Assay Detail
Binding
CHEMBL915600
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Inhibition of DPP4 in rat plasma by fluorescence assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Lead optimization of [(S)-gamma-(arylamino)prolyl]thiazolidine focused on gamma-substituent: Indoline compounds as potent DPP-IV inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.53 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL389848 | — | — | 1 | 8.30 |
| CHEMBL388111 | — | — | 1 | 8.21 |
| CHEMBL228021 | — | — | 1 | 8.03 |
| CHEMBL223914 | — | — | 1 | 8.00 |
| CHEMBL225493 | — | — | 1 | 7.99 |
| CHEMBL223916 | — | — | 1 | 7.97 |
| CHEMBL227800 | — | — | 1 | 7.90 |
| CHEMBL227737 | — | — | 1 | 7.87 |
| CHEMBL390512 | — | — | 1 | 7.87 |
| CHEMBL389624 | — | — | 1 | 7.82 |
| CHEMBL227482 | — | — | 1 | 7.79 |
| CHEMBL228243 | — | — | 1 | 7.78 |
| CHEMBL389244 | — | — | 1 | 7.71 |
| CHEMBL224346 | — | — | 1 | 7.68 |
| CHEMBL226771 | — | — | 1 | 7.64 |
| CHEMBL374688 | — | — | 1 | 7.47 |
| CHEMBL441559 | — | — | 1 | 7.47 |
| CHEMBL223497 | — | — | 1 | 7.46 |
| CHEMBL227615 | — | — | 1 | 7.41 |
| CHEMBL411561 | — | — | 1 | 7.26 |
| CHEMBL223915 | — | — | 1 | 7.26 |
| CHEMBL227418 | — | — | 1 | 7.12 |
| CHEMBL223865 | — | — | 1 | 7.00 |
| CHEMBL376562 | — | — | 1 | 6.82 |
| CHEMBL228032 | — | — | 1 | 6.78 |
| CHEMBL223060 | — | — | 1 | 6.77 |
| CHEMBL223114 | — | — | 1 | 6.72 |
| CHEMBL376587 | — | — | 1 | 6.63 |
| CHEMBL387666 | — | — | 1 | - |
| CHEMBL227867 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL389848 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL388111 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL228021 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL223914 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL225493 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL223916 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL227800 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL227737 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL390512 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL389624 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL227482 | — | IC50 | = | 16.3 | nM | 7.79 |
| CHEMBL228243 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL389244 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL224346 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL226771 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL441559 | — | IC50 | = | 34.1 | nM | 7.47 |
| CHEMBL374688 | — | IC50 | = | 33.6 | nM | 7.47 |
| CHEMBL223497 | — | IC50 | = | 34.3 | nM | 7.46 |
| CHEMBL227615 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL411561 | — | IC50 | = | 54.9 | nM | 7.26 |
| CHEMBL223915 | — | IC50 | = | 55.1 | nM | 7.26 |
| CHEMBL227418 | — | IC50 | = | 76.2 | nM | 7.12 |
| CHEMBL223865 | — | IC50 | = | 99.8 | nM | 7.00 |
| CHEMBL376562 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL228032 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL223060 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL223114 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL376587 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL387666 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL227867 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL389906 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL224421 | — | IC50 | > | 300.0 | nM | - |