Assay Detail
Binding
CHEMBL1821018
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of DPP4 in human plasma assessed as formation of 7-amino-4-methylcoumarin from glycyl-L-proline 4-methylcoumaryl-7-amide by fluorescence assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.79 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1819089 | — | — | 1 | 9.47 |
| CHEMBL142703 | VILDAGLIPTIN | 4.0 | 1 | 9.24 |
| CHEMBL376359 | ALOGLIPTIN | 4.0 | 1 | 9.00 |
| CHEMBL1819090 | — | — | 1 | 8.96 |
| CHEMBL1422 | SITAGLIPTIN | 4.0 | 1 | 8.46 |
| CHEMBL1819091 | — | — | 1 | 7.58 |
| CHEMBL1819092 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1819089 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL142703 | VILDAGLIPTIN | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL376359 | ALOGLIPTIN | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1819090 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1422 | SITAGLIPTIN | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL1819091 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1819092 | — | IC50 | > | 1000.0 | nM | - |