| Assay ID | Title | Year | Journal | Article |
|---|
| AID351506 | Cmax in Sprague-Dawley rat at 5 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351526 | Selectivity ratio of IC50 for DPP3 in human erythrocytes to IC50 for human plasma DPP4 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351499 | Metabolic stability in human liver microsomes assessed as intrinsic clearance | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351493 | Apparent permeability from apical to basolateral side in MDCK cells | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351513 | Clearance in dog plasma at 1 mg/kg, iv and 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351529 | Selectivity ratio of IC50 for human FAP expressed in african green monkey COS1 cells to IC50 for human plasma DPP4 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351516 | Bioavailability in dog at 1 mg/kg, iv and 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID1220297 | Drug level in urine of Sprague-Dawley rat treated with [14C]PF-00734200 at 5 mg/kg, po administered as single dose by LC-MS/MS method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID351515 | Half life in dog at 1 mg/kg, iv and 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351534 | Inhibition of CYP2D6 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351491 | Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells at 10 uM | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351508 | Volume of distribution at steady state in cynomolgus monkey at 1 mg/kg, iv and 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID1220318 | Drug level in feces of beagle dog treated with [14C]PF-00734200 at 5 mg/kg, po administered as single dose by LC-MS/MS method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID351507 | Clearance in cynomolgus monkey plasma at 1 mg/kg, iv and 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID1220313 | Tmax in human treated with [14C]PF-00734200 at 20 mg/kg, po administered as single dose | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID351509 | Half life in cynomolgus monkey at 1 mg/kg, iv and 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351533 | Inhibition of CYP2C19 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351538 | Fraction unbound in dog | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351678 | Fraction unbound in human | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID1220317 | Drug level in urine of beagle dog treated with [14C]PF-00734200 at 5 mg/kg, po administered as single dose by LC-MS/MS method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID351536 | Ex vivo inhibition of DPP4 in Sprague-Dawley rat | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID1220324 | Drug level in beagle dog plasma treated with [14C]PF-00734200 at 5 mg/kg, po administered as single dose by LC-MS/MS method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID1220309 | AUC (0 to infinity) in human treated with [14C]PF-00734200 at 20 mg/kg, po administered as single dose | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID351505 | AUC in Sprague-Dawley rat at 5 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID1220330 | Drug metabolism assessed as human CYP3A4-mediated metabolite (3,3-difluoropyrrolidin-1-yl){(2S,4S)-4-[4-(5-hydroxypyrimidin-2-yl)piperazin-1-yl]pyrrolidin-2-yl}methanone formation by LC-MS/MS method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID351502 | Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv and 5 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID1220329 | Drug metabolism assessed as human CYP2D6-mediated metabolite (3,3-difluoropyrrolidin-1-yl){(2S,4S)-4-[4-(5-hydroxypyrimidin-2-yl)piperazin-1-yl]pyrrolidin-2-yl}methanone formation by LC-MS/MS method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID1220320 | Drug level in urine of human treated with [14C]PF-00734200 at 20 mg/kg, po administered as single dose by LC-MS/MS method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID351523 | Inhibition of APP in human leukocytes | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351520 | Inhibition of rat plasma DPP4 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351521 | Inhibition of DPP3 in human erythrocytes | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351497 | Inhibition of human ERG by patch-clamp technique | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351519 | Inhibition of human plasma DPP4 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351527 | Selectivity ratio of IC50 for human DPP9 to IC50 for human plasma DPP4 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351522 | Inhibition of human DPP9 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID1220316 | Oral clearance in human treated with [14C]PF-00734200 at 20 mg/kg, po administered as single dose | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID1220321 | Drug level in feces of human treated with [14C]PF-00734200 at 20 mg/kg, po administered as single dose by LC-MS/MS method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID1220298 | Drug level in feces of Sprague-Dawley rat treated with [14C]PF-00734200 at 5 mg/kg, po administered as single dose by LC-MS/MS method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID351518 | Cmax in dog at 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID1220323 | Drug level in Sprague-Dawley rat plasma treated with [14C]PF-00734200 at 5 mg/kg, po administered as single dose by LC-MS/MS method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID351501 | Clearance in Sprague-Dawley rat plasma at 1 mg/kg, iv and 5 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID1395907 | Elimination half life in human | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. |
| AID351524 | Inhibition of human FAP expressed in african green monkey COS1 cells | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351535 | Inhibition of CYP3A4 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID1220315 | Elimination half life in human treated with [14C]PF-00734200 at 20 mg/kg, po administered as single dose | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID351517 | AUC in dog at 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351496 | Inhibition of human recombinant DPP2 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351510 | Bioavailability in cynomolgus monkey at 1 mg/kg, iv and 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351537 | Fraction unbound in rat | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351528 | Selectivity ratio of IC50 for APP in human leukocytes to IC50 for human plasma DPP4 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351680 | Terminal half life in human at 0.3 to 300 mg | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351512 | Cmax in cynomolgus monkey at 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351679 | Tmax in human at 0.3 to 300 mg | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351677 | Fraction unbound in monkey | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID1220335 | Total drug level in Sprague-Dawley rat treated with [14C]PF-00734200 assessed as total radio activity at 5 mg/kg, po administered as single dose by LC-MS/MS method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID1220319 | Total drug level in beagle dog treated with [14C]PF-00734200 assessed as total radio activity at 5 mg/kg, po administered as single dose by LC-MS/MS method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID351532 | Inhibition of CYP2C9 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351503 | Half life in Sprague-Dawley rat at 1 mg/kg, iv and 5 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351500 | Metabolic stability in human hepatocytes assessed as intrinsic clearance | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351511 | AUC in cynomolgus monkey at 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID1220322 | Total drug level in human treated with [14C]PF-00734200 assessed as total radio activity at 20 mg/kg, po administered as single dose by LC-MS/MS method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID351495 | Inhibition of human recombinant DPP4 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID1220308 | AUC (0 to 168 hrs) in human treated with [14C]PF-00734200 at 20 mg/kg, po administered as single dose | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID351525 | Inhibition of POP | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351531 | Inhibition of CYP1A2 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351504 | Bioavailability in Sprague-Dawley rat at 1 mg/kg, iv and 5 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID1220314 | Cmax in human treated with [14C]PF-00734200 at 20 mg/kg, po administered as single dose | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| AID351514 | Volume of distribution at steady state in dog at 1 mg/kg, iv and 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351494 | Inhibition of human recombinant DPP8 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351492 | Apparent permeability from basolateral to apical side in MDCK cells | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID351530 | Selectivity ratio of IC50 for POP to IC50 for human plasma DPP4 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
| AID1220325 | Drug level in human serum treated with [14C]PF-00734200 at 20 mg/kg, po administered as single dose by LC-MS/MS method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11
| Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |