Cloned (Comment) | Organism |
---|---|
expressed in Escherichia coli | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(4-benzylpiperidin-1-yl)[5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-1,2-oxazol-3-yl]methanone | - |
Homo sapiens | |
(E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-hydroxyphenyl)-isoxazol-3-yl)-1-(4-(2-methoxyphenyl)piperazin-1-yl)prop-2-en-1-one | - |
Homo sapiens | |
(E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-hydroxyphenyl)-isoxazol-3-yl)-1-(4-(3,4-dichlorophenyl)piperazin-1-yl)prop-2-en-1-one | - |
Homo sapiens | |
(E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-hydroxyphenyl)-isoxazol-3-yl)-1-(4-(3-(trifluoromethyl)phenyl)piperazin-1-yl)prop-2-en-1-one | - |
Homo sapiens | |
(E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-hydroxyphenyl)-isoxazol-3-yl)-1-(4-(3-methoxyphenyl)piperazin-1-yl)prop-2-en-1-one | - |
Homo sapiens | |
(E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-hydroxyphenyl)-isoxazol-3-yl)-1-(4-(4-methoxyphenyl)piperazin-1-yl)prop-2-en-1-one | - |
Homo sapiens | |
(E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-hydroxyphenyl)-isoxazol-3-yl)-1-(4-(pyridin-2-yl)piperazin-1-yl)prop-2-en-1-one | - |
Homo sapiens | |
(E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-hydroxyphenyl)-isoxazol-3-yl)-1-(4-(pyrimidin-2-yl)piperazin-1-yl)prop-2-en-1-one | - |
Homo sapiens | |
(E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-isoxazol-3-yl)-1-(4-(2-methoxyphenyl)piperazin-1-yl)prop-2-en-1-one | - |
Homo sapiens | |
(E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-isoxazol-3-yl)-1-(4-(3,4-dichlorophenyl)piperazin-1-yl)prop-2-en-1-one | - |
Homo sapiens | |
(E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-isoxazol-3-yl)-1-(4-(3-(trifluoromethyl)phenyl)piperazin-1-yl)prop-2-en-1-one | - |
Homo sapiens | |
(E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-isoxazol-3-yl)-1-(4-(3-methoxyphenyl)piperazin-1-yl)prop-2-en-1-one | - |
Homo sapiens | |
(E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-isoxazol-3-yl)-1-(4-(4-methoxyphenyl)piperazin-1-yl)prop-2-en-1-one | - |
Homo sapiens | |
(E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-isoxazol-3-yl)-1-(4-(pyridin-2-yl)piperazin-1-yl)prop-2-en-1-one | - |
Homo sapiens | |
(E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-isoxazol-3-yl)-1-(4-(pyrimidin-2-yl)piperazin-1-yl)prop-2-en-1-one | - |
Homo sapiens | |
(E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-isoxazol-3-yl)-1-(4-phenylpiperazin-1-yl)prop-2-en-1-one | - |
Homo sapiens | |
4-[[5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-1,2-oxazole-3-carbonyl]amino]-N-ethylpiperidine-1-carboxamide | - |
Homo sapiens | |
5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-N-(pyridin-4-yl)-1,2-oxazole-3-carboxamide | - |
Homo sapiens | |
5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-N-[1-(2-methylpropyl)piperidin-4-yl]-1,2-oxazole-3-carboxamide | - |
Homo sapiens | |
5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-N-[1-[(4-methoxyphenyl)methyl]piperidin-4-yl]-1,2-oxazole-3-carboxamide | - |
Homo sapiens | |
5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-N-[1-[(pyridin-4-yl)methyl]piperidin-4-yl]-1,2-oxazole-3-carboxamide | - |
Homo sapiens | |
5-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)-1,2-oxazole-3-carboxamide | - |
Homo sapiens | |
5-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-[4-[(morpholin-4-yl)methyl]phenyl]-1,2-oxazole-3-carboxamide | - |
Homo sapiens | |
5-(5-chloro-2,4-dihydroxyphenyl)-N-[(2,4-dichlorophenyl)methyl]-4-(4-methoxyphenyl)-1,2-oxazole-3-carboxamide | - |
Homo sapiens | |
5-(5-chloro-2,4-dihydroxyphenyl)-N-[1-(cyclopropylmethyl)piperidin-4-yl]-4-(4-methoxyphenyl)-1,2-oxazole-3-carboxamide | - |
Homo sapiens | |
5-(5-chloro-2,4-dihydroxyphenyl)-N-[1-[(2,4-dichlorophenyl)methyl]piperidin-4-yl]-4-(4-methoxyphenyl)-1,2-oxazole-3-carboxamide | - |
Homo sapiens | |
5-(5-chloro-2,4-dihydroxyphenyl)-N-[4-(dimethylamino)phenyl]-4-(4-methoxyphenyl)-1,2-oxazole-3-carboxamide | - |
Homo sapiens | |
AUY922 | - |
Homo sapiens | |
AZD7545 | - |
Homo sapiens | |
Dichloroacetate | - |
Homo sapiens | |
M77976 | - |
Homo sapiens | |
methyl 4-[[5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-1,2-oxazole-3-carbonyl]amino]piperidine-1-sulfinate | - |
Homo sapiens | |
N-(1-acetylpiperidin-4-yl)-5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-1,2-oxazole-3-carboxamide | - |
Homo sapiens | |
N-(1-benzylpiperidin-4-yl)-5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-1,2-oxazole-3-carboxamide | - |
Homo sapiens | |
Nov3r | - |
Homo sapiens | |
radicicol | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + [pyruvate dehydrogenase A1 (acetyl-transferring)] | Homo sapiens | - |
ADP + [pyruvate dehydrogenase A1 (acetyl-transferring)] phosphate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q15118 | - |
- |
Purification (Comment) | Organism |
---|---|
nickel column chromatography | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
A-549 cell | - |
Homo sapiens | - |
H-460 cell | - |
Homo sapiens | - |
HCT-116 cell | - |
Homo sapiens | - |
MDA-MB-231 cell | - |
Homo sapiens | - |
NCI-H1299 cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + [pyruvate dehydrogenase A1 (acetyl-transferring)] | - |
Homo sapiens | ADP + [pyruvate dehydrogenase A1 (acetyl-transferring)] phosphate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
PDHK1 | - |
Homo sapiens |
pyruvate dehydrogenase kinase | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000017 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-N-[1-[(4-methoxyphenyl)methyl]piperidin-4-yl]-1,2-oxazole-3-carboxamide | |
0.000025 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(1-benzylpiperidin-4-yl)-5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-1,2-oxazole-3-carboxamide | |
0.000028 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-(5-chloro-2,4-dihydroxyphenyl)-N-[1-(cyclopropylmethyl)piperidin-4-yl]-4-(4-methoxyphenyl)-1,2-oxazole-3-carboxamide | |
0.000059 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-N-[1-[(pyridin-4-yl)methyl]piperidin-4-yl]-1,2-oxazole-3-carboxamide | |
0.000068 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-N-[1-(2-methylpropyl)piperidin-4-yl]-1,2-oxazole-3-carboxamide | |
0.00013 | - |
pH and temperature not specified in the publication | Homo sapiens | methyl 4-[[5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-1,2-oxazole-3-carbonyl]amino]piperidine-1-sulfinate | |
0.00015 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-[[5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-1,2-oxazole-3-carbonyl]amino]-N-ethylpiperidine-1-carboxamide | |
0.00016 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-(5-chloro-2,4-dihydroxyphenyl)-N-[1-[(2,4-dichlorophenyl)methyl]piperidin-4-yl]-4-(4-methoxyphenyl)-1,2-oxazole-3-carboxamide | |
0.00021 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(1-acetylpiperidin-4-yl)-5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-1,2-oxazole-3-carboxamide | |
0.00038 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-(5-chloro-2,4-dihydroxyphenyl)-N-[4-(dimethylamino)phenyl]-4-(4-methoxyphenyl)-1,2-oxazole-3-carboxamide | |
0.000491 | - |
pH and temperature not specified in the publication | Homo sapiens | (E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-isoxazol-3-yl)-1-(4-(3-methoxyphenyl)piperazin-1-yl)prop-2-en-1-one | |
0.000521 | - |
pH and temperature not specified in the publication | Homo sapiens | (E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-hydroxyphenyl)-isoxazol-3-yl)-1-(4-(pyrimidin-2-yl)piperazin-1-yl)prop-2-en-1-one | |
0.000557 | - |
pH and temperature not specified in the publication | Homo sapiens | (E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-isoxazol-3-yl)-1-(4-(4-methoxyphenyl)piperazin-1-yl)prop-2-en-1-one | |
0.00058 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-N-(pyridin-4-yl)-1,2-oxazole-3-carboxamide | |
0.000604 | - |
pH and temperature not specified in the publication | Homo sapiens | (E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-hydroxyphenyl)-isoxazol-3-yl)-1-(4-(2-methoxyphenyl)piperazin-1-yl)prop-2-en-1-one | |
0.00061 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)-1,2-oxazole-3-carboxamide | |
0.00061 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-(5-chloro-2,4-dihydroxyphenyl)-N-[(2,4-dichlorophenyl)methyl]-4-(4-methoxyphenyl)-1,2-oxazole-3-carboxamide | |
0.000776 | - |
pH and temperature not specified in the publication | Homo sapiens | (E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-hydroxyphenyl)-isoxazol-3-yl)-1-(4-(3-methoxyphenyl)piperazin-1-yl)prop-2-en-1-one | |
0.000845 | - |
pH and temperature not specified in the publication | Homo sapiens | (E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-isoxazol-3-yl)-1-(4-(2-methoxyphenyl)piperazin-1-yl)prop-2-en-1-one | |
0.000878 | - |
pH and temperature not specified in the publication | Homo sapiens | (E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-hydroxyphenyl)-isoxazol-3-yl)-1-(4-(pyridin-2-yl)piperazin-1-yl)prop-2-en-1-one | |
0.00095 | - |
pH and temperature not specified in the publication | Homo sapiens | 5-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-[4-[(morpholin-4-yl)methyl]phenyl]-1,2-oxazole-3-carboxamide | |
0.000952 | - |
pH and temperature not specified in the publication | Homo sapiens | (E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-hydroxyphenyl)-isoxazol-3-yl)-1-(4-(4-methoxyphenyl)piperazin-1-yl)prop-2-en-1-one | |
0.00105 | - |
pH and temperature not specified in the publication | Homo sapiens | (E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-isoxazol-3-yl)-1-(4-(pyridin-2-yl)piperazin-1-yl)prop-2-en-1-one | |
0.00107 | - |
pH and temperature not specified in the publication | Homo sapiens | (E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-isoxazol-3-yl)-1-(4-(pyrimidin-2-yl)piperazin-1-yl)prop-2-en-1-one | |
0.001417 | - |
pH and temperature not specified in the publication | Homo sapiens | (E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-hydroxyphenyl)-isoxazol-3-yl)-1-(4-(3,4-dichlorophenyl)piperazin-1-yl)prop-2-en-1-one | |
0.001916 | - |
pH and temperature not specified in the publication | Homo sapiens | (E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-isoxazol-3-yl)-1-(4-phenylpiperazin-1-yl)prop-2-en-1-one | |
0.002369 | - |
pH and temperature not specified in the publication | Homo sapiens | (E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-isoxazol-3-yl)-1-(4-(3-(trifluoromethyl)phenyl)piperazin-1-yl)prop-2-en-1-one | |
0.002949 | - |
pH and temperature not specified in the publication | Homo sapiens | (E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-hydroxyphenyl)-isoxazol-3-yl)-1-(4-(3-(trifluoromethyl)phenyl)piperazin-1-yl)prop-2-en-1-one | |
0.004306 | - |
pH and temperature not specified in the publication | Homo sapiens | (E)-3-(5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-isoxazol-3-yl)-1-(4-(3,4-dichlorophenyl)piperazin-1-yl)prop-2-en-1-one | |
0.01 | - |
IC50 above 0.01 mM, pH and temperature not specified in the publication | Homo sapiens | (4-benzylpiperidin-1-yl)[5-(5-chloro-2,4-dihydroxyphenyl)-4-(4-methoxyphenyl)-1,2-oxazol-3-yl]methanone | |
0.0113 | - |
pH and temperature not specified in the publication | Homo sapiens | AUY922 |