Assay Detail
Functional
CHEMBL984534
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Inhibition of LPS-induced TNFalpha production in human whole blood
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.76 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL499477 | — | — | 1 | 8.52 |
| CHEMBL514564 | — | — | 1 | 8.30 |
| CHEMBL520502 | — | — | 1 | 7.18 |
| CHEMBL484753 | — | — | 1 | 7.16 |
| CHEMBL519193 | — | — | 1 | 7.12 |
| CHEMBL485620 | — | — | 1 | 6.92 |
| CHEMBL484931 | — | — | 1 | 6.85 |
| CHEMBL372575 | — | — | 1 | 6.80 |
| CHEMBL521509 | — | — | 1 | 6.80 |
| CHEMBL519355 | — | — | 1 | 6.80 |
| CHEMBL485629 | MK-0873 | 2.0 | 1 | 6.75 |
| CHEMBL456171 | — | — | 1 | 6.75 |
| CHEMBL520463 | — | — | 1 | 6.52 |
| CHEMBL464804 | — | — | 1 | 6.33 |
| CHEMBL485547 | — | — | 1 | 6.19 |
| CHEMBL484754 | — | — | 1 | 6.17 |
| CHEMBL456172 | — | — | 1 | 6.16 |
| CHEMBL456173 | — | — | 1 | 6.16 |
| CHEMBL456808 | — | — | 1 | 6.08 |
| CHEMBL464600 | — | — | 1 | 5.68 |
| CHEMBL464803 | — | — | 1 | - |
| CHEMBL511368 | — | — | 1 | - |
| CHEMBL464802 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL499477 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL514564 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL520502 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL484753 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL519193 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL485620 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL484931 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL372575 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL521509 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL519355 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL485629 | MK-0873 | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL456171 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL520463 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL464804 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL485547 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL484754 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL456172 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL456173 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL456808 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL464600 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL464803 | — | IC50 | - | — | - | |
| CHEMBL511368 | — | IC50 | - | — | - | |
| CHEMBL464802 | — | IC50 | - | — | - |