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Literature summary for 2.6.1.7 extracted from

  • Kalliokoski, T.; Rummakko, P.; Rantanen, M.; Blaesse, M.; Augustin, M.; Ummenthala, G.R.; Choudhary, S.; Venaelaeinen, J.
    Discovery of sulfonamides and 9-oxo-2,8-diazaspiro[5,5]undecane-2-carboxamides as human kynurenine aminotransferase 2 (KAT2) inhibitors (2020), Bioorg. Med. Chem. Lett., 30, 127060 .
    View publication on PubMed
Search for more literature for 2.6.1.7

Inhibitors

Inhibitors Comment Organism Structure
(2S)-2-(5,6-dichloro-1,3-dioxo-2,3-dihydro-1H-inden-2-yl)-3-phenylpropanoic acid reversible inhibitor Homo sapiens
(2S)-2-amino-4-[4-(ethylsulfonyl)phenyl]-4-oxobutanoic acid reversible inhibitor Homo sapiens
(3S)-3-amino-1-hydroxy-3,4-dihydroquinolin-2(1H)-one irreversible inhibitor Homo sapiens
(5Z)-5-[3-(4-oxo-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-7-yl)benzylidene]-1,3-thiazolidine-2,4-dione reversible inhibitor Homo sapiens
(6R)-8-cyclopropyl-N-(3,5-dimethylphenyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
-
 Homo sapiens
(6R)-8-cyclopropyl-N-(4-methoxyphenyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
-
 Homo sapiens
(6R)-N-(3-chloro-4-fluorophenyl)-8-(cyclopropylmethyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
-
 Homo sapiens
(6R)-N-(3-ethylphenyl)-8-(3-methylbutyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
-
 Homo sapiens
(6S)-8-cyclopropyl-N-(3,5-dimethylphenyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
-
 Homo sapiens
(6S)-8-cyclopropyl-N-(4-methoxyphenyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
-
 Homo sapiens
(6S)-N-(3-chloro-4-fluorophenyl)-8-(cyclopropylmethyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
-
 Homo sapiens
(6S)-N-(3-ethylphenyl)-8-(3-methylbutyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
-
 Homo sapiens
3,5-difluoro-N-[5-(1-phenylcyclopropyl)-1,3,4-thiadiazol-2-yl]benzenesulfonamide
-
 Homo sapiens
3,5-difluoro-N-{5-[(2R)-2-(3-fluorophenyl)-3-methylbutyl]-1,3,4-thiadiazol-2-yl}benzenesulfonamide
-
 Homo sapiens
3,5-difluoro-N-{5-[(2S)-2-(3-fluorophenyl)-3-methylbutyl]-1,3,4-thiadiazol-2-yl}benzenesulfonamide
-
 Homo sapiens
3,5-difluoro-N-{5-[2-(3-fluorophenyl)-3-methylbutyl]-1,3,4-thiadiazol-2-yl}benzenesulfonamide
-
 Homo sapiens
4-chloro-N-(pyrrolidin-3-yl)-2-(trifluoromethyl)benzenesulfonamide
-
 Homo sapiens
BFF-122 irreversible inhibitor Homo sapiens
N-(3-chloro-4-methylphenyl)-8-(3-methylbutyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
-
 Homo sapiens
N-(3-ethylphenyl)-8-(3-methylbutyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
-
 Homo sapiens
N-benzyl-1-[6-methyl-5-(oxan-4-yl)-7-oxo-6,7-dihydro[1,3]thiazolo[5,4-d]pyrimidin-2-yl]-D-prolinamide reversible inhibitor Homo sapiens
N-[5-(cyclopentylmethyl)-1,3,4-oxadiazol-2-yl]benzenesulfonamide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
L-kynurenine + 2-oxoglutarate Homo sapiens
-
 4-(2-aminophenyl)-2,4-dioxobutanoate + L-glutamate + H2O
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q8N5Z0
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-kynurenine + 2-oxoglutarate
-
 Homo sapiens 4-(2-aminophenyl)-2,4-dioxobutanoate + L-glutamate + H2O
-
 ?

Synonyms

Synonyms Comment Organism
KAT2
-
 Homo sapiens
kynurenine aminotransferase 2
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
pyridoxal 5'-phosphate
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00081
-
 pH and temperature not specified in the publication Homo sapiens N-(3-chloro-4-methylphenyl)-8-(3-methylbutyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
0.0024
-
 pH and temperature not specified in the publication Homo sapiens (6R)-N-(3-chloro-4-fluorophenyl)-8-(cyclopropylmethyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
0.0045
-
 pH and temperature not specified in the publication Homo sapiens (6R)-8-cyclopropyl-N-(3,5-dimethylphenyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
0.008
-
 pH and temperature not specified in the publication Homo sapiens N-(3-ethylphenyl)-8-(3-methylbutyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
0.0155
-
 pH and temperature not specified in the publication Homo sapiens (6S)-8-cyclopropyl-N-(4-methoxyphenyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
0.044
-
 pH and temperature not specified in the publication Homo sapiens (6R)-N-(3-ethylphenyl)-8-(3-methylbutyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
0.0749
-
 pH and temperature not specified in the publication Homo sapiens (6S)-8-cyclopropyl-N-(3,5-dimethylphenyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
0.0965
-
 pH and temperature not specified in the publication Homo sapiens (6S)-N-(3-chloro-4-fluorophenyl)-8-(cyclopropylmethyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
0.097
-
 pH and temperature not specified in the publication Homo sapiens (6S)-N-(3-ethylphenyl)-8-(3-methylbutyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide
0.1
-
 IC50 above 0.1 mM, pH and temperature not specified in the publication Homo sapiens (6R)-8-cyclopropyl-N-(4-methoxyphenyl)-9-oxo-2,8-diazaspiro[5.5]undecane-2-carboxamide