Assay Detail
Binding
CHEMBL4053403
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human DPP-4 expressed in HEK293 cells using H-Gly-Pro-AMC as substrate measured over 15 mins by fluorescence analysis
17
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase δ (PI3Kδ) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.25 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL393336 | — | — | 2 | 7.66 |
| CHEMBL3425747 | — | — | 2 | 7.56 |
| CHEMBL4063983 | — | — | 2 | 7.56 |
| CHEMBL4085550 | — | — | 2 | 7.50 |
| CHEMBL4062977 | — | — | 1 | 7.36 |
| CHEMBL4071607 | — | — | 1 | 7.30 |
| CHEMBL4090906 | — | — | 1 | 7.22 |
| CHEMBL4066703 | — | — | 1 | 7.16 |
| CHEMBL4077174 | — | — | 1 | 6.91 |
| CHEMBL4093298 | — | — | 1 | 6.86 |
| CHEMBL3425748 | — | — | 1 | 6.84 |
| CHEMBL4098632 | — | — | 1 | 6.82 |
| CHEMBL4077696 | — | — | 1 | 6.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL393336 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL393336 | — | IC50 | = | 21.88 | nM | 7.66 |
| CHEMBL4063983 | — | IC50 | = | 27.54 | nM | 7.56 |
| CHEMBL3425747 | — | IC50 | = | 27.54 | nM | 7.56 |
| CHEMBL4063983 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3425747 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4085550 | — | IC50 | = | 31.8 | nM | 7.50 |
| CHEMBL4085550 | — | IC50 | = | 32.36 | nM | 7.49 |
| CHEMBL4062977 | — | IC50 | = | 43.4 | nM | 7.36 |
| CHEMBL4071607 | — | IC50 | = | 50.2 | nM | 7.30 |
| CHEMBL4090906 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4066703 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4077174 | — | IC50 | = | 123.3 | nM | 6.91 |
| CHEMBL4093298 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL3425748 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL4098632 | — | IC50 | = | 151.7 | nM | 6.82 |
| CHEMBL4077696 | — | IC50 | = | 537.0 | nM | 6.27 |