Assay Detail
Binding
CHEMBL5622975
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Inhibition of human DPP4 using Gly-Pro-NA as substrate incubated for 30 mins by absorbance based assay
21
Total Activities
21
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
SAR and lead optimization of (Z)-5-(4-hydroxy-3-methoxybenzylidene)-3-(2-morpholinoacetyl)thiazolidine-2,4-dione as a potential multi-target antidiabetic agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.17 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1422 | SITAGLIPTIN | 4.0 | 1 | 8.10 |
| CHEMBL5630676 | — | — | 1 | 7.44 |
| CHEMBL5631075 | — | — | 1 | 7.17 |
| CHEMBL5624847 | — | — | 1 | 7.08 |
| CHEMBL5624535 | — | — | 1 | 7.05 |
| CHEMBL5631021 | — | — | 1 | 7.05 |
| CHEMBL5630566 | — | — | 1 | 6.93 |
| CHEMBL5624515 | — | — | 1 | 6.90 |
| CHEMBL5624476 | — | — | 1 | 6.77 |
| CHEMBL5630180 | — | — | 1 | 6.66 |
| CHEMBL5624539 | — | — | 1 | 6.37 |
| CHEMBL5629890 | — | — | 1 | 5.91 |
| CHEMBL5624654 | — | — | 1 | 5.67 |
| CHEMBL5624938 | — | — | 1 | 5.56 |
| CHEMBL5624477 | — | — | 1 | 5.51 |
| CHEMBL5630679 | — | — | 1 | 5.20 |
| CHEMBL5630880 | — | — | 1 | 5.10 |
| CHEMBL5630820 | — | — | 1 | 5.09 |
| CHEMBL5630282 | — | — | 1 | 4.83 |
| CHEMBL5630847 | — | — | 1 | 4.79 |
| CHEMBL5630400 | — | — | 1 | 4.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1422 | SITAGLIPTIN | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5630676 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5631075 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5624847 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL5624535 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5631021 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5630566 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL5624515 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL5624476 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL5630180 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5624539 | — | IC50 | = | 428.0 | nM | 6.37 |
| CHEMBL5629890 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL5624654 | — | IC50 | = | 2130.0 | nM | 5.67 |
| CHEMBL5624938 | — | IC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL5624477 | — | IC50 | = | 3070.0 | nM | 5.51 |
| CHEMBL5630679 | — | IC50 | = | 6270.0 | nM | 5.20 |
| CHEMBL5630880 | — | IC50 | = | 8010.0 | nM | 5.10 |
| CHEMBL5630820 | — | IC50 | = | 8030.0 | nM | 5.09 |
| CHEMBL5630282 | — | IC50 | = | 14940.0 | nM | 4.83 |
| CHEMBL5630847 | — | IC50 | = | 16210.0 | nM | 4.79 |
| CHEMBL5630400 | — | IC50 | = | 34340.0 | nM | 4.46 |