11.52 extracted from

  • Markwalder, J.A.; Seitz, S.P.; Blat, Y.; Elkin, L.; Hunt, J.T.; Pabalan, J.G.; Jure-Kunkel, M.N.; Vite, G.D.; Covello, K.
    Identification and optimization of a novel series of indoleamine 2,3-dioxygenase inhibitors (2017), Bioorg. Med. Chem. Lett., 27, 582-585 .
    View publication on PubMed
Search for more literature for 1.13.11.52

Inhibitors

Inhibitors Comment Organism Structure
3'-[[(2-chlorophenyl)carbamoyl]amino]-4-methoxy-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
3'-[[(2-fluorophenyl)carbamoyl]amino]-4-methoxy-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4'-(2,3-dimethylphenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4'-(2-chlorophenoxy)-3'-([[4-(2-hydroxypropan-2-yl)phenyl]carbamoyl]amino)-4-methoxy[1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4'-(2-chlorophenoxy)-3'-[[(4-chlorophenyl)carbamoyl]amino]-4-methoxy[1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4'-(2-chlorophenoxy)-3'-[[(4-cyanophenyl)carbamoyl]amino]-4-methoxy[1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4'-(2-chlorophenoxy)-4-methoxy-3'-[[(4-methoxyphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4'-(2-chlorophenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4'-(2-ethylphenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4'-(2-tert-butylphenoxy)-2-fluoro-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4'-(2-tert-butylphenoxy)-4-chloro-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4'-(2-tert-butylphenoxy)-4-ethoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4'-(2-tert-butylphenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4'-(2-tert-butylphenoxy)-5-chloro-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4'-(3-tert-butylphenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4'-[(2,3-dihydro-1H-inden-4-yl)oxy]-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4-methoxy-3'-[(phenylcarbamoyl)amino]-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4-methoxy-3'-[[(2-methylphenyl)carbamoyl]amino]-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4-methoxy-3'-[[(3-methylphenyl)carbamoyl]amino]-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino]-4'-(2-propylphenoxy)[1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino]-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino]-4'-[2-(propan-2-yl)phenoxy][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino]-4'-[2-methyl-3-[(prop-2-yn-1-yl)oxy]phenoxy][1,1'-biphenyl]-3-carboxylic acid
-
 Homo sapiens
N-(4-bromophenyl)-N'-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]urea
-
 Homo sapiens
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-(2-methylphenyl)urea
-
 Homo sapiens
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-(3-methylphenyl)urea
-
 Homo sapiens
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-(4-methoxyphenyl)urea
-
 Homo sapiens
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-(4-methylphenyl)urea
-
 Homo sapiens
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-phenylurea
-
 Homo sapiens
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-[4-(difluoromethoxy)phenyl]urea
-
 Homo sapiens
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-[4-(trifluoromethoxy)phenyl]urea
-
 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
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HeLa cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000022
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 3'-[[(2-chlorophenyl)carbamoyl]amino]-4-methoxy-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
0.000049
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4-methoxy-3'-[[(2-methylphenyl)carbamoyl]amino]-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
0.00005
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 3'-[[(2-fluorophenyl)carbamoyl]amino]-4-methoxy-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
0.00005
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino]-4'-[2-methyl-3-[(prop-2-yn-1-yl)oxy]phenoxy][1,1'-biphenyl]-3-carboxylic acid
0.000062
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4-methoxy-3'-[(phenylcarbamoyl)amino]-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
0.0001
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4-methoxy-3'-[[(3-methylphenyl)carbamoyl]amino]-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
0.0001
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino]-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
0.00012
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4'-(2-tert-butylphenoxy)-4-ethoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
0.00016
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4'-(2,3-dimethylphenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
0.00025
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4'-(2-tert-butylphenoxy)-5-chloro-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
0.00028
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4'-[(2,3-dihydro-1H-inden-4-yl)oxy]-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
0.00033
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino]-4'-(2-propylphenoxy)[1,1'-biphenyl]-3-carboxylic acid
0.00034
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino]-4'-[2-(propan-2-yl)phenoxy][1,1'-biphenyl]-3-carboxylic acid
0.00035
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4'-(2-tert-butylphenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
0.00054
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4'-(2-ethylphenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
0.00057
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-(3-methylphenyl)urea
0.00069
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4'-(3-tert-butylphenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
0.00079
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-(4-methylphenyl)urea
0.00083
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4'-(2-chlorophenoxy)-3'-[[(4-chlorophenyl)carbamoyl]amino]-4-methoxy[1,1'-biphenyl]-3-carboxylic acid
0.00084
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4'-(2-chlorophenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
0.001
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-(2-methylphenyl)urea
0.0015
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-phenylurea
0.0018
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-(4-methoxyphenyl)urea
0.0021
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4'-(2-chlorophenoxy)-4-methoxy-3'-[[(4-methoxyphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
0.0024
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4'-(2-chlorophenoxy)-3'-([[4-(2-hydroxypropan-2-yl)phenyl]carbamoyl]amino)-4-methoxy[1,1'-biphenyl]-3-carboxylic acid
0.0024
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4'-(2-tert-butylphenoxy)-4-chloro-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
0.0026
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-[4-(difluoromethoxy)phenyl]urea
0.0029
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens N-(4-bromophenyl)-N'-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]urea
0.004
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-[4-(trifluoromethoxy)phenyl]urea
0.0045
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4'-(2-tert-butylphenoxy)-2-fluoro-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
0.006
-
 pH and temperature not specified in the publication, cellular assay of kynurenine production Homo sapiens 4'-(2-chlorophenoxy)-3'-[[(4-cyanophenyl)carbamoyl]amino]-4-methoxy[1,1'-biphenyl]-3-carboxylic acid