Cloned (Comment) | Organism |
---|---|
cloning of rod PDE6 alpha and beta subunits and cone PDE6alpha', expression in Sf9 cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-bromo-5-ethyl-7,8-dihydro-1-[(4-hydroxyphenyl)methyl]-7(R)-(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one | - |
Homo sapiens | |
3,7-dihydro-8-[(1-hydroxymethyl)-3-cyclopenten-1-yl]amino-7-[(4-methoxyphenyl)methyl]-1,3-dimethyl-1H-purine-2,6-dione | - |
Homo sapiens | |
3-isobutyl-1-methylxanthine | - |
Homo sapiens | |
5-ethyl-7,8-dihydro-2,7(R)-bis(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one | - |
Homo sapiens | |
8-bromo-1-ethyl-3,7-dihydro-7-[(4-methoxyphenyl)methyl]-3-(2-methylpropyl)-1H-purine-2,6-dione | - |
Homo sapiens | |
E4021 | - |
Homo sapiens | |
additional information | recombinant and native PDE6s exhibit differential sensitivity to inhibitors. This data caution the use of recombinant catalytic subunits of PDE6 in drug discovery or in structural/functional studies | Homo sapiens | |
sildenafil | - |
Homo sapiens | |
zaprinast | - |
Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
recombinant and native | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
photoreceptor | - |
Homo sapiens | - |
retinal cone | - |
Homo sapiens | - |
retinal rod | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
3',5'-cGMP + H2O | - |
Homo sapiens | 5'-GMP | - |
? |
Synonyms | Comment | Organism |
---|---|---|
PDE6 | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0000026 | - |
8-bromo-1-ethyl-3,7-dihydro-7-[(4-methoxyphenyl)methyl]-3-(2-methylpropyl)-1H-purine-2,6-dione | 30°C, pH 7.4, recombinant rod PDE6alphabeta | Homo sapiens | |
0.0000035 | - |
E4021 | 30°C, pH 7.4, native PDE6 | Homo sapiens | |
0.0000036 | - |
8-bromo-1-ethyl-3,7-dihydro-7-[(4-methoxyphenyl)methyl]-3-(2-methylpropyl)-1H-purine-2,6-dione | 30°C, pH 7.4, recombinant cone PDE6alpha' | Homo sapiens | |
0.0000173 | - |
5-ethyl-7,8-dihydro-2,7(R)-bis(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one | 30°C, pH 7.4, native PDE6 | Homo sapiens | |
0.0000183 | - |
8-bromo-1-ethyl-3,7-dihydro-7-[(4-methoxyphenyl)methyl]-3-(2-methylpropyl)-1H-purine-2,6-dione | 30°C, pH 7.4, native PDE6 | Homo sapiens | |
0.0000245 | - |
sildenafil | 30°C, pH 7.4, native PDE6 | Homo sapiens | |
0.0000487 | - |
3,7-dihydro-8-[(1-hydroxymethyl)-3-cyclopenten-1-yl]amino-7-[(4-methoxyphenyl)methyl]-1,3-dimethyl-1H-purine-2,6-dione | 30°C, pH 7.4, recombinant rod PDE6alphabeta | Homo sapiens | |
0.0000546 | - |
3,7-dihydro-8-[(1-hydroxymethyl)-3-cyclopenten-1-yl]amino-7-[(4-methoxyphenyl)methyl]-1,3-dimethyl-1H-purine-2,6-dione | 30°C, pH 7.4, recombinant cone PDE6alpha' | Homo sapiens | |
0.0000936 | - |
sildenafil | 30°C, pH 7.4, recombinant rod PDE6alphabeta | Homo sapiens | |
0.0000984 | - |
sildenafil | 30°C, pH 7.4, recombinant cone PDE6alpha' | Homo sapiens | |
0.0001014 | - |
E4021 | 30°C, pH 7.4, recombinant rod PDE6alphabeta | Homo sapiens | |
0.0001735 | - |
E4021 | 30°C, pH 7.4, recombinant cone PDE6alpha' | Homo sapiens | |
0.000176 | - |
2-bromo-5-ethyl-7,8-dihydro-1-[(4-hydroxyphenyl)methyl]-7(R)-(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one | 30°C, pH 7.4, native PDE6 | Homo sapiens | |
0.0001778 | - |
zaprinast | 30°C, pH 7.4, native PDE6 | Homo sapiens | |
0.0003616 | - |
2-bromo-5-ethyl-7,8-dihydro-1-[(4-hydroxyphenyl)methyl]-7(R)-(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one | 30°C, pH 7.4, recombinant rod PDE6alphabeta | Homo sapiens | |
0.0006608 | - |
2-bromo-5-ethyl-7,8-dihydro-1-[(4-hydroxyphenyl)methyl]-7(R)-(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one | 30°C, pH 7.4, recombinant cone PDE6alpha' | Homo sapiens | |
0.0007215 | - |
3,7-dihydro-8-[(1-hydroxymethyl)-3-cyclopenten-1-yl]amino-7-[(4-methoxyphenyl)methyl]-1,3-dimethyl-1H-purine-2,6-dione | 30°C, pH 7.4, native PDE6 | Homo sapiens | |
0.001206 | - |
5-ethyl-7,8-dihydro-2,7(R)-bis(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one | 30°C, pH 7.4, recombinant rod PDE6alphabeta | Homo sapiens | |
0.001605 | - |
5-ethyl-7,8-dihydro-2,7(R)-bis(phenylmethyl)-1H-imidazo[2,1-b]purin-4(5H)-one | 30°C, pH 7.4, recombinant cone PDE6alpha' | Homo sapiens | |
0.01145 | - |
zaprinast | 30°C, pH 7.4 cone PDE6alpha' | Homo sapiens | |
0.01212 | - |
3-isobutyl-1-methylxanthine | 30°C, pH 7.4, native PDE6 | Homo sapiens | |
0.01438 | - |
zaprinast | 30°C, pH 7.4 rod PDE6alphabeta | Homo sapiens | |
0.06084 | - |
3-isobutyl-1-methylxanthine | 30°C, pH 7.4, recombinant rod PDE6alphabeta | Homo sapiens | |
0.09485 | - |
3-isobutyl-1-methylxanthine | 30°C, pH 7.4, recombinant | Homo sapiens |