| Assay ID | Title | Year | Journal | Article |
|---|
| AID709196 | Inhibition of human seminal plasma DPP4 assessed as pNA release from Gly-Pro-p-nitroanilide substrate pre-incubated with enzyme for 15 min prior to substrate addition by fluorescence technique | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| P2-substituted N-acylprolylpyrrolidine inhibitors of prolyl oligopeptidase: biochemical evaluation, binding mode determination, and assessment in a cellular model of synucleinopathy. |
| AID238565 | Inhibitory activity against prolyl oligopeptidase of porcine brain homogenate | 2004 | Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
| A cyclopent-2-enecarbonyl group mimics proline at the P2 position of prolyl oligopeptidase inhibitors. |
| AID241048 | Inhibitory activity against prolyl oligopeptidase of porcine brain homogenate | 2004 | Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
| A cyclopent-2-enecarbonyl group mimics proline at the P2 position of prolyl oligopeptidase inhibitors. |
| AID1611791 | Inhibition of mouse PREP in N2A cells co-transfected with luciferase assessed as reduction in alpha-synuclein dimerization at 10 uM measured after 4 hrs by protein fragment complementation assay relative to control | 2019 | ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12
| Tetrazole as a Replacement of the Electrophilic Group in Characteristic Prolyl Oligopeptidase Inhibitors. |
| AID709198 | Inhibition of pig PREP expressed in Escherichia coli using Z-Gly-Pro-p-nitroanilide substrate | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| P2-substituted N-acylprolylpyrrolidine inhibitors of prolyl oligopeptidase: biochemical evaluation, binding mode determination, and assessment in a cellular model of synucleinopathy. |
| AID1611789 | Inhibition of PREP in C57BL/6 mouse cortex homogenate assessed as formation of 7-amido-4-methylcoumarin using Suc-Gly-Pro-amido-4-methylcoumarin as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorometric as | 2019 | ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12
| Tetrazole as a Replacement of the Electrophilic Group in Characteristic Prolyl Oligopeptidase Inhibitors. |
| AID709194 | Inhibition of bovine testes DPP9 assessed as pNA release from Ala-Pro- p-nitroanilide substrate pre-incubated with enzyme for 15 min prior to substrate addition by fluorescence technique | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| P2-substituted N-acylprolylpyrrolidine inhibitors of prolyl oligopeptidase: biochemical evaluation, binding mode determination, and assessment in a cellular model of synucleinopathy. |
| AID1307738 | Inhibition of human POP expressed in Escherichia coli BL21 pre-incubated for 30 mins before ZGP-pNA substrate addition | 2016 | Journal of medicinal chemistry, 05-12, Volume: 59, Issue:9
| 3-Oxo-hexahydro-1H-isoindole-4-carboxylic Acid as a Drug Chiral Bicyclic Scaffold: Structure-Based Design and Preparation of Conformationally Constrained Covalent and Noncovalent Prolyl Oligopeptidase Inhibitors. |
| AID1611790 | Inhibition of mouse PREP in N2A cells co-transfected with luciferase assessed as remaining alpha-synuclein dimerization at 10 uM measured after 4 hrs by protein fragment complementation assay relative to control | 2019 | ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12
| Tetrazole as a Replacement of the Electrophilic Group in Characteristic Prolyl Oligopeptidase Inhibitors. |
| AID1127417 | Inhibition of prolyl oligopeptidase (unknown origin) | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Synthesis and biological evaluation of novel (123)I-labeled 4-(4-iodophenyl)butanoyl-L-prolyl-(2S)-pyrrolidines for imaging prolyl oligopeptidase in vivo. |
| AID1896135 | Inhibition of DPP4 (unknown origin) | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Modulating the selectivity of inhibitors for prolyl oligopeptidase inhibitors and fibroblast activation protein-α for different indications. |
| AID1307737 | Inhibition of human POP by tight binding based Morrison equation analysis | 2016 | Journal of medicinal chemistry, 05-12, Volume: 59, Issue:9
| 3-Oxo-hexahydro-1H-isoindole-4-carboxylic Acid as a Drug Chiral Bicyclic Scaffold: Structure-Based Design and Preparation of Conformationally Constrained Covalent and Noncovalent Prolyl Oligopeptidase Inhibitors. |
| AID242814 | In vitro inhibitory activity against porcine prolyl oligopeptidase by using 4 mM Suc-Gly-Pro-7-amido-4-methylcoumarin as substrate (pH 7.0) at 30 degree C for 60 min | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
| Dicarboxylic acid azacycle l-prolyl-pyrrolidine amides as prolyl oligopeptidase inhibitors and three-dimensional quantitative structure-activity relationship of the enzyme-inhibitor interactions. |
| AID1896133 | Inhibition of POP (unknown origin) | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Modulating the selectivity of inhibitors for prolyl oligopeptidase inhibitors and fibroblast activation protein-α for different indications. |
| AID709197 | Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| P2-substituted N-acylprolylpyrrolidine inhibitors of prolyl oligopeptidase: biochemical evaluation, binding mode determination, and assessment in a cellular model of synucleinopathy. |
| AID1896134 | Inhibition of FAP (unknown origin) | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Modulating the selectivity of inhibitors for prolyl oligopeptidase inhibitors and fibroblast activation protein-α for different indications. |
| AID1307745 | Inhibition of POP in Han/Wistar rat brain using Suc-Gly-Pro-AMC substrate incubated for 60 mins | 2016 | Journal of medicinal chemistry, 05-12, Volume: 59, Issue:9
| 3-Oxo-hexahydro-1H-isoindole-4-carboxylic Acid as a Drug Chiral Bicyclic Scaffold: Structure-Based Design and Preparation of Conformationally Constrained Covalent and Noncovalent Prolyl Oligopeptidase Inhibitors. |
| AID1766468 | Inhibition of recombinant porcine PREP expressed in Escherichia coli using Suc-Gly-Pro-AMC as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins by multilabel counter analysis | 2021 | ACS medicinal chemistry letters, Oct-14, Volume: 12, Issue:10
| 2-Imidazole as a Substitute for the Electrophilic Group Gives Highly Potent Prolyl Oligopeptidase Inhibitors. |
| AID237428 | Partition coefficient (logP) determined in a 1-octanol-phosphate buffer system | 2004 | Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
| A cyclopent-2-enecarbonyl group mimics proline at the P2 position of prolyl oligopeptidase inhibitors. |
| AID1127418 | Inhibition of porcine prolyl oligopeptidase using Z-Gly-Pro-AMC as substrate after 60 mins by double-reciprocal plot analysis | 2014 | European journal of medicinal chemistry, May-22, Volume: 79 | Synthesis and biological evaluation of novel (123)I-labeled 4-(4-iodophenyl)butanoyl-L-prolyl-(2S)-pyrrolidines for imaging prolyl oligopeptidase in vivo. |
| AID1611788 | Inhibition of recombinant porcine brain PREP expressed in Escherichia coli assessed as formation of 7-amido-4-methylcoumarin using Suc-Gly-Pro-amido-4-methylcoumarin as substrate preincubated for 30 mins followed by substrate addition measured after 60 mi | 2019 | ACS medicinal chemistry letters, Dec-12, Volume: 10, Issue:12
| Tetrazole as a Replacement of the Electrophilic Group in Characteristic Prolyl Oligopeptidase Inhibitors. |
| AID709195 | Inhibition of human seminal plasma DPP2 assessed as pNA release from Lys-Ala-p-nitroanilide substrate pre-incubated with enzyme for 15 min prior to substrate addition by fluorescence technique | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| P2-substituted N-acylprolylpyrrolidine inhibitors of prolyl oligopeptidase: biochemical evaluation, binding mode determination, and assessment in a cellular model of synucleinopathy. |
| AID481393 | Inhibition of pig POP | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
| Inhibitors of prolyl oligopeptidases for the therapy of human diseases: defining diseases and inhibitors. |
| AID1766470 | Inhibition of human PREP expressed in N2A cells assessed as decrease in alpha-synuclein dimerization by measuring decrease in luminescence at 10 uM measured after 4 hrs by protein fragment complementation assay relative to control | 2021 | ACS medicinal chemistry letters, Oct-14, Volume: 12, Issue:10
| 2-Imidazole as a Substitute for the Electrophilic Group Gives Highly Potent Prolyl Oligopeptidase Inhibitors. |
| AID1766471 | Induction of autophagy in human HEK293 cells expressing GFP-LC3B-RFP assessed as decrease in fluorescence at 10 uM after 24 hrs by multilabel counter method | 2021 | ACS medicinal chemistry letters, Oct-14, Volume: 12, Issue:10
| 2-Imidazole as a Substitute for the Electrophilic Group Gives Highly Potent Prolyl Oligopeptidase Inhibitors. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2012 | Biochimie, Jun, Volume: 94, Issue:6
| Molecular dynamics, crystallography and mutagenesis studies on the substrate gating mechanism of prolyl oligopeptidase. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |