Assay Detail
Binding
CHEMBL901593
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Inhibition of human DPP8
33
Total Activities
25
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.01 | 6.91 |
| Kd | 4 | 5.18 | 6.11 |
| Kinact | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL397070 | — | — | 1 | 6.91 |
| CHEMBL235766 | — | — | 1 | 6.28 |
| CHEMBL440982 | — | — | 3 | 6.28 |
| CHEMBL236781 | — | — | 3 | 6.04 |
| CHEMBL398373 | — | — | 1 | 5.68 |
| CHEMBL392162 | — | — | 1 | 5.11 |
| CHEMBL391721 | — | — | 1 | 5.09 |
| CHEMBL439205 | — | — | 1 | 5.07 |
| CHEMBL238050 | — | — | 3 | 5.04 |
| CHEMBL392163 | — | — | 1 | 4.90 |
| CHEMBL237860 | — | — | 3 | 4.80 |
| CHEMBL399189 | — | — | 1 | 4.60 |
| CHEMBL399402 | — | — | 1 | 4.44 |
| CHEMBL238114 | — | — | 1 | 4.37 |
| CHEMBL437965 | — | — | 1 | 4.32 |
| CHEMBL439382 | — | — | 1 | 4.25 |
| CHEMBL1182947 | — | — | 1 | 4.15 |
| CHEMBL427850 | — | — | 1 | 4.15 |
| CHEMBL392139 | — | — | 1 | 4.07 |
| CHEMBL237672 | — | — | 1 | - |
| CHEMBL391720 | — | — | 1 | - |
| CHEMBL237658 | — | — | 1 | - |
| CHEMBL236586 | — | — | 1 | - |
| CHEMBL237673 | — | — | 1 | - |
| CHEMBL236602 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL397070 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL235766 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL440982 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL440982 | — | Kd | = | 770.0 | nM | 6.11 |
| CHEMBL236781 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL398373 | — | IC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL236781 | — | Kd | = | 7300.0 | nM | 5.14 |
| CHEMBL392162 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL391721 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL439205 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL238050 | — | Kd | = | 9100.0 | nM | 5.04 |
| CHEMBL392163 | — | IC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL237860 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL238050 | — | IC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL399189 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL399402 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL237860 | — | Kd | = | 39000.0 | nM | 4.41 |
| CHEMBL238114 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL437965 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL439382 | — | IC50 | = | 56000.0 | nM | 4.25 |
| CHEMBL427850 | — | IC50 | = | 71000.0 | nM | 4.15 |
| CHEMBL1182947 | — | IC50 | = | 71000.0 | nM | 4.15 |
| CHEMBL392139 | — | IC50 | = | 86000.0 | nM | 4.07 |
| CHEMBL440982 | — | Kinact | = | 0.0029 | /s | - |
| CHEMBL237860 | — | Kinact | = | 0.0017 | /s | - |
| CHEMBL238050 | — | Kinact | = | 0.0013 | /s | - |
| CHEMBL236781 | — | Kinact | = | 0.005 | /s | - |
| CHEMBL236586 | — | IC50 | = | 126000.0 | nM | - |
| CHEMBL237658 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL391720 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL237672 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL237673 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL236602 | — | IC50 | > | 1000000.0 | nM | - |