Assay Detail
Binding
CHEMBL2149434
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Inhibition of DPP4 in human plasma using Gly-Pro-AMC as substrate by fluorimetric analysis
52
Total Activities
52
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 7.40 | 9.32 |
| Ki | 1 | 8.52 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2147070 | — | — | 1 | 9.32 |
| CHEMBL2147056 | — | — | 1 | 9.26 |
| CHEMBL237500 | LINAGLIPTIN | 4.0 | 1 | 9.00 |
| CHEMBL2147073 | — | — | 1 | 8.80 |
| CHEMBL142703 | VILDAGLIPTIN | 4.0 | 1 | 8.52 |
| CHEMBL385517 | SAXAGLIPTIN ANHYDROUS | 4.0 | 1 | 8.47 |
| CHEMBL2147083 | — | — | 1 | 8.46 |
| CHEMBL2147074 | — | — | 1 | 8.42 |
| CHEMBL376359 | ALOGLIPTIN | 4.0 | 1 | 8.40 |
| CHEMBL2147069 | — | — | 1 | 8.32 |
| CHEMBL2147082 | — | — | 1 | 8.24 |
| CHEMBL2147072 | — | — | 1 | 8.20 |
| CHEMBL2147071 | — | — | 1 | 8.00 |
| CHEMBL2147058 | — | — | 1 | 7.96 |
| CHEMBL2147196 | — | — | 1 | 7.92 |
| CHEMBL2147081 | — | — | 1 | 7.89 |
| CHEMBL2147080 | — | — | 1 | 7.85 |
| CHEMBL2147195 | — | — | 1 | 7.80 |
| CHEMBL2147194 | — | — | 1 | 7.77 |
| CHEMBL2147085 | — | — | 1 | 7.77 |
| CHEMBL1422 | SITAGLIPTIN | 4.0 | 1 | 7.75 |
| CHEMBL2147079 | — | — | 1 | 7.68 |
| CHEMBL2147183 | — | — | 1 | 7.66 |
| CHEMBL2147068 | — | — | 1 | 7.60 |
| CHEMBL2147059 | — | — | 1 | 7.42 |
| CHEMBL2147066 | — | — | 1 | 7.29 |
| CHEMBL2147084 | — | — | 1 | 7.27 |
| CHEMBL2147077 | — | — | 1 | 7.25 |
| CHEMBL2147078 | — | — | 1 | 7.22 |
| CHEMBL2147086 | — | — | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2147070 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL2147056 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL237500 | LINAGLIPTIN | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2147073 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL142703 | VILDAGLIPTIN | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL385517 | SAXAGLIPTIN ANHYDROUS | IC50 | = | 3.37 | nM | 8.47 |
| CHEMBL2147083 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL2147074 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL376359 | ALOGLIPTIN | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2147069 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL2147082 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL2147072 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL2147071 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2147058 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2147196 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2147081 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2147080 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2147195 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2147194 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2147085 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1422 | SITAGLIPTIN | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2147079 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2147183 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2147068 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2147059 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2147066 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2147084 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL2147077 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL2147078 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2147086 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2147193 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2147190 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2147191 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL2147189 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL2147075 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2147067 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2147076 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL2147087 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL2147049 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2147062 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2147060 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2147188 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL2147192 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL2147184 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2147057 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL2147187 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL2147185 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL2147064 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL2147063 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL2147065 | — | IC50 | = | 8900.0 | nM | 5.05 |