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Literature summary for 2.7.11.4 extracted from

  • Tso, S.C.; Gui, W.J.; Wu, C.Y.; Chuang, J.L.; Qi, X.; Skvora, K.J.; Dork, K.; Wallace, A.L.; Morlock, L.K.; Lee, B.H.; Hutson, S.M.; Strom, S.C.; Williams, N.S.; Tambar, U.K.; Wynn, R.M.; Chuang, D.T.
    Benzothiophene carboxylate derivatives as novel allosteric inhibitors of branched-chain alpha-ketoacid dehydrogenase kinase (2014), J. Biol. Chem., 289, 20583-20593.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with 3,6-dichlorobenzo[b]thiophene-2-carboxylic acid Homo sapiens
in complex with 3,6-dichlorobenzo[b]thiophene-2-carboxylic acid Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
3,6-dichlorobenzo[b]thiophene-2-carboxylic acid
-
Homo sapiens
3,6-dichlorobenzo[b]thiophene-2-carboxylic acid
-
Mus musculus
3-chloro-6-fluorobenzo[b]thiophene-2-carboxylic acid
-
Homo sapiens
3-chloro-6-fluorobenzo[b]thiophene-2-carboxylic acid
-
Mus musculus
N,N'-(1,2,5-oxadiazole-3,4-diyl)bis(3,6-dichlorobenzo[b]thiophene-2-carboxamide
-
Homo sapiens
N,N'-(1,2,5-oxadiazole-3,4-diyl)bis(3,6-dichlorobenzo[b]thiophene-2-carboxamide
-
Mus musculus
N-(4-acetamido-1,2,5-oxadiazol-3-yl)-3,6-dichlorobenzo[b]thiophene-2-carboxamide
-
Homo sapiens
N-(4-acetamido-1,2,5-oxadiazol-3-yl)-3,6-dichlorobenzo[b]thiophene-2-carboxamide
-
Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + [3-methyl-2-oxobutanoate dehydrogenase (acetyl-transferring)] Homo sapiens
-
ADP + [3-methyl-2-oxobutanoate dehydrogenase (acetyl-transferring)] phosphate
-
?
ATP + [3-methyl-2-oxobutanoate dehydrogenase (acetyl-transferring)] Mus musculus
-
ADP + [3-methyl-2-oxobutanoate dehydrogenase (acetyl-transferring)] phosphate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q14874
-
-
Mus musculus O55028
-
-

Source Tissue

Source Tissue Comment Organism Textmining
heart
-
Mus musculus
-
kidney
-
Mus musculus
-
liver
-
Mus musculus
-
lymphoblast
-
Homo sapiens
-
MEF cell
-
Mus musculus
-
muscle
-
Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + [3-methyl-2-oxobutanoate dehydrogenase (acetyl-transferring)]
-
Homo sapiens ADP + [3-methyl-2-oxobutanoate dehydrogenase (acetyl-transferring)] phosphate
-
?
ATP + [3-methyl-2-oxobutanoate dehydrogenase (acetyl-transferring)]
-
Mus musculus ADP + [3-methyl-2-oxobutanoate dehydrogenase (acetyl-transferring)] phosphate
-
?

Synonyms

Synonyms Comment Organism
BCKDC kinase
-
Homo sapiens
BCKDC kinase
-
Mus musculus
BDK
-
Homo sapiens
BDK
-
Mus musculus
branched-chain alpha-ketoacid dehydrogenase kinase
-
Homo sapiens
branched-chain alpha-ketoacid dehydrogenase kinase
-
Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00319
-
pH and temperature not specified in the publication Homo sapiens 3,6-dichlorobenzo[b]thiophene-2-carboxylic acid
0.00319
-
pH and temperature not specified in the publication Mus musculus 3,6-dichlorobenzo[b]thiophene-2-carboxylic acid