Assay Detail
Binding
CHEMBL2176528
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Inhibition of PDE4 in human PBMC assessed as inhibition of LPS-induced TNFalpha production incubated for 10 mins prior to LPS-challenge measured after 20 hrs by sandwich ELISA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Solubility-driven optimization of phosphodiesterase-4 inhibitors leading to a clinical candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.73 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2172376 | — | — | 1 | 7.72 |
| CHEMBL2172373 | — | — | 1 | 7.28 |
| CHEMBL2172375 | — | — | 1 | 7.28 |
| CHEMBL77826 | — | — | 1 | 7.17 |
| CHEMBL2172374 | — | — | 1 | 6.90 |
| CHEMBL2172372 | — | — | 1 | 6.82 |
| CHEMBL2172369 | — | — | 1 | 6.27 |
| CHEMBL2172368 | — | — | 1 | 6.11 |
| CHEMBL2172370 | — | — | 1 | 6.07 |
| CHEMBL2172366 | — | — | 1 | 5.71 |
| CHEMBL2172367 | — | — | 1 | - |
| CHEMBL2172371 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2172376 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2172373 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL2172375 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL77826 | — | IC50 | = | 67.6 | nM | 7.17 |
| CHEMBL2172374 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL2172372 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL2172369 | — | IC50 | = | 541.0 | nM | 6.27 |
| CHEMBL2172368 | — | IC50 | = | 769.0 | nM | 6.11 |
| CHEMBL2172370 | — | IC50 | = | 851.0 | nM | 6.07 |
| CHEMBL2172366 | — | IC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL2172367 | — | IC50 | - | — | - | |
| CHEMBL2172371 | — | IC50 | - | — | - |