Assay Detail
Binding
CHEMBL3096167
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 6xHis-tagged recombinant FAP (unknown origin) expressed in baculovirus expression system assessed as hydrolysis of Nle-Pro-aminomethylcoumarin after 20 mins by fluorometric assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 5.90 | 7.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3093903 | — | — | 1 | 7.09 |
| CHEMBL3093905 | — | — | 1 | 6.85 |
| CHEMBL3093910 | — | — | 1 | 6.85 |
| CHEMBL3093913 | — | — | 1 | 6.82 |
| CHEMBL3091488 | — | — | 1 | 6.66 |
| CHEMBL3093914 | — | — | 1 | 6.46 |
| CHEMBL3093904 | — | — | 1 | 6.33 |
| CHEMBL3093907 | — | — | 1 | 6.33 |
| CHEMBL3093908 | — | — | 1 | 6.21 |
| CHEMBL3093923 | — | — | 1 | 6.10 |
| CHEMBL3093915 | — | — | 1 | 6.05 |
| CHEMBL200347 | — | — | 1 | 5.85 |
| CHEMBL3093919 | — | — | 1 | 5.84 |
| CHEMBL3093902 | — | — | 1 | 5.82 |
| CHEMBL3093918 | — | — | 1 | 5.80 |
| CHEMBL3093900 | — | — | 1 | 5.80 |
| CHEMBL3093909 | — | — | 1 | 5.77 |
| CHEMBL3093920 | — | — | 1 | 5.67 |
| CHEMBL3093916 | — | — | 1 | 5.65 |
| CHEMBL3093899 | — | — | 1 | 5.58 |
| CHEMBL3093896 | — | — | 1 | 5.57 |
| CHEMBL3093925 | — | — | 1 | 5.52 |
| CHEMBL3093906 | — | — | 1 | 5.44 |
| CHEMBL142703 | VILDAGLIPTIN | 4.0 | 1 | 5.43 |
| CHEMBL3093911 | — | — | 1 | 5.41 |
| CHEMBL3093897 | — | — | 1 | 5.24 |
| CHEMBL3093912 | — | — | 1 | 5.21 |
| CHEMBL3093924 | — | — | 1 | 5.10 |
| CHEMBL3093898 | — | — | 1 | 4.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3093903 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3093905 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3093910 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3093913 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3091488 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3093914 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3093904 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3093907 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3093908 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL3093923 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3093915 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL200347 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL3093919 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL3093902 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL3093918 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL3093900 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL3093909 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3093920 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL3093916 | — | IC50 | = | 2220.0 | nM | 5.65 |
| CHEMBL3093899 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3093896 | — | IC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL3093925 | — | IC50 | = | 3010.0 | nM | 5.52 |
| CHEMBL3093906 | — | IC50 | = | 3650.0 | nM | 5.44 |
| CHEMBL142703 | VILDAGLIPTIN | IC50 | = | 3720.0 | nM | 5.43 |
| CHEMBL3093911 | — | IC50 | = | 3910.0 | nM | 5.41 |
| CHEMBL3093897 | — | IC50 | = | 5810.0 | nM | 5.24 |
| CHEMBL3093912 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL3093924 | — | IC50 | = | 7870.0 | nM | 5.10 |
| CHEMBL3093898 | — | IC50 | = | 27630.0 | nM | 4.56 |