| Assay ID | Title | Year | Journal | Article |
|---|
| AID1223625 | Inhibition of human MetAP2 assessed as remaining enzyme activity after 8 hrs | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223664 | Activity of rat recombinant CYP3A5 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-((E)-4-hydroxy-3-methylbut-2-en-1-yl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation per pmol of enzyme | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223604 | Inhibition of MetAP2 level in Sprague-Dawley rat thymus assessed as free enzyme level at 0.3 mg/kg, po by ELISA | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223610 | Ratio of Vmax to Km for rat recombinant CYP3A4 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-(((S)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223607 | Inhibition of MetAP2 level in Sprague-Dawley rat liver assessed as free enzyme level at 0.3 mg/kg, iv by ELISA | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223634 | Apparent oral clearance in non-Hodgkin lymphoma patient at 15 mg, po alternate days for 21 days | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223614 | Activity of rat recombinant CYP3A5 assessed as ((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-hydroxy-3-methyl-1-oxobutan-2-yl)carbamate) formation | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223612 | Ratio of Vmax to Km for rat recombinant CYP3A4 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-((E)-4-hydroxy-3-methylbut-2-en-1-yl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223657 | Activity of rat recombinant CYP3A4 assessed as ((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-hydroxy-3-methyl-1-oxobutan-2-yl)carbamate) formation per pmol of enzyme | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223581 | Inhibition of MetAP2 level in Sprague-Dawley rat lymph nodes assessed as free enzyme level at 3 mg/kg, po by ELISA | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223615 | Activity of rat recombinant CYP3A4 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-(((R)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223609 | Ratio of Vmax to Km for rat recombinant CYP3A5 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-(((R)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223591 | Metabolic stability in dog liver microsomes assessed as retention time of ((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-hydroxy-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM by LC | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223602 | Inhibition of MetAP2 level in Sprague-Dawley rat liver assessed as free enzyme level at 0.3 mg/kg, po by ELISA | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223644 | Ratio of Vmax to Km for rat recombinant CYP3A4 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-(((R)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223623 | Inhibition of CYP3A4 activity in human liver microsomes using nifedipine as a substrate by LC/MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223659 | Activity of rat recombinant CYP3A4 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-(((R)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation per pmol of enzyme | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223647 | Inhibition of MetAP2 level in Sprague-Dawley rat thymus assessed as free enzyme level at 0.3 mg/kg, iv by ELISA | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223661 | Activity of rat recombinant CYP3A4 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-(((S)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation per pmol of enzyme | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223624 | Inhibition of CYP3A4 activity in human liver microsomes using testosterone as a substrate by LC/MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223632 | AUC (0 to infinity) in non-Hodgkin lymphoma patient at 15 mg, po alternate days for 21 days | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223626 | Inhibition of human MetAP2 assessed as remaining enzyme activity after 1 hr | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223628 | Inhibition of MetAP2 activity in HUVEC assessed as inhibition of cell proliferation by MTT assay | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223618 | Activity of rat recombinant CYP3A5 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-(((S)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223646 | Inhibition of MetAP2 level in Sprague-Dawley rat lymph nodes assessed as free enzyme level at 0.3 mg/kg, iv by ELISA | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223608 | Inhibition of MetAP2 level in Sprague-Dawley rat lung assessed as free enzyme level at 3 mg/kg, po by ELISA | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223584 | Metabolic stability in mouse liver microsomes assessed as retention time of ((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-hydroxy-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM by | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223630 | Cmax in non-Hodgkin lymphoma patient at 15 mg, po alternate days for 21 days | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223606 | Inhibition of MetAP2 level in Sprague-Dawley rat liver assessed as free enzyme level at 3 mg/kg, po by ELISA | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223652 | Metabolic stability in rat liver S9 fraction assessed as retention time of glutathione conjugate at 5 mM by LC/MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223658 | Activity of rat recombinant CYP3A5 assessed as ((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-hydroxy-3-methyl-1-oxobutan-2-yl)carbamate) formation per pmol of enzyme | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223582 | Inhibition of MetAP2 level in Sprague-Dawley rat thymus assessed as free enzyme level at 3 mg/kg, po by ELISA | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223592 | Metabolic stability in dog liver microsomes assessed as retention time of ((3R,4S,5S,6R)-4-((2R,3R)-3-(((R)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM b | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223588 | Metabolic stability in rat liver microsomes assessed as retention time of ((3R,4S,5S,6R)-4-((2R,3R)-3-(((R)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM b | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223665 | Ratio of Vmax to Km for rat recombinant CYP3A4 assessed as ((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-hydroxy-3-methyl-1-oxobutan-2-yl)carbamate) formation | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223596 | Metabolic stability in monkey liver microsomes assessed as retention time of ((3R,4S,5S,6R)-4-((2R,3R)-3-(((R)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) at 5 m | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223619 | Activity of rat recombinant CYP3A4 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-((E)-4-hydroxy-3-methylbut-2-en-1-yl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223622 | Inhibition of CYP3A4 activity in human liver microsomes using midazolam as a substrate by LC/MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223616 | Activity of rat recombinant CYP3A5 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-(((R)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223590 | Metabolic stability in rat liver microsomes assessed as retention time of ((3R,4S,5S,6R)-4-((2R,3R)-3-((E)-4-hydroxy-3-methylbut-2-en-1-yl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM by | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223613 | Ratio of Vmax to Km for rat recombinant CYP3A5 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-((E)-4-hydroxy-3-methylbut-2-en-1-yl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223635 | Oral steady-state volume of distribution in non-Hodgkin lymphoma patient at 15 mg, po alternate days for 21 days | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223601 | Metabolic stability in mouse liver microsomes assessed as retention time of ((3R,4S,5S,6R)-4-((2R,3R)-3-(((S)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223621 | Inhibition of CYP3A4 activity in human liver microsomes assessed as dibenzo fluuorescene oxidation up to 40 uM | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223643 | Ratio of Vmax to Km for rat recombinant CYP3A5 assessed as ((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-hydroxy-3-methyl-1-oxobutan-2-yl)carbamate) formation | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223620 | Activity of rat recombinant CYP3A5 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-((E)-4-hydroxy-3-methylbut-2-en-1-yl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223598 | Metabolic stability in monkey liver microsomes assessed as retention time of ((3R,4S,5S,6R)-4-((2R,3R)-3-((E)-4-hydroxy-3-methylbut-2-en-1-yl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223662 | Activity of rat recombinant CYP3A5 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-(((S)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation per pmol of enzyme | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223594 | Metabolic stability in dog liver microsomes assessed as retention time of ((3R,4S,5S,6R)-4-((2R,3R)-3-((E)-4-hydroxy-3-methylbut-2-en-1-yl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM by | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223653 | Activity of rat recombinant CYP3A4 assessed as ((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-hydroxy-3-methyl-1-oxobutan-2-yl)carbamate) formation | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223595 | Metabolic stability in monkey liver microsomes assessed as retention time of ((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-hydroxy-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM by | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223629 | Tmax in non-Hodgkin lymphoma patient at 15 mg, po alternate days for 21 days | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223585 | Metabolic stability in mouse liver microsomes assessed as retention time of ((3R,4S,5S,6R)-4-((2R,3R)-3-(((R)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223605 | Inhibition of MetAP2 level in Sprague-Dawley rat whole blood assessed as free enzyme level at 0.3 mg/kg, po by ELISA | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223583 | Inhibition of MetAP2 level in Sprague-Dawley rat whole blood assessed as free enzyme level at 3 mg/kg, po by ELISA | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223645 | Inhibition of MetAP2 level in Sprague-Dawley rat whole blood assessed as free enzyme level at 0.3 mg/kg, iv by ELISA | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223633 | Half life in non-Hodgkin lymphoma patient at 15 mg, po alternate days for 21 days | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223649 | Metabolic stability in human liver microsomes assessed as retention time of ((3R,4S,5S,6R)-4-((2R,3R)-3-(((R)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223611 | Ratio of Vmax to Km for rat recombinant CYP3A5 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-(((S)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223651 | Metabolic stability in human liver microsomes assessed as retention time of ((3R,4S,5S,6R)-4-((2R,3R)-3-((E)-4-hydroxy-3-methylbut-2-en-1-yl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223597 | Metabolic stability in monkey liver microsomes assessed as retention time of ((3R,4S,5S,6R)-4-((2R,3R)-3-(((S)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) at 5 m | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223650 | Metabolic stability in human liver microsomes assessed as retention time of ((3R,4S,5S,6R)-4-((2R,3R)-3-(((S)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223617 | Activity of rat recombinant CYP3A4 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-(((S)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223599 | Metabolic stability in human liver microsomes assessed as retention time of ((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-hydroxy-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM by | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223593 | Metabolic stability in dog liver microsomes assessed as retention time of ((3R,4S,5S,6R)-4-((2R,3R)-3-(((S)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM b | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223587 | Metabolic stability in rat liver microsomes assessed as retention time of ((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-hydroxy-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM by LC | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223603 | Inhibition of MetAP2 level in Sprague-Dawley rat lymph nodes assessed as free enzyme level at 0.3 mg/kg, po by ELISA | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223663 | Activity of rat recombinant CYP3A4 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-((E)-4-hydroxy-3-methylbut-2-en-1-yl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation per pmol of enzyme | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223586 | Metabolic stability in mouse liver microsomes assessed as retention time of ((3R,4S,5S,6R)-4-((2R,3R)-3-((E)-4-hydroxy-3-methylbut-2-en-1-yl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223631 | AUC (0 to t hrs) in non-Hodgkin lymphoma patient at 15 mg, po alternate days for 21 days | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223600 | Inhibition of MetAP2 level in Sprague-Dawley rat lung assessed as free enzyme level at 0.3 mg/kg, po by ELISA | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223589 | Metabolic stability in rat liver microsomes assessed as retention time of ((3R,4S,5S,6R)-4-((2R,3R)-3-(((S)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) at 5 mM b | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223648 | Inhibition of MetAP2 level in Sprague-Dawley rat lung assessed as free enzyme level at 0.3 mg/kg, iv by ELISA | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| AID1223660 | Activity of rat recombinant CYP3A5 assessed as ((3R,4S,5S,6R)-4-((2R,3R)-3-(((R)-3,3-dimethyloxiran-2-yl)methyl)-2-methyloxiran-2-yl)-5-methoxy-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate) formation per pmol of enzyme | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
| Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |