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Literature summary for 2.6.1.42 extracted from

  • Hu, L.Y.; Boxer, P.A.; Kesten, S.R.; Lei, H.J.; Wustrow, D.J.; Moreland, D.W.; Zhang, L.; Ahn, K.; Ryder, T.R.; Liu, X.; Rubin, J.R.; Fahnoe, K.; Carroll, R.T.; Dutta, S.; Fahnoe, D.C.; Probert, A.W.; Roof, R.L.; Rafferty, M.F.; Kostlan, C.R.; Scholten, J.D.; Hood, M.; Ren, X.D.; Schielke, G.P.; Su, T.Z.; Taylor, C.P.; Mi, M.i.s.
    The design and synthesis of human branched-chain amino acid aminotransferase inhibitors for treatment of neurodegenerative diseases (2006), Bioorg. Med. Chem. Lett., 16, 2337-2340.
    View publication on PubMed
Search for more literature for 2.6.1.42

Inhibitors

Inhibitors Comment Organism Structure
5-bromo-N'-(phenylsulfonyl)-1-benzofuran-2-carbohydrazide IC50: 0.0025 mM Homo sapiens
5-bromo-N'-(phenylsulfonyl)-1H-indole-2-carbohydrazide IC50: 0.015 mM Homo sapiens
5-chloro-N'-(phenylsulfonyl)-1-benzofuran-2-carbohydrazide IC50: 0.0042 mM Homo sapiens
5-chloro-N'-[(2-chlorophenyl)sulfonyl]-1-benzofuran-2-carbohydrazide IC50: 0.0057 mM Homo sapiens
5-chloro-N'-[(2-methylphenyl)sulfonyl]-1-benzofuran-2-carbohydrazide IC50: 0.00116 mM Homo sapiens
5-chloro-N'-[(3-methylphenyl)sulfonyl]-1-benzofuran-2-carbohydrazide IC50: 0.0012 mM Homo sapiens
5-chloro-N'-[[2-(trifluoromethyl)phenyl]sulfonyl]-1-benzofuran-2-carbohydrazide IC50: 0.0008 mM, potent inhibitor Homo sapiens
5-methoxy-N'-(phenylsulfonyl)-1-benzofuran-2-carbohydrazide IC50: 0.0128 mM Homo sapiens
5-methoxy-N'-(phenylsulfonyl)-1H-indole-2-carbohydrazide IC50: 0.0568 mM Homo sapiens
N'-(phenylsulfonyl)-1-benzofuran-2-carbohydrazide IC50: 0.0183 mM Homo sapiens
N'-(phenylsulfonyl)-1H-indole-2-carbohydrazide IC50: 0.036 mM Homo sapiens
N'-(phenylsulfonyl)dibenzo[b,d]furan-2-carbohydrazide IC50: 0.00235 mM Homo sapiens
N'-(phenylsulfonyl)quinoline-3-carbohydrazide IC50: 0.0333 mM Homo sapiens
N'-(phenylsulfonyl)quinoline-6-carbohydrazide IC50: 0.0133 mM Homo sapiens
N'-[(2-chlorophenyl)sulfonyl]dibenzo[b,d]furan-2-carbohydrazide IC50: 0.0129 mM Homo sapiens
N'-[(2-methylphenyl)sulfonyl]dibenzo[b,d]furan-2-carbohydrazide IC50: 0.0032 mM Homo sapiens
N'-[(3-chlorophenyl)sulfonyl]dibenzo[b,d]furan-2-carbohydrazide IC50: above 0.035 mM Homo sapiens
N'-[(3-methylphenyl)sulfonyl]dibenzo[b,d]furan-2-carbohydrazide IC50: 0.0028 mM Homo sapiens
N'-[(4-chlorophenyl)sulfonyl]dibenzo[b,d]furan-2-carbohydrazide IC50: 0.0372 mM Homo sapiens
N'-[(4-methylphenyl)sulfonyl]dibenzo[b,d]furan-2-carbohydrazide IC50: 0.051 mM Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
 Homo sapiens 5829
-

Organism

Organism UniProt Comment Textmining
Homo sapiens P54687
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-leucine + 2-oxoglutarate
-
 Homo sapiens 4-methyl-2-oxopentanoate + L-glutamate
-
 ?

Synonyms

Synonyms Comment Organism
BCATc
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0008
-
 IC50: 0.0008 mM, potent inhibitor Homo sapiens 5-chloro-N'-[[2-(trifluoromethyl)phenyl]sulfonyl]-1-benzofuran-2-carbohydrazide
0.00116
-
 IC50: 0.00116 mM Homo sapiens 5-chloro-N'-[(2-methylphenyl)sulfonyl]-1-benzofuran-2-carbohydrazide
0.0012
-
 IC50: 0.0012 mM Homo sapiens 5-chloro-N'-[(3-methylphenyl)sulfonyl]-1-benzofuran-2-carbohydrazide
0.00235
-
 IC50: 0.00235 mM Homo sapiens N'-(phenylsulfonyl)dibenzo[b,d]furan-2-carbohydrazide
0.0025
-
 IC50: 0.0025 mM Homo sapiens 5-bromo-N'-(phenylsulfonyl)-1-benzofuran-2-carbohydrazide
0.0028
-
 IC50: 0.0028 mM Homo sapiens N'-[(3-methylphenyl)sulfonyl]dibenzo[b,d]furan-2-carbohydrazide
0.0032
-
 IC50: 0.0032 mM Homo sapiens N'-[(2-methylphenyl)sulfonyl]dibenzo[b,d]furan-2-carbohydrazide
0.0042
-
 IC50: 0.0042 mM Homo sapiens 5-chloro-N'-(phenylsulfonyl)-1-benzofuran-2-carbohydrazide
0.0057
-
 IC50: 0.0057 mM Homo sapiens 5-chloro-N'-[(2-chlorophenyl)sulfonyl]-1-benzofuran-2-carbohydrazide
0.0128
-
 IC50: 0.0128 mM Homo sapiens 5-methoxy-N'-(phenylsulfonyl)-1-benzofuran-2-carbohydrazide
0.0129
-
 IC50: 0.0129 mM Homo sapiens N'-[(2-chlorophenyl)sulfonyl]dibenzo[b,d]furan-2-carbohydrazide
0.0133
-
 IC50: 0.0133 mM Homo sapiens N'-(phenylsulfonyl)quinoline-6-carbohydrazide
0.015
-
 IC50: 0.015 mM Homo sapiens 5-bromo-N'-(phenylsulfonyl)-1H-indole-2-carbohydrazide
0.0183
-
 IC50: 0.0183 mM Homo sapiens N'-(phenylsulfonyl)-1-benzofuran-2-carbohydrazide
0.0333
-
 IC50: 0.0333 mM Homo sapiens N'-(phenylsulfonyl)quinoline-3-carbohydrazide
0.035
-
 IC50: above 0.035 mM Homo sapiens N'-[(3-chlorophenyl)sulfonyl]dibenzo[b,d]furan-2-carbohydrazide
0.036
-
 IC50: 0.036 mM Homo sapiens N'-(phenylsulfonyl)-1H-indole-2-carbohydrazide
0.0372
-
 IC50: 0.0372 mM Homo sapiens N'-[(4-chlorophenyl)sulfonyl]dibenzo[b,d]furan-2-carbohydrazide
0.051
-
 IC50: 0.051 mM Homo sapiens N'-[(4-methylphenyl)sulfonyl]dibenzo[b,d]furan-2-carbohydrazide
0.0568
-
 IC50: 0.0568 mM Homo sapiens 5-methoxy-N'-(phenylsulfonyl)-1H-indole-2-carbohydrazide