Activating Compound | Comment | Organism | Structure |
---|---|---|---|
ascorbate | - |
Homo sapiens |
Cloned (Comment) | Organism |
---|---|
expression of His-tagged human PHD3 in Escherichia coli strain BL21(DE3) | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1,1',1'',1'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetrapropan-2-ol | chelates Fe2+ in a hexacoordinative mode through four nitrogens of the macrocycle and two oxygens in side arms | Homo sapiens | |
2,2',2'',2'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetamide | chelates Fe2+ in a hexacoordinative mode through four nitrogens of the macrocycle and two oxygens in side arms | Homo sapiens | |
3,6,9-tris(naphthalen-1-ylmethyl)-3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-triene | coordinates Fe2+ via triad or tetrad from nitrogen atoms of the parent ring, which leaves vacant position for other ligands binding | Homo sapiens | |
additional information | inhibition of the recombinant human PHD3 activity by tetraazamacrocycles, overview | Homo sapiens | |
N,N-dimethyl-5-[3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-trien-6-ylsulfonyl]naphthalen-1-amine | coordinates Fe2+ via triad or tetrad from nitrogen atoms of the parent ring, which leaves vacant position for other ligands binding | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | kinetics, overview | Homo sapiens | |
0.067 | - |
hypoxia-inducible factor-L-proline | recombinant enzyme, pH 7.0, 37°C | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Fe2+ | dependent on | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
hypoxia-inducible factor-L-proline + 2-oxoglutarate + O2 | Homo sapiens | - |
hypoxia-inducible factor-trans-4-hydroxy-L-proline + succinate + CO2 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
recombinant His-tagged enzyme from Escherichia coli strain BL21(DE3) by nickel affinity chromatography | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
hypoxia-inducible factor-L-proline + 2-oxoglutarate + O2 | - |
Homo sapiens | hypoxia-inducible factor-trans-4-hydroxy-L-proline + succinate + CO2 | - |
? |
Synonyms | Comment | Organism |
---|---|---|
HIF-1alpha prolyl hydroxylase 3 | - |
Homo sapiens |
PHD3 | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00191 | - |
3,6,9-tris(naphthalen-1-ylmethyl)-3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-triene | recombinant enzyme, pH 7.0, 37°C | Homo sapiens | |
0.00249 | - |
N,N-dimethyl-5-[3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-trien-6-ylsulfonyl]naphthalen-1-amine | recombinant enzyme, pH 7.0, 37°C | Homo sapiens | |
0.00628 | - |
1,1',1'',1'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetrapropan-2-ol | recombinant enzyme, pH 7.0, 37°C | Homo sapiens | |
0.00998 | - |
2,2',2'',2'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetamide | recombinant enzyme, pH 7.0, 37°C | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0103 | - |
recombinant enzyme, pH 7.0, 37°C | Homo sapiens | 3,6,9-tris(naphthalen-1-ylmethyl)-3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-triene | |
0.0207 | - |
recombinant enzyme, pH 7.0, 37°C | Homo sapiens | N,N-dimethyl-5-[3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-trien-6-ylsulfonyl]naphthalen-1-amine | |
0.0309 | - |
recombinant enzyme, pH 7.0, 37°C | Homo sapiens | 2,2',2'',2'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetamide | |
0.0397 | - |
recombinant enzyme, pH 7.0, 37°C | Homo sapiens | 1,1',1'',1'''-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetrapropan-2-ol |