Cytochrome P450 3A5 from Homo sapiens
Enzyme Description
Sequence
MDLIPNLAVETWLLLAVSLVLLYLYGTRTHGLFKRLGIPGPTPLPLLGNVLSYRQGLWKFDTECYKKYGKMWGTYEGQLPVLAITDPDVIRTVLVKECYSVFTNRRSLGPVGFMKSAISLAEDEEWKRIRSLLSPTFTSGKLKEMFPIIAQYGDVLVRNLRREAEKGKPVTLKDIFGAYSMDVITGTSFGVNIDSLNNPQDPFVESTKKFLKFGFLDPLFLSIILFPFLTPVFEALNVSLFPKDTINFLSKSVNRMKKSRLNDKQKHRLDFLQLMIDSQNSKETESHKALSDLELAAQSIIFIFAGYETTSSVLSFTLYELATHPDVQQKLQKEIDAVLPNKAPPTYDAVVQMEYLDMVVNETLRLFPVAIRLERTCKKDVEINGVFIPKGSMVVIPTYALHHDPKYWTEPEEFRPERFSKKKDSIDPYIYTPFGTGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLDTQGLLQPEKPIVLKVDSRDGTLSGE
Vanessa GonzΓ‘lez-PΓ©rez et al. (2012)
β Impact of Organic Solvents on Cytochrome P450 Probe Reactions: Filling the Gap with (S)-Warfarin and Midazolam Hydroxylation
Drug Metabolism and Disposition
Β· doi:10.1124/dmd.112.047134 β
Β· Activity - Classical
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Database ID
UniProt: P20815 β
Sequence Annotation
Inferred - from protein name
Protein Source
Recombinant, host insect cells
Experimental Data (18 measurements)
18 measurements
| Property | Assay | Solvent | Solvent Volume | Aqueous Reference | Measured Value | Units | Solution | pH | Temperature | Substrate(s) | Product(s) | Cofactor(s) | Shaking | Comments |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Dimethyl Sulfoxide (DMSO) | 0.1% | 100 | 93 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Isopropanol | 2% | 100 | 83 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Isopropanol | 1% | 100 | 101 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Isopropanol | 0.1% | 100 | 109 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Acetone | 2% | 100 | 47 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Acetone | 1% | 100 | 61 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Acetone | 0.1% | 100 | 100 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Dimethyl Sulfoxide (DMSO) | 2% | 100 | 48 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Dimethyl Sulfoxide (DMSO) | 1% | 100 | 58 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Acetonitrile | 0.1% | 100 | 122 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Ethanol | 2% | 100 | 113 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Ethanol | 1% | 100 | 108 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Ethanol | 0.1% | 100 | 110 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Methanol | 2% | 100 | 96 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Methanol | 1% | 100 | 96 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Methanol | 0.1% | 100 | 116 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Acetonitrile | 2% | 100 | 108 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
| Activity - Classical | Activity measured by HPLC-coupled mass spectrometry in the presence of organic solvent | Acetonitrile | 1% | 100 | 122 | % | 100 mM potassium phosphate buffer | 7.4 | 37Β°C | 4 Β΅M Midazolam | 1β²-Hydroxymidazolam | 1 mM NADPH | β | Classical aqueous control (in %) |
Visualization : Activity β Classical
One bar per measurement. Colour = solvent, shade = solvent volume. β β β Reference value. Hover for details.