An EC 3.4.14.* (dipeptidyl- and tripeptidyl-peptidases) inhibitor that specifically inhibits dipeptidyl peptidase-4 (EC 3.4.14.5).
| Member | Definition | Class |
|---|
| alogliptin | A piperidine that is 3-methyl-2,4-dioxo-3,4-dihydropyrimidine carrying additional 2-cyanobenzyl and 3-aminopiperidin-1-yl groups at positions 1 and 2 respectively (the R-enantiomer). Used in the form of its benzoate salt for treatment of type 2 diabetes. | alogliptin |
| berberine | | berberine |
| bms 477118 | A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2S)-amino(3-hydroxyadamantan-1-yl)acetic acid with the amino group of (1S,3S,5S)-2-azabicyclo[3.1.0]hexane-3-carbonitrile. Used in its monohydrate form for the treatment of Type II diabetes. | saxagliptin |
| linagliptin | A xanthine that is 7H-xanthine bearing (4-methylquinazolin-2-yl)methyl, methyl, but-2-yn-1-yl and 3-aminopiperidin-1-yl substituents at positions 1, 3, 7 and 8 respectively (the R-enantiomer). Used for treatment of type II diabetes. | linagliptin |
| sitagliptin | A triazolopyrazine that exhibits hypoglycemic activity. | sitagliptin |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| Acetylcholinesterase | Electrophorus electricus (electric eel) | IC50 | 0.7827 | 3 | 3 |
| Acetylcholinesterase | Homo sapiens (human) | IC50 | 0.4000 | 2 | 2 |
| Aldo-keto reductase family 1 member C2 | Homo sapiens (human) | IC50 | 6.7100 | 1 | 1 |
| Aldo-keto reductase family 1 member C3 | Homo sapiens (human) | IC50 | 4.9900 | 2 | 2 |
| Aminopeptidase N | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Angiotensin-converting enzyme | Homo sapiens (human) | IC50 | 11.0000 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 138.5000 | 3 | 3 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Carbonic anhydrase 1 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| Carbonic anhydrase 2 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| Carbonic anhydrase 4 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| Carbonic anhydrase 5A, mitochondrial | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| Carbonic anhydrase 5B, mitochondrial | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| Carbonic anhydrase 9 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| Catechol O-methyltransferase | Homo sapiens (human) | IC50 | 147.1000 | 1 | 1 |
| Catechol O-methyltransferase | Rattus norvegicus (Norway rat) | IC50 | 147.1000 | 1 | 1 |
| Chain A, Dipeptidyl peptidase IV | Homo sapiens (human) | IC50 | 0.0180 | 1 | 1 |
| Cholinesterase | Equus caballus (horse) | IC50 | 15.2667 | 3 | 3 |
| Cholinesterase | Homo sapiens (human) | IC50 | 15.8950 | 2 | 2 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 | 5.1500 | 2 | 2 |
| Cytochrome P450 1B1 | Homo sapiens (human) | IC50 | 0.9747 | 3 | 3 |
| Cytochrome P450 1B1 | Homo sapiens (human) | Ki | 0.0440 | 1 | 1 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 | 70.0000 | 2 | 3 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 68.0000 | 4 | 5 |
| Dipeptidyl peptidase 2 | Homo sapiens (human) | IC50 | 93.3225 | 19 | 30 |
| Dipeptidyl peptidase 4 | Homo sapiens (human) | IC50 | 5.0957 | 79 | 100 |
| Dipeptidyl peptidase 4 | Mus musculus (house mouse) | IC50 | 50.0230 | 2 | 2 |
| Dipeptidyl peptidase 4 | Rattus norvegicus (Norway rat) | IC50 | 0.0255 | 2 | 2 |
| Dipeptidyl peptidase 4 | Homo sapiens (human) | Ki | 0.0006 | 6 | 6 |
| Dipeptidyl peptidase 8 | Homo sapiens (human) | IC50 | 50.7538 | 33 | 47 |
| Dipeptidyl peptidase 8 | Homo sapiens (human) | Ki | 0.1300 | 1 | 1 |
| Dipeptidyl peptidase 9 | Bos taurus (cattle) | IC50 | 100.0000 | 1 | 2 |
| Dipeptidyl peptidase 9 | Homo sapiens (human) | IC50 | 71.8866 | 26 | 35 |
| Dipeptidyl peptidase 9 | Homo sapiens (human) | Ki | 0.0710 | 1 | 1 |
| Dipeptidyl peptidase IV | Porphyromonas gingivalis | IC50 | 14.0000 | 1 | 2 |
| Kynurenine 3-monooxygenase | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| Lysine-specific histone demethylase 1A | Homo sapiens (human) | IC50 | 6.9700 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | IC50 | 0.2967 | 3 | 3 |
| Neprilysin | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Neuraminidase | Influenza A virus (A/USSR/90/1977(H1N1)) | IC50 | 35.3500 | 2 | 2 |
| Neuraminidase | Influenza A virus (A/Puerto Rico/8/1934(H1N1)) | Ki | 14.3000 | 1 | 1 |
| Potassium voltage-gated channel subfamily D member 3 | Homo sapiens (human) | IC50 | 100,000.0000 | 1 | 1 |
| Potassium voltage-gated channel subfamily E member 1 | Homo sapiens (human) | IC50 | 316.2280 | 1 | 1 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 351.1491 | 5 | 5 |
| Potassium voltage-gated channel subfamily KQT member 1 | Homo sapiens (human) | IC50 | 316.2280 | 1 | 1 |
| POU domain, class 2, transcription factor 1 | Homo sapiens (human) | IC50 | 43.0000 | 2 | 2 |
| POU domain, class 2, transcription factor 2 | Homo sapiens (human) | IC50 | 80.0000 | 1 | 1 |
| Prolyl endopeptidase | Homo sapiens (human) | IC50 | 114.5000 | 6 | 6 |
| Prolyl endopeptidase FAP | Homo sapiens (human) | IC50 | 196.5595 | 13 | 21 |
| Prolyl endopeptidase FAP | Mus musculus (house mouse) | IC50 | 33.5800 | 3 | 3 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 | 16.1400 | 1 | 1 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | IC50 | 16.1400 | 1 | 1 |
| Sodium channel protein type 5 subunit alpha | Homo sapiens (human) | IC50 | 712.6425 | 2 | 2 |
| Solute carrier family 22 member 8 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Solute carrier organic anion transporter family member 1B1 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Telomerase reverse transcriptase | Homo sapiens (human) | IC50 | 37.0000 | 1 | 1 |
| Thromboxane-A synthase | Homo sapiens (human) | IC50 | 0.0194 | 1 | 1 |
| Tyrosine-protein phosphatase non-receptor type 1 | Homo sapiens (human) | IC50 | 67.0000 | 1 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1C | Homo sapiens (human) | IC50 | 50,073.5500 | 2 | 2 |
| Voltage-dependent L-type calcium channel subunit alpha-1C | Rattus norvegicus (Norway rat) | IC50 | 100,000.0000 | 1 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1D | Homo sapiens (human) | IC50 | 147.1000 | 1 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1F | Homo sapiens (human) | IC50 | 147.1000 | 1 | 1 |
| Voltage-dependent L-type calcium channel subunit alpha-1S | Homo sapiens (human) | IC50 | 147.1000 | 1 | 1 |