Assay Detail
Binding
CHEMBL915599
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Inhibition of DPP4 in human plasma by fluorescence assay
39
Total Activities
39
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 | 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 | 39 | 7.70 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL195420 | — | — | 1 | 9.60 |
| CHEMBL77538 | — | — | 1 | 8.85 |
| CHEMBL381626 | — | — | 1 | 8.54 |
| CHEMBL388111 | — | — | 1 | 8.32 |
| CHEMBL223914 | — | — | 1 | 8.24 |
| CHEMBL223916 | — | — | 1 | 8.19 |
| CHEMBL228021 | — | — | 1 | 8.19 |
| CHEMBL192165 | — | — | 1 | 8.18 |
| CHEMBL390512 | — | — | 1 | 8.15 |
| CHEMBL227800 | — | — | 1 | 8.15 |
| CHEMBL225493 | — | — | 1 | 8.10 |
| CHEMBL389848 | — | — | 1 | 8.04 |
| CHEMBL227737 | — | — | 1 | 8.02 |
| CHEMBL389244 | — | — | 1 | 7.96 |
| CHEMBL389624 | — | — | 1 | 7.87 |
| CHEMBL228243 | — | — | 1 | 7.86 |
| CHEMBL227482 | — | — | 1 | 7.78 |
| CHEMBL226771 | — | — | 1 | 7.77 |
| CHEMBL224346 | — | — | 1 | 7.72 |
| CHEMBL374688 | — | — | 1 | 7.60 |
| CHEMBL390513 | — | — | 1 | 7.59 |
| CHEMBL227615 | — | — | 1 | 7.58 |
| CHEMBL223497 | — | — | 1 | 7.47 |
| CHEMBL441559 | — | — | 1 | 7.43 |
| CHEMBL223915 | — | — | 1 | 7.34 |
| CHEMBL411561 | — | — | 1 | 7.29 |
| CHEMBL227418 | — | — | 1 | 7.07 |
| CHEMBL223865 | — | — | 1 | 6.95 |
| CHEMBL223114 | — | — | 1 | 6.83 |
| CHEMBL376562 | — | — | 1 | 6.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL195420 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL77538 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL381626 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL388111 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL223914 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL223916 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL228021 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL192165 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL390512 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL227800 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL225493 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL389848 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL227737 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL389244 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL389624 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL228243 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL227482 | — | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL226771 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL224346 | — | IC50 | = | 19.2 | nM | 7.72 |
| CHEMBL374688 | — | IC50 | = | 25.2 | nM | 7.60 |
| CHEMBL390513 | — | IC50 | = | 25.4 | nM | 7.59 |
| CHEMBL227615 | — | IC50 | = | 26.4 | nM | 7.58 |
| CHEMBL223497 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL441559 | — | IC50 | = | 37.2 | nM | 7.43 |
| CHEMBL223915 | — | IC50 | = | 45.4 | nM | 7.34 |
| CHEMBL411561 | — | IC50 | = | 51.5 | nM | 7.29 |
| CHEMBL227418 | — | IC50 | = | 85.9 | nM | 7.07 |
| CHEMBL223865 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL223114 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL376562 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL223060 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL228032 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL224419 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL224435 | — | IC50 | = | 558.0 | nM | 6.25 |
| CHEMBL224421 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL376587 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL389906 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL227867 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL387666 | — | IC50 | > | 300.0 | nM | - |