Assay Detail
Binding
CHEMBL2060147
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat DPP4 using Gly-Pro-MCA as substrate after 60 mins by fluorometry
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Fused bicyclic heteroarylpiperazine-substituted L-prolylthiazolidines as highly potent DPP-4 inhibitors lacking the electrophilic nitrile group.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 9.03 | 9.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2058975 | — | — | 1 | 9.25 |
| CHEMBL2058971 | — | — | 1 | 9.23 |
| CHEMBL2058762 | — | — | 1 | 9.21 |
| CHEMBL2058972 | — | — | 1 | 9.21 |
| CHEMBL2058758 | — | — | 1 | 9.16 |
| CHEMBL2058756 | — | — | 1 | 9.14 |
| CHEMBL2058757 | — | — | 1 | 9.11 |
| CHEMBL2058974 | — | — | 1 | 9.10 |
| CHEMBL2058973 | — | — | 1 | 9.08 |
| CHEMBL2058969 | — | — | 1 | 9.00 |
| CHEMBL2058761 | — | — | 1 | 8.99 |
| CHEMBL2058760 | — | — | 1 | 8.96 |
| CHEMBL399610 | — | — | 1 | 8.96 |
| CHEMBL2058759 | — | — | 1 | 8.89 |
| CHEMBL2058970 | — | — | 1 | 8.82 |
| CHEMBL2058967 | — | — | 1 | 8.82 |
| CHEMBL2058968 | — | — | 1 | 8.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2058975 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL2058971 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL2058762 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL2058972 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL2058758 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL2058756 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL2058757 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL2058974 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL2058973 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL2058969 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2058761 | — | IC50 | = | 1.03 | nM | 8.99 |
| CHEMBL2058760 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL399610 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2058759 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2058970 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2058967 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2058968 | — | IC50 | = | 3.0 | nM | 8.52 |