Page last updated: 2024-12-11
talabostat
Description
Research Excerpts
Clinical Trials
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Study Profile
Bioassays
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Description
talabostat: an antineoplastic agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 6918572 |
| CHEMBL ID | 67279 |
| SCHEMBL ID | 393024 |
| MeSH ID | M0502720 |
Synonyms (46)
| Synonym |
|---|
| ketopyrrolidine derivative |
| (r)-1-((s)-2-amino-3-methylbutanoyl)pyrrolidin-2-ylboronic acid |
| bdbm50050513 |
| (s)-2-amino-1-((r)-2-dihydroxyboron-pyrrolidin-1-yl)-3-methyl-butan-1-one |
| (s)-2-amino-3-methyl-2-boronic acid-1-pyrrolidin-1-yl-butan-1-one |
| pyrrolidine derivative |
| talabostat |
| valboropro |
| 149682-77-9 |
| D05989 |
| talabostat (usan/inn) |
| valinyl-l-boroproline |
| CHEMBL67279 , |
| [(2r)-1-[(2s)-2-amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid |
| val-boro-pro |
| boronic acid, (1-(2-amino-3-methyl-1-oxobutyl)-2-pyrrolidinyl)-, (r-(r*,s*))- |
| valinyl-boroproline |
| pt100 cpd |
| pt 100 |
| kz1o2sh88z , |
| boronic acid, ((2r)-1-((2s)-2-amino-3-methyl-1-oxobutyl)-2-pyrrolidinyl)- |
| ((2r)-1-((2s)-2-amino-3-methylbutanoyl)pyrrolidin-2-yl)boronic acid |
| unii-kz1o2sh88z |
| talabostat [usan:inn] |
| talabostat [usan] |
| boronic acid, ((2r)-1-((2s)-2-amino-3-methyl-1-oxobutyl)-2-pyrrolidinyl) |
| talabostat [inn] |
| AKOS022185199 |
| SCHEMBL393024 |
| ((r)-1-((s)-2-amino-3-methylbutanoyl)pyrrolidin-2-yl)boronic acid |
| HY-13233 |
| CS-6996 |
| gtpl9892 |
| compound 1 [pmid: 18783201] |
| ((r)-1-(l-valyl)pyrrolidin-2-yl)boronic acid |
| DB06182 |
| val-boropro;pt100 |
| AMY22689 |
| EX-A3155 |
| Q27282515 |
| nsc-762155 |
| nsc762155 |
| ((r)-1-((s)-2-amino-3-methylbutanoyl)pyrrolidin-2-yl)boronicacid |
| nsc840949 |
| nsc-840949 |
| DTXSID70869984 |
Research Excerpts
Overview
Talabostat mesilate is an orally active, specific inhibitor of dipeptidyl peptidases, including tumor-associated fibroblast activation protein.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Talabostat is a novel dipeptidyl peptidase inhibitor with immunostimulatory properties." | ( Phase II assessment of talabostat and cisplatin in second-line stage IV melanoma. Anthony, SP; Cunningham, CC; Eager, RM; Frenette, G; Jones, B; Nemunaitis, J; O'Day, SJ; Pavlick, AC; Senzer, NN; Stephenson, J; Uprichard, M, 2009) | 1.38 |
| "Talabostat mesilate is an orally active, specific inhibitor of dipeptidyl peptidases, including tumor-associated fibroblast activation protein. " | ( Talabostat. Cunningham, CC, 2007) | 3.23 |
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| " The adverse effects induced by boronic acid-based DPP-IV inhibitors are essentially limited to what has been observed previously for non-boronic acid inhibitors and attributed to cross-reactivity with DPP8/9." | ( Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. Bachovchin, WW; Chiluwal, AK; Connolly, BA; Dimare, MT; Healey, SE; Jin, Z; Lai, JH; Li, Y; Liu, Y; Maw, H; Peters, DE; Sanford, DG; Sudmeier, JL; Wu, W; Zhou, Y, 2008) | 0.35 |
Pharmacokinetics
| Excerpt | Reference | Relevance |
|---|---|---|
| " Pharmacokinetic evaluation in mice of selected inhibitors demonstrated high oral bioavailability, plasma half-life, and the potential to selectively and completely inhibit FAP in vivo." | ( Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). Augustyns, K; Cheng, JD; Cos, P; De Meester, I; Heirbaut, L; Jansen, K; Joossens, J; Lambeir, AM; Maes, L; Van der Veken, P; Verkerk, R, 2014) | 0.4 |
Compound-Compound Interactions
| Excerpt | Reference | Relevance |
|---|---|---|
| " Immunogenicity of electroporated DNA (HIV env) and recombinant gp120, administered with either QS-21 or the orally administered immunomodulator, Talabostat, was evaluated in BALB/c mice." | ( HIV-1 Env vaccine comprised of electroporated DNA and protein co-administered with Talabostat. Aziz, N; Cristillo, AD; Draghia-Akli, R; Galmin, L; Hudacik, L; Lewis, B; Markham, P; Pal, R; Restrepo, S; Suschak, J; Weiss, D, 2008) | 0.77 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| "9%NaCl) was dosed per os twice daily from day 1-14." | ( Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Beckmann, N; Cannet, C; Egger, C; Gérard, C; Jarman, E; Ksiazek, I; Suply, T, 2017) | 0.46 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (11)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Kynurenine 3-monooxygenase | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0660 | 0.0220 | 1.3749 | 8.0000 | AID659183 |
| Prothrombin | Homo sapiens (human) | Ki | 0.0020 | 0.0000 | 0.7846 | 9.0000 | AID238304 |
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.9800 | 0.0004 | 0.9086 | 10.0000 | AID1129903 |
| Glutamate receptor ionotropic, kainate 1 | Rattus norvegicus (Norway rat) | Ki | 0.1250 | 0.0007 | 1.7175 | 8.1800 | AID57546 |
| Dipeptidyl peptidase 4 | Homo sapiens (human) | IC50 (µMol) | 0.1666 | 0.0001 | 0.4444 | 10.0000 | AID1539749; AID1709023; AID1896135; AID287008; AID287009; AID305097; AID56232; AID592141; AID592142; AID659183; AID736688 |
| Dipeptidyl peptidase 4 | Homo sapiens (human) | Ki | 0.2866 | 0.0000 | 0.3414 | 2.2000 | AID1850425; AID238304; AID287007; AID390968; AID56048; AID56218 |
| Prolyl endopeptidase | Homo sapiens (human) | IC50 (µMol) | 4.4916 | 0.0011 | 1.9896 | 9.7500 | AID1129903; AID1539747; AID160222; AID1709024; AID305102; AID659184; AID736684; AID748310 |
| Prolyl endopeptidase FAP | Mus musculus (house mouse) | IC50 (µMol) | 0.0673 | 0.0660 | 0.1884 | 0.3700 | AID1129901; AID659183; AID748314 |
| Prolyl endopeptidase FAP | Homo sapiens (human) | IC50 (µMol) | 0.0792 | 0.0120 | 1.1589 | 5.8300 | AID1539748; AID1663821; AID1709022; AID305099; AID736685 |
| Prolyl endopeptidase FAP | Homo sapiens (human) | Ki | 0.0355 | 0.0050 | 0.0355 | 0.0660 | AID1850424; AID1896134 |
| Dipeptidyl peptidase 8 | Homo sapiens (human) | IC50 (µMol) | 0.0113 | 0.0019 | 2.6532 | 10.0000 | AID305100; AID736687 |
| Dipeptidyl peptidase 8 | Homo sapiens (human) | Ki | 0.0015 | 0.0015 | 0.4624 | 1.3420 | AID390967 |
| Dipeptidyl peptidase 9 | Homo sapiens (human) | IC50 (µMol) | 2.2681 | 0.0001 | 1.4207 | 10.0000 | AID305101; AID390975; AID736686 |
| Dipeptidyl peptidase 9 | Homo sapiens (human) | Ki | 0.0008 | 0.0005 | 0.2062 | 1.3420 | AID390966 |
| Dipeptidyl peptidase 2 | Homo sapiens (human) | IC50 (µMol) | 0.0437 | 0.0002 | 0.9316 | 6.6000 | AID1709025; AID305098; AID56223 |
| Dipeptidyl peptidase 2 | Homo sapiens (human) | Ki | 41.7500 | 0.0001 | 0.0938 | 0.1250 | AID238649; AID56222; AID57546 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (66)
Molecular Functions (21)
Ceullar Components (32)
Bioassays (90)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID160222 | Compound was tested in vitro for inhibition of Prolyl endopeptidase | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10 | Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides. |
| AID1539747 | Inhibition of POP (unknown origin) | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | Integrated Synthetic, Biophysical, and Computational Investigations of Covalent Inhibitors of Prolyl Oligopeptidase and Fibroblast Activation Protein α. |
| AID1709024 | Inhibition of PREP (unknown origin) using AMC substrate by fluorometric assay | 2021 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 37 | Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor. |
| AID736686 | Inhibition of human DPP9 using H-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase. |
| AID305099 | Inhibition of human FAP | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2 | Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor. |
| AID56223 | Compound was tested in vitro for inhibition of Dipeptidylpeptidase II | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10 | Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides. |
| AID748313 | Inhibition of DPP4 in human seminal plasma using Gly-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold. |
| AID56218 | Inhibitory activity of compound against Dipeptidylpeptidase IV (DPP IV) | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23 | Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases. |
| AID390984 | Inhibition of human recombinant DPP9 expressed in HEK293T cells relative to Ala-boroPro | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID736682 | Selectivity ratio of IC50 for human FAP to IC50 for human PREP | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase. |
| AID56232 | In vitro for inhibition of Dipeptidylpeptidase IV. | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10 | Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides. |
| AID659185 | 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 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity. |
| AID390983 | Inhibition of human placental DPP4 after 2 hrs relative to Ala-boroPro | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID736675 | Cytotoxicity against human HEK293 cells expressing murine FAP at 0.0001 uM to 100 uM after 48 hrs by CellTiter-Blue assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase. |
| AID56222 | Inhibitory activity of compound against Dipeptidylpeptidase II (DPP II) | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23 | Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases. |
| AID592150 | Antidiabetic activity in po dosed C57BL/KS01HSDLeprdb mouse assessed as decrease in serum glucose AUC level by oral glucose tolerance test | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Pro-soft Val-boroPro: a strategy for enhancing in vivo performance of boronic acid inhibitors of serine proteases. |
| AID57546 | Inhibition of Dipeptidyl Peptidase II (Quiescent cell proline peptidase) | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20 | Development of potent and selective dipeptidyl peptidase II inhibitors. |
| AID305117 | Inhibition of DPP2 expressed in Jurkat cells assessed as remaining Ala-Pro-AFC substrate cleavage activity at 10 uM | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2 | Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor. |
| AID390967 | Inhibition of human recombinant DPP8 expressed in HEK293T cells | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID390981 | Inhibition of human recombinant DPP9 expressed in intact HEK293T cells assessed as residual enzyme activity at 10 uM | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID592152 | Toxicity in po dosed Fisher rat assessed as mortality measured up to 24 hrs | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Pro-soft Val-boroPro: a strategy for enhancing in vivo performance of boronic acid inhibitors of serine proteases. |
| AID305101 | Inhibition of human DPP9 | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2 | Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor. |
| AID240875 | Inhibitory concentration against dipeptidyl peptidase IV | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22 | Ketopyrrolidines and ketoazetidines as potent dipeptidyl peptidase IV (DPP IV) inhibitors. |
| AID390966 | Inhibition of human recombinant DPP9 expressed in HEK293T cells | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID1709022 | Inhibition of FAP (unknown origin) using AMC substrate by fluorometric assay | 2021 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 37 | Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor. |
| AID659183 | 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 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity. |
| AID659186 | 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 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity. |
| AID390975 | Inhibition of human recombinant DPP9 expressed in intact HEK293T cells after 2 hrs | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID1129904 | Inhibition of DPP9 purified from bovine testes using Ala-Pro-p-nitroanilide as substrate by spectrophotometry | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). |
| AID390969 | Selectivity ratio of Ki for human recombinant DPP8 to Ki for human placental DPP4 | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID390978 | Reduction of glucose level in po dosed C57BL/6 mouse assessed as drug level causing maximal reduction of glucose AUC by oral glucose tolerance test | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID1129901 | Inhibition of recombinant mouse FAP purified from HEK293 cell supernatant using Ala-Pro-p-nitroanilide as substrate by spectrophotometry | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). |
| AID1129905 | Inhibition of DPP2 purified from human seminal plasma using Lys-Ala-p-nitroanilide as substrate by spectrophotometry | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). |
| AID1896136 | Selectivity ratio of Ki for POP (unknown origin) to Ki for 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. |
| AID390986 | Therapeutic index, ratio of MTD to drug level causing maximal reduction of glucose AUC in po dosed Sprague-Dawley rat | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID305125 | Effect on cell death in resting PBMCs assessed as reduction of annexin V positive cells in presence of 100 uM Zvad-fmk | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2 | Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor. |
| AID659184 | Inhibition of human recombinant PREP expressed in Escherichia coli assessed as pNA release from Z-Gly-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity. |
| AID305098 | Inhibition of human DPP2 | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2 | Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor. |
| AID748311 | Inhibition of DPP2 in human seminal plasma using Lys-Ala-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold. |
| AID390971 | Reduction of glucose level in po dosed C57BL/6 mouse by oral glucose tolerance test | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID659187 | 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 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity. |
| AID748312 | Inhibition of DPP9 in bovine testis using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold. |
| AID1850425 | Binding affinity to DPP-4 (unknown origin) assessed as inhibition constant | 2022 | Bioorganic & medicinal chemistry, 06-01, Volume: 63 | Boron-Containing heterocycles as promising pharmacological agents. |
| AID390977 | Inhibition of human recombinant DPP9 expressed in intact HEK293T cells assessed as residual enzyme activity at 1 mM | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID736688 | Inhibition of human DPP4 using H-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase. |
| AID736687 | Inhibition of human DPP8 using H-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase. |
| AID1850424 | Binding affinity to FAP (unknown origin) assessed as inhibition constant | 2022 | Bioorganic & medicinal chemistry, 06-01, Volume: 63 | Boron-Containing heterocycles as promising pharmacological agents. |
| 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. |
| AID287010 | Ratio of IC50 for human placental DPP4 at pH 2 to IC50 for human placental DPP4 at pH 8 | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Synthesis and characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines. |
| AID1539749 | Inhibition of DPP4 (unknown origin) | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | Integrated Synthetic, Biophysical, and Computational Investigations of Covalent Inhibitors of Prolyl Oligopeptidase and Fibroblast Activation Protein α. |
| AID748314 | Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold. |
| AID1663821 | Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | A cell-based fluorescent assay for FAP inhibitor discovery. |
| AID1709025 | Inhibition of DPP2 (unknown origin) using AMC substrate by fluorometric assay | 2021 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 37 | Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor. |
| AID390982 | Inhibition of human recombinant DPP9 expressed in intact HEK293T cells assessed as residual enzyme activity at 1 uM | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID287008 | Inhibition of human placental DPP4 at pH 2 | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Synthesis and characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines. |
| AID592141 | Inhibition of DDP4 at pH 2 preincubated for 10 mins | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Pro-soft Val-boroPro: a strategy for enhancing in vivo performance of boronic acid inhibitors of serine proteases. |
| AID287009 | Inhibition of human placental DPP4 at pH 8 | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Synthesis and characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines. |
| AID736685 | Inhibition of human FAP using Z-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase. |
| AID305102 | Inhibition of prolyl oligopeptidase | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2 | Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor. |
| AID390980 | Inhibition of human recombinant DPP9 expressed in intact HEK293T cells assessed as residual enzyme activity at 100 uM | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID1539748 | Inhibition of FAP (unknown origin) | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | Integrated Synthetic, Biophysical, and Computational Investigations of Covalent Inhibitors of Prolyl Oligopeptidase and Fibroblast Activation Protein α. |
| AID235490 | Selectivity for Dipeptidylpeptidase IV over Dipeptidylpeptidase II. | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20 | Development of potent and selective dipeptidyl peptidase II inhibitors. |
| AID238649 | Inhibition of quiescent cell proline dipeptidase (QPP) | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17 | Dipeptidyl peptidase IV inhibitors for the treatment of diabetes. |
| AID390979 | Toxicity in po dosed Sprague-Dawley rat assessed as maximum tolerated dose | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID390968 | Inhibition of human placental DPP4 | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID390970 | Selectivity ratio of Ki for human recombinant DPP9 to Ki for human placental DPP4 | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID56229 | Selectivity index of compound was determined as value for DPP IV divided by value for DPP II | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23 | Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases. |
| AID390976 | Inhibition of human recombinant DPP9 expressed in intact HEK293T cells after 2 hrs relative to Val-boroPro | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID305110 | Inhibition of DPP expressed in HEK 293T cells assessed as remaining Ala-Pro-AFC substrate cleavage activity at 10 uM | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2 | Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor. |
| AID1129906 | Selectivity index, ratio of IC50 for recombinant human PREP purified from Escherichia coli to IC50 for recombinant mouse FAP purified from HEK293 cell supernatant | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). |
| AID592151 | Antidiabetic activity in C57BL/KS01HSDLeprdb mouse assessed as decrease in serum glucose AUC level at 0.5 mg/kg, po by oral glucose tolerance test | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Pro-soft Val-boroPro: a strategy for enhancing in vivo performance of boronic acid inhibitors of serine proteases. |
| AID1129903 | Inhibition of recombinant human PREP purified from Escherichia coli using Z-Gly-Pro-p-nitroanilide as substrate by spectrophotometry | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). |
| AID1129902 | Inhibition of DPP4 purified from human seminal plasma using Gly-Pro-p-nitroanilide as substrate by spectrophotometry | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). |
| AID238304 | Binding affinity for dipeptidylpeptidase IV | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17 | Dipeptidyl peptidase IV inhibitors for the treatment of diabetes. |
| AID390973 | Inhibition of DPP4 in po dosed Sprague-Dawley rat plasma after 24 hrs | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID736684 | Inhibition of human PREP using Z-Gly-Pro-AMC as substrate preincubated for 10 mins prior to substrate addition by fluorescence assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9 | Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase. |
| AID592142 | Inhibition of DDP4 at pH 7.4 preincubated for 10 mins | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7 | Pro-soft Val-boroPro: a strategy for enhancing in vivo performance of boronic acid inhibitors of serine proteases. |
| AID390985 | Toxicity in po dosed Sprague-Dawley rat assessed as maximum tolerated dose relative to Val-boroPro | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID748310 | Inhibition of human recombinant PREP expressed in Escherichia coli using Z-Gly-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5 | Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold. |
| AID305100 | Inhibition of human DPP8 | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2 | Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor. |
| AID1709023 | Inhibition of DPP4 (unknown origin) using AMC substrate by fluorometric assay | 2021 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 37 | Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor. |
| AID305124 | Effect on cell death in resting PBMCs at 10 uM | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2 | Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor. |
| 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. |
| 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. |
| AID305103 | Inhibition of DPP2 expressed in HEK 293T cells assessed as remaining Ala-Pro-AFC substrate cleavage activity at 10 uM | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2 | Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor. |
| AID287007 | Inhibition of human placental DPP4 | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Synthesis and characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines. |
| AID305097 | Inhibition of human DPP4 | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2 | Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor. |
| AID56048 | Inhibition of Dipeptidyl Peptidase IV | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20 | Development of potent and selective dipeptidyl peptidase II inhibitors. |
| AID1345889 | Human dipeptidyl peptidase 9 (S9: Prolyl oligopeptidase) | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| AID1345443 | Human dipeptidyl peptidase 4 (S9: Prolyl oligopeptidase) | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (33)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (3.03) | 18.2507 |
| 2000's | 14 (42.42) | 29.6817 |
| 2010's | 12 (36.36) | 24.3611 |
| 2020's | 6 (18.18) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 33.57
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (33.57) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 4 (12.12%) | 5.53% |
| Reviews | 4 (12.12%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 25 (75.76%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||