Cloned (Comment) | Organism |
---|---|
the catalytic domain is expressed in Sf9 insect cells | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
hanging drop vapor diffusion method, using 30% (w/v) PEG 3350, 0.1 M Tris pH 7.5, and 0.2 M MgCl2 | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(S)-N-(2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-(trifluoromethyl)-1H-imidazol-1-yl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide | - |
Homo sapiens | |
(S)-N-(2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-6-methyl-5-(4-methyl-1H-1,2,3-triazol-1-yl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide | - |
Homo sapiens | |
5-(1-(difluoromethyl)-1H-pyrazol-4-yl)-N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)phenyl)propyl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide | - |
Homo sapiens | |
6-methyl-N-[(1R)-1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide | - |
Homo sapiens | |
N-((1S)-1-(3-fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide | TAK-915 | Homo sapiens | |
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(1H-pyrazol-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide | - |
Homo sapiens | |
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(2-methylpyridin-4-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide | - |
Homo sapiens | |
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(3-methyl-1H-1,2,4-triazol-1-yl)pyrazolo-[1,5-a]pyrimidine-3-carboxamide | - |
Homo sapiens | |
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-methyl-1H-1,2,3-triazol-1-yl)pyrazolo-[1,5-a]pyrimidine-3-carboxamide | - |
Homo sapiens | |
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-methyl-1H-imidazol-1-yl)pyrazolo [1,5-a]pyrimidine-3-carboxamide | - |
Homo sapiens | |
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(6-methylpyridin-3-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide | - |
Homo sapiens | |
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(pyridin-2-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide | - |
Homo sapiens | |
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(tetrahydro-2H-pyran-4-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide | - |
Homo sapiens | |
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-isopropylpyrazolo[1,5-a]pyrimidine-3-carboxamide | - |
Homo sapiens | |
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)phenyl)propyl)-6-methyl-5-(3-methyl-1H-1,2,4-triazol-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide | - |
Homo sapiens | |
N-[(1S)-2-hydroxy-2-methyl-1-[4-(trifluoromethoxy)phenyl]propyl]-6-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide | - |
Homo sapiens | |
N-[(1S)-2-hydroxy-2-methyl-1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide | - |
Homo sapiens | |
N-[1-(4-methoxyphenyl)propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide | - |
Homo sapiens | |
N-[1-[3-fluoro-4-(trifluoromethoxy)phenyl]-2-hydroxy-2-methylpropyl]-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide | - |
Homo sapiens | |
N-[1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide | - |
Homo sapiens | |
TAK-915 | i.e. 2 N-((1S)-1-(3-fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
nucleoside 3',5'-cyclic phosphate + H2O | Homo sapiens | - |
nucleoside 5'-phosphate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
Mono Q column chromatography and Superdex 200 gel filtration | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
brain | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
3',5'-cAMP + H2O | - |
Homo sapiens | 5'-AMP | - |
? | |
3',5'-cGMP + H2O | - |
Homo sapiens | 5'-GMP | - |
? | |
nucleoside 3',5'-cyclic phosphate + H2O | - |
Homo sapiens | nucleoside 5'-phosphate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
PDE2A | - |
Homo sapiens |
phosphodiesterase 2A | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00000031 | - |
at pH 7.4 and 25°C | Homo sapiens | (S)-N-(2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-6-methyl-5-(4-methyl-1H-1,2,3-triazol-1-yl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide | |
0.00000051 | - |
at pH 7.4 and 25°C | Homo sapiens | N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)phenyl)propyl)-6-methyl-5-(3-methyl-1H-1,2,4-triazol-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide | |
0.00000077 | - |
at pH 7.4 and 25°C | Homo sapiens | N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(2-methylpyridin-4-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide | |
0.00000098 | - |
at pH 7.4 and 25°C | Homo sapiens | N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(6-methylpyridin-3-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide | |
0.0000012 | - |
at pH 7.4 and 25°C | Homo sapiens | N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-methyl-1H-imidazol-1-yl)pyrazolo [1,5-a]pyrimidine-3-carboxamide | |
0.0000012 | - |
at pH 7.4 and 25°C | Homo sapiens | N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(pyridin-2-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide | |
0.0000017 | - |
at pH 7.4 and 25°C | Homo sapiens | 5-(1-(difluoromethyl)-1H-pyrazol-4-yl)-N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)phenyl)propyl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide | |
0.0000051 | - |
at pH 7.4 and 25°C | Homo sapiens | N-[(1S)-2-hydroxy-2-methyl-1-[4-(trifluoromethoxy)phenyl]propyl]-6-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide | |
0.0000054 | - |
at pH 7.4 and 25°C | Homo sapiens | N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(1H-pyrazol-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide | |
0.0000054 | - |
at pH 7.4 and 25°C | Homo sapiens | N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-methyl-1H-1,2,3-triazol-1-yl)pyrazolo-[1,5-a]pyrimidine-3-carboxamide | |
0.0000071 | - |
at pH 7.4 and 25°C | Homo sapiens | (S)-N-(2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-(trifluoromethyl)-1H-imidazol-1-yl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide | |
0.00001 | - |
at pH 7.4 and 25°C | Homo sapiens | N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(tetrahydro-2H-pyran-4-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide | |
0.000011 | - |
at pH 7.4 and 25°C | Homo sapiens | N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(3-methyl-1H-1,2,4-triazol-1-yl)pyrazolo-[1,5-a]pyrimidine-3-carboxamide | |
0.000024 | - |
at pH 7.4 and 25°C | Homo sapiens | 6-methyl-N-[(1R)-1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide | |
0.000024 | - |
at pH 7.4 and 25°C | Homo sapiens | N-[1-[3-fluoro-4-(trifluoromethoxy)phenyl]-2-hydroxy-2-methylpropyl]-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide | |
0.000034 | - |
at pH 7.4 and 25°C | Homo sapiens | N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-isopropylpyrazolo[1,5-a]pyrimidine-3-carboxamide | |
0.000061 | - |
at pH 7.4 and 25°C | Homo sapiens | N-((1S)-1-(3-fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide | |
0.000061 | - |
at pH 7.4 and 25°C | Homo sapiens | TAK-915 | |
0.000066 | - |
at pH 7.4 and 25°C | Homo sapiens | N-[(1S)-2-hydroxy-2-methyl-1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide | |
0.00048 | - |
at pH 7.4 and 25°C | Homo sapiens | N-[1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide | |
0.0038 | - |
at pH 7.4 and 25°C | Homo sapiens | N-[1-(4-methoxyphenyl)propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide |