Assay Detail
Binding
CHEMBL925952
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Inhibition of DPP4 in human Caco-2 cells after 1 hr
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Caco-2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.86 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL257376 | — | — | 1 | 9.00 |
| CHEMBL237500 | LINAGLIPTIN | 4.0 | 1 | 9.00 |
| CHEMBL256121 | — | — | 1 | 9.00 |
| CHEMBL403553 | — | — | 1 | 9.00 |
| CHEMBL403408 | — | — | 1 | 8.70 |
| CHEMBL402819 | — | — | 1 | 8.70 |
| CHEMBL401502 | — | — | 1 | 8.52 |
| CHEMBL257999 | — | — | 1 | 8.52 |
| CHEMBL404220 | — | — | 1 | 8.40 |
| CHEMBL256969 | — | — | 1 | 8.40 |
| CHEMBL401971 | — | — | 1 | 8.30 |
| CHEMBL256521 | — | — | 1 | 8.30 |
| CHEMBL255709 | — | — | 1 | 8.15 |
| CHEMBL401709 | — | — | 1 | 7.89 |
| CHEMBL256729 | — | — | 1 | 7.85 |
| CHEMBL404326 | — | — | 1 | 7.82 |
| CHEMBL255862 | — | — | 1 | 7.72 |
| CHEMBL255492 | — | — | 1 | 7.68 |
| CHEMBL255517 | — | — | 1 | 7.62 |
| CHEMBL256929 | — | — | 1 | 7.60 |
| CHEMBL256928 | — | — | 1 | 7.58 |
| CHEMBL255864 | — | — | 1 | 7.28 |
| CHEMBL255491 | — | — | 1 | 7.05 |
| CHEMBL257795 | — | — | 1 | 7.00 |
| CHEMBL401972 | — | — | 1 | 6.97 |
| CHEMBL402111 | — | — | 1 | 6.25 |
| CHEMBL402573 | — | — | 1 | 6.24 |
| CHEMBL257589 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL257376 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL237500 | LINAGLIPTIN | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL256121 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL403553 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL403408 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL402819 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL401502 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL257999 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL404220 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL256969 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL401971 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL256521 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL255709 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL401709 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL256729 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL404326 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL255862 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL255492 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL255517 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL256929 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL256928 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL255864 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL255491 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL257795 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL401972 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL402111 | — | IC50 | = | 559.0 | nM | 6.25 |
| CHEMBL402573 | — | IC50 | = | 582.0 | nM | 6.24 |
| CHEMBL257589 | — | IC50 | = | 3059.0 | nM | 5.51 |