Assay Detail
Binding
CHEMBL2060146
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Inhibition of human DPP4 using Gly-Pro-MCA as substrate after 60 mins by fluorometry
18
Total Activities
18
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
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 | 18 | 9.14 | 9.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2058971 | — | — | 1 | 9.43 |
| CHEMBL2058762 | — | — | 1 | 9.41 |
| CHEMBL2058758 | — | — | 1 | 9.38 |
| CHEMBL2058756 | — | — | 1 | 9.30 |
| CHEMBL2058975 | — | — | 1 | 9.29 |
| CHEMBL2058757 | — | — | 1 | 9.26 |
| CHEMBL2058970 | — | — | 1 | 9.25 |
| CHEMBL2058761 | — | — | 1 | 9.23 |
| CHEMBL2058973 | — | — | 1 | 9.21 |
| CHEMBL2058972 | — | — | 1 | 9.21 |
| CHEMBL2058974 | — | — | 1 | 9.14 |
| CHEMBL2058760 | — | — | 1 | 9.10 |
| CHEMBL399610 | — | — | 1 | 9.04 |
| CHEMBL2058969 | — | — | 1 | 9.02 |
| CHEMBL2058967 | — | — | 1 | 8.92 |
| CHEMBL2058759 | — | — | 1 | 8.80 |
| CHEMBL391466 | — | — | 1 | 8.80 |
| CHEMBL2058968 | — | — | 1 | 8.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2058971 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL2058762 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL2058758 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL2058756 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL2058975 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL2058757 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL2058970 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL2058761 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL2058973 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL2058972 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL2058974 | — | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL2058760 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL399610 | — | IC50 | = | 0.92 | nM | 9.04 |
| CHEMBL2058969 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL2058967 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2058759 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL391466 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2058968 | — | IC50 | = | 2.2 | nM | 8.66 |