Cloned (Comment) | Organism |
---|---|
expressed in Escherichia coli BL21(DE3) cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3-[(4-cyanobenzene-1-sulfonyl)amino]benzamide | - |
Homo sapiens | |
4-chloro-N-(1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl)benzene-1-sulfonamide | - |
Homo sapiens | |
4-cyano-N-(1-oxo-1,2-dihydroisoquinolin-7-yl)benzene-1-sulfonamide | - |
Homo sapiens | |
4-cyano-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)benzene-1-sulfonamide | - |
Homo sapiens | |
4-cyano-N-phenylbenzene-1-sulfonamide | - |
Homo sapiens | |
5-(5,5-dimethyl-6-oxo-1,4-dihydropyridin-3-yl)-N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)thiophene-2-sulfonamide | - |
Homo sapiens | |
5-(5-ethyl-5-methyl-6-oxo-1,4-dihydropyridin-3-yl)-N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)thiophene-2-sulfonamide | - |
Homo sapiens | |
5-[(3R,4S)-3-fluoro-4-hydroxypyrrolidin-1-yl]-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)thiophene-2-sulfonamide | - |
Homo sapiens | |
5-[(3S,4R)-3-fluoro-4-hydroxypyrrolidin-1-yl]-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)thiophene-2-sulfonamide | - |
Homo sapiens | |
5-[(4R)-3,3-difluoro-4-hydroxypyrrolidin-1-yl]-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)thiophene-2-sulfonamide | - |
Homo sapiens | |
5-[(4S)-3,3-difluoro-4-hydroxypyrrolidin-1-yl]-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)thiophene-2-sulfonamide | - |
Homo sapiens | |
methotrexate | - |
Homo sapiens | |
N-(2-amino-4-oxo-3,4-dihydroquinazolin-6-yl)-4-cyanobenzene-1-sulfonamide | - |
Homo sapiens | |
N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-(4-hydroxypiperidin-1-yl)thiophene-2-sulfonamide | - |
Homo sapiens | |
N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide | LSN 3213128, potent and selective inhibitor | Homo sapiens | |
N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)-5-(6-oxo-1H-pyridin-3-yl)thiophene-2-sulfonamide | - |
Homo sapiens | |
N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)-5-[(3R)-3-hydroxy-1-piperidyl]thiophene-2-sulfonamide | - |
Homo sapiens | |
N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)-5-[(3S)-3-hydroxy-1-piperidyl]thiophene-2-sulfonamide | - |
Homo sapiens | |
N-[(4-[[(2-amino-4-oxo-3,4-dihydroquinazolin-6-yl)amino]sulfonyl]-phenyl)carbonyl]-L-glutamic acid | - |
Homo sapiens | |
pemetrexed | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
10-formyltetrahydrofolate + 5-amino-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide | Homo sapiens | - |
tetrahydrofolate + 5-formamido-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P31939 | - |
- |
Purification (Comment) | Organism |
---|---|
Ni-NTA agarose resin column chromatography and Superdex 200 gel filtration | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
MDA-MB-231-Met2 cell | - |
Homo sapiens | - |
NCI-H460 cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
10-formyltetrahydrofolate + 5-amino-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide | - |
Homo sapiens | tetrahydrofolate + 5-formamido-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide | - |
? |
Synonyms | Comment | Organism |
---|---|---|
AICARFT | - |
Homo sapiens |
aminoimidazole-4-carboxamide ribonucleotide formyltransferase | - |
Homo sapiens |
ATIC | bifunctional enzyme showing 5-aminoimidazole-4-carboxamide ribonucleotide transformylase and inosine monophosphate cyclohydrolase activities | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000005 | - |
IC50 below 0.000005 mM, at pH 7.5 and 25°C | Homo sapiens | 5-(5,5-dimethyl-6-oxo-1,4-dihydropyridin-3-yl)-N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)thiophene-2-sulfonamide | |
0.000005 | - |
IC50 below 0.000005 mM, at pH 7.5 and 25°C | Homo sapiens | 5-(5-ethyl-5-methyl-6-oxo-1,4-dihydropyridin-3-yl)-N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)thiophene-2-sulfonamide | |
0.000005 | - |
IC50 below 0.000005 mM, at pH 7.5 and 25°C | Homo sapiens | N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)-5-(6-oxo-1H-pyridin-3-yl)thiophene-2-sulfonamide | |
0.0000078 | - |
at pH 7.5 and 25°C | Homo sapiens | 5-[(3S,4R)-3-fluoro-4-hydroxypyrrolidin-1-yl]-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)thiophene-2-sulfonamide | |
0.000012 | - |
at pH 7.5 and 25°C | Homo sapiens | 5-[(4R)-3,3-difluoro-4-hydroxypyrrolidin-1-yl]-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)thiophene-2-sulfonamide | |
0.000013 | - |
at pH 7.5 and 25°C | Homo sapiens | 5-[(4S)-3,3-difluoro-4-hydroxypyrrolidin-1-yl]-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)thiophene-2-sulfonamide | |
0.000013 | - |
at pH 7.5 and 25°C | Homo sapiens | N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-(4-hydroxypiperidin-1-yl)thiophene-2-sulfonamide | |
0.000014 | - |
at pH 7.5 and 25°C | Homo sapiens | N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide | |
0.000016 | - |
at pH 7.5 and 25°C | Homo sapiens | N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide | |
0.000018 | - |
at pH 7.5 and 25°C | Homo sapiens | N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)-5-[(3S)-3-hydroxy-1-piperidyl]thiophene-2-sulfonamide | |
0.00002 | - |
at pH 7.5 and 25°C | Homo sapiens | 5-[(3R,4S)-3-fluoro-4-hydroxypyrrolidin-1-yl]-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)thiophene-2-sulfonamide | |
0.000026 | - |
at pH 7.5 and 25°C | Homo sapiens | N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)-5-[(3R)-3-hydroxy-1-piperidyl]thiophene-2-sulfonamide | |
0.000608 | - |
at pH 7.5 and 25°C | Homo sapiens | 4-cyano-N-(1-oxo-1,2-dihydroisoquinolin-7-yl)benzene-1-sulfonamide | |
0.000723 | - |
at pH 7.5 and 25°C | Homo sapiens | 4-cyano-N-(6-fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)benzene-1-sulfonamide | |
0.0181 | - |
at pH 7.5 and 25°C | Homo sapiens | N-(2-amino-4-oxo-3,4-dihydroquinazolin-6-yl)-4-cyanobenzene-1-sulfonamide | |
0.0348 | - |
at pH 7.5 and 25°C | Homo sapiens | 4-chloro-N-(1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl)benzene-1-sulfonamide | |
0.09 | - |
at pH 7.5 and 25°C | Homo sapiens | 3-[(4-cyanobenzene-1-sulfonyl)amino]benzamide | |
0.1 | - |
IC50 above 0.1 mM, at pH 7.5 and 25°C | Homo sapiens | 4-cyano-N-phenylbenzene-1-sulfonamide |