Assay Detail
Binding
CHEMBL2406783
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Inhibition of human full length PDE4A4 expressed in baculovirus infected sf21 cells
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
3',5'-cyclic-AMP phosphodiesterase 4A (CHEMBL254) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of triazines as potent, selective and orally active PDE4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 7.78 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2402362 | — | — | 1 | 9.82 |
| CHEMBL2402363 | — | — | 1 | 9.70 |
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 9.46 |
| CHEMBL2402361 | — | — | 1 | 9.38 |
| CHEMBL2402509 | — | — | 1 | 9.09 |
| CHEMBL2402511 | — | — | 1 | 9.05 |
| CHEMBL2402358 | — | — | 1 | 9.00 |
| CHEMBL2402366 | — | — | 1 | 8.96 |
| CHEMBL2402360 | — | — | 1 | 8.85 |
| CHEMBL2402364 | — | — | 1 | 8.80 |
| CHEMBL2402530 | — | — | 1 | 8.77 |
| CHEMBL2402510 | — | — | 1 | 8.62 |
| CHEMBL2402512 | — | — | 1 | 8.57 |
| CHEMBL2402529 | — | — | 1 | 8.44 |
| CHEMBL2402520 | — | — | 1 | 8.36 |
| CHEMBL2402359 | — | — | 1 | 8.31 |
| CHEMBL2402365 | — | — | 1 | 8.19 |
| CHEMBL2402527 | — | — | 1 | 8.18 |
| CHEMBL2402528 | — | — | 1 | 7.92 |
| CHEMBL2402525 | — | — | 1 | 7.75 |
| CHEMBL2402517 | — | — | 1 | 7.72 |
| CHEMBL2402519 | — | — | 1 | 7.72 |
| CHEMBL2402518 | — | — | 1 | 7.42 |
| CHEMBL2402526 | — | — | 1 | 7.42 |
| CHEMBL2402532 | — | — | 1 | 7.40 |
| CHEMBL2402534 | — | — | 1 | 7.36 |
| CHEMBL2402533 | — | — | 1 | 7.27 |
| CHEMBL2402524 | — | — | 1 | 7.25 |
| CHEMBL2402523 | — | — | 1 | 7.23 |
| CHEMBL2402535 | — | — | 1 | 7.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2402362 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL2402363 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL193240 | ROFLUMILAST | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL2402361 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL2402509 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL2402511 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL2402358 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2402366 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2402360 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL2402364 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2402530 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2402510 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2402512 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL2402529 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL2402520 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL2402359 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL2402365 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL2402527 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL2402528 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2402525 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2402517 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2402519 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2402526 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2402518 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2402532 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2402534 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL2402533 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL2402524 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL2402523 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL2402535 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL511115 | CILOMILAST | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL2402531 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL2402542 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL2402514 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL2402536 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL2402522 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL2402541 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL2402540 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2402513 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL2402538 | — | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL1501511 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL2402516 | — | IC50 | = | 563.0 | nM | 6.25 |
| CHEMBL2402515 | — | IC50 | = | 668.0 | nM | 6.17 |
| CHEMBL2402537 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL2402521 | — | IC50 | > | 1000.0 | nM | - |