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Literature summary for 1.1.1.153 extracted from

  • Alen, J.; Schade, M.; Wagener, M.; Christian, F.; Nordhoff, S.; Merla, B.; Dunkern, T.R.; Bahrenberg, G.; Ratcliffe, P.
    Fragment-based discovery of novel potent sepiapterin reductase inhibitors (2019), J. Med. Chem., 62, 6391-6397 .
    View publication on PubMed
Search for more literature for 1.1.1.153

Inhibitors

Inhibitors Comment Organism Structure
(2,4-dichloro-6-hydroxyphenyl)(1,3-dihydro-2H-isoindol-2-yl)methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)(2,3-dihydro-1H-indol-1-yl)methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)(2-methyl-2,3-dihydro-1H-indol-1-yl)methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)(2-methyl-2,6-diazaspiro[3.4]octan-6-yl)methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)(2-oxa-6-azaspiro[3.4]octan-6-yl)methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)(3,3-dimethylpyrrolidin-1-yl)methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)(3,4-dihydroisoquinolin-2(1H)-yl)methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)(3,4-dihydroquinolin-1(2H)-yl)methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)(3-fluoro-3-methylpyrrolidin-1-yl)methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)(3-phenylpyrrolidin-1-yl)methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)(4-phenylpiperidin-1-yl)methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)(pyrrolidin-1-yl)methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)[3-(1-methyl-1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)[3-(2-phenylethyl)pyrrolidin-1-yl]methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)[3-(pyridin-2-yl)pyrrolidin-1-yl]methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)[3-(pyridin-3-yl)pyrrolidin-1-yl]methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)[3-(pyridin-4-yl)pyrrolidin-1-yl]methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)[3-(trifluoromethyl)pyrrolidin-1-yl]methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)[3-[(pyridin-3-yl)methyl]pyrrolidin-1-yl]methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)[3-[(pyridin-3-yl)oxy]pyrrolidin-1-yl]methanone
-
 Homo sapiens
(2,4-dichloro-6-hydroxyphenyl)[3-[(pyridin-4-yl)methyl]pyrrolidin-1-yl]methanone
-
 Homo sapiens
(2-azaspiro[3.4]octan-2-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
-
 Homo sapiens
(2-azaspiro[4.4]nonan-2-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
-
 Homo sapiens
(2-azaspiro[4.5]decan-2-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
-
 Homo sapiens
(3-anilinopyrrolidin-1-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
-
 Homo sapiens
(3-benzylpyrrolidin-1-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
-
 Homo sapiens
(4-benzylpiperidin-1-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
-
 Homo sapiens
(5-azaspiro[2.4]heptan-5-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
-
 Homo sapiens
(6-aza-spiro[3.4]oct-6-yl)-(2,4-difluoro-6-hydroxyphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(2,3-dichloro-6-hydroxyphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(2,4-dichloro-3-fluoro-6-hydroxyphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(2,4-dichloro-6-methoxyphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(2-chloro-4-fluoro-6-hydroxyphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(2-chloro-6-hydroxy-4-methoxyphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(2-chloro-6-hydroxy-4-methylphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(2-chloro-6-hydroxyphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(2-fluoro-6-hydroxy-4-methylphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(2-fluoro-6-hydroxyphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(2-hydroxypyridin-3-yl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(3,4-dichloro-2-hydroxyphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(3,6-dichloro-2-hydroxyphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(3-chloro-5-hydroxypyridin-4-yl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(3-hydroxypyridin-2-yl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(3-hydroxypyridin-4-yl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(4,5-dichloro-2-hydroxyphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(4-chloro-2-fluoro-6-hydroxyphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(4-chloro-2-hydroxy-6-methylphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(4-chloro-2-hydroxyphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(4-fluoro-2-hydroxyphenyl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(4-hydroxypyridin-3-yl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(5-chloro-3-hydroxypyridin-2-yl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(5-fluoro-3-hydroxypyridin-2-yl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)(5-hydroxypyrimidin-4-yl)methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)[2-chloro-4-(dimethylamino)-6-hydroxyphenyl]methanone
-
 Homo sapiens
(6-azaspiro[3.4]octan-6-yl)[2-chloro-6-hydroxy-4-(trifluoromethyl)phenyl]methanone
-
 Homo sapiens
(6-azaspiro[3.5]nonan-6-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
-
 Homo sapiens
2-(6-azaspiro[3.4]octane-6-sulfonyl)-3,5-dichlorophenol
-
 Homo sapiens
2-(6-azaspiro[3.4]octane-6-sulfonyl)-3,5-difluorophenol
-
 Homo sapiens
2-(6-azaspiro[3.4]octane-6-sulfonyl)-3-fluorophenol
-
 Homo sapiens
2-(6-azaspiro[3.4]octane-6-sulfonyl)-5-fluorophenol
-
 Homo sapiens
4-(6-azaspiro[3.4]octane-6-carbonyl)-3-chloro-5-hydroxybenzamide
-
 Homo sapiens
4-(6-azaspiro[3.4]octane-6-carbonyl)-3-chloro-5-hydroxybenzonitrile
-
 Homo sapiens
N-acetylserotonine
-
 Homo sapiens
SPRi3
-
 Homo sapiens
sulfapyridine
-
 Homo sapiens
sulfasalazine
-
 Homo sapiens
xanthurenic acid
-
 Homo sapiens
[4-(benzenesulfonyl)piperidin-1-yl](2,4-dichloro-6-hydroxyphenyl)methanone
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
sepiapterin + NADPH + H+ Homo sapiens
-
 7,8-dihydrobiopterin + NADP+
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P35270
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
sepiapterin + NADPH + H+
-
 Homo sapiens 7,8-dihydrobiopterin + NADP+
-
 ?

Synonyms

Synonyms Comment Organism
SPR
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00003
-
 at pH 7.4, temperature not specified in the publication Homo sapiens 2-(6-azaspiro[3.4]octane-6-sulfonyl)-3,5-difluorophenol
0.00004
-
 at pH 7.4, temperature not specified in the publication Homo sapiens 2-(6-azaspiro[3.4]octane-6-sulfonyl)-5-fluorophenol
0.000057
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (6-aza-spiro[3.4]oct-6-yl)-(2,4-difluoro-6-hydroxyphenyl)methanone
0.000083
-
 at pH 7.4, temperature not specified in the publication Homo sapiens 2-(6-azaspiro[3.4]octane-6-sulfonyl)-3,5-dichlorophenol
0.00012
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)(2,3-dihydro-1H-indol-1-yl)methanone
0.00021
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)(3,4-dihydroisoquinolin-2(1H)-yl)methanone
0.00024
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)(4-phenylpiperidin-1-yl)methanone
0.00028
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (3-anilinopyrrolidin-1-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
0.00029
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(2-fluoro-6-hydroxyphenyl)methanone
0.00031
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)[3-[(pyridin-3-yl)oxy]pyrrolidin-1-yl]methanone
0.00031
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (4-benzylpiperidin-1-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
0.00031
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(5-chloro-3-hydroxypyridin-2-yl)methanone
0.00035
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(5-fluoro-3-hydroxypyridin-2-yl)methanone
0.00037
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)[3-(pyridin-3-yl)pyrrolidin-1-yl]methanone
0.00038
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)[3-(2-phenylethyl)pyrrolidin-1-yl]methanone
0.00046
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.5]nonan-6-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
0.00052
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)(3-phenylpyrrolidin-1-yl)methanone
0.00055
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)[3-[(pyridin-4-yl)methyl]pyrrolidin-1-yl]methanone
0.00058
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
0.0006
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)[3-(1-methyl-1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
0.0006
-
 at pH 7.4, temperature not specified in the publication Homo sapiens [4-(benzenesulfonyl)piperidin-1-yl](2,4-dichloro-6-hydroxyphenyl)methanone
0.00061
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)[3-[(pyridin-3-yl)methyl]pyrrolidin-1-yl]methanone
0.00061
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(3-hydroxypyridin-2-yl)methanone
0.00062
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)[3-(pyridin-4-yl)pyrrolidin-1-yl]methanone
0.00067
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(2-chloro-4-fluoro-6-hydroxyphenyl)methanone
0.00068
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)(3,4-dihydroquinolin-1(2H)-yl)methanone
0.00074
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (3-benzylpyrrolidin-1-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
0.00079
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)[3-(pyridin-2-yl)pyrrolidin-1-yl]methanone
0.00098
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (5-azaspiro[2.4]heptan-5-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
0.00131
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)[3-(trifluoromethyl)pyrrolidin-1-yl]methanone
0.00145
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(2-chloro-6-hydroxyphenyl)methanone
0.00155
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(5-hydroxypyrimidin-4-yl)methanone
0.00157
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(2,4-dichloro-3-fluoro-6-hydroxyphenyl)methanone
0.00168
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)(2-oxa-6-azaspiro[3.4]octan-6-yl)methanone
0.00199
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)(pyrrolidin-1-yl)methanone
0.00232
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)[2-chloro-4-(dimethylamino)-6-hydroxyphenyl]methanone
0.0024
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2-azaspiro[4.4]nonan-2-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
0.00244
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)(2-methyl-2,3-dihydro-1H-indol-1-yl)methanone
0.00256
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)(1,3-dihydro-2H-isoindol-2-yl)methanone
0.00404
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(4-chloro-2-hydroxyphenyl)methanone
0.00478
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2-azaspiro[3.4]octan-2-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
0.0051
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)(3,3-dimethylpyrrolidin-1-yl)methanone
0.00527
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)(3-fluoro-3-methylpyrrolidin-1-yl)methanone
0.00585
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2-azaspiro[4.5]decan-2-yl)(2,4-dichloro-6-hydroxyphenyl)methanone
0.00748
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(2,3-dichloro-6-hydroxyphenyl)methanone
0.00772
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(4-chloro-2-fluoro-6-hydroxyphenyl)methanone
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens (2,4-dichloro-6-hydroxyphenyl)(2-methyl-2,6-diazaspiro[3.4]octan-6-yl)methanone
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(2,4-dichloro-6-methoxyphenyl)methanone
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(2-chloro-6-hydroxy-4-methoxyphenyl)methanone
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(2-chloro-6-hydroxy-4-methylphenyl)methanone
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(2-fluoro-6-hydroxy-4-methylphenyl)methanone
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(2-hydroxypyridin-3-yl)methanone
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(3,4-dichloro-2-hydroxyphenyl)methanone
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(3,6-dichloro-2-hydroxyphenyl)methanone
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(3-chloro-5-hydroxypyridin-4-yl)methanone
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(3-hydroxypyridin-4-yl)methanone
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(4,5-dichloro-2-hydroxyphenyl)methanone
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(4-chloro-2-hydroxy-6-methylphenyl)methanone
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(4-fluoro-2-hydroxyphenyl)methanone
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)(4-hydroxypyridin-3-yl)methanone
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens (6-azaspiro[3.4]octan-6-yl)[2-chloro-6-hydroxy-4-(trifluoromethyl)phenyl]methanone
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens 2-(6-azaspiro[3.4]octane-6-sulfonyl)-3-fluorophenol
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens 4-(6-azaspiro[3.4]octane-6-carbonyl)-3-chloro-5-hydroxybenzamide
0.01
-
 IC50 above 0.01 mM, at pH 7.4, temperature not specified in the publication Homo sapiens 4-(6-azaspiro[3.4]octane-6-carbonyl)-3-chloro-5-hydroxybenzonitrile