Assay Detail
Binding
CHEMBL757891
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Inhibition of phosphodiesterase 4 (PDE4) in human neutrophils
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Novel selective PDE4 inhibitors. 2. Synthesis and structure-activity relationships of 4-aryl-substituted cis-tetra- and cis-hexahydrophthalazinones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 8.01 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL314936 | — | — | 1 | 9.70 |
| CHEMBL82399 | — | — | 1 | 9.50 |
| CHEMBL312886 | — | — | 1 | 9.50 |
| CHEMBL315762 | — | — | 1 | 9.20 |
| CHEMBL85005 | — | — | 1 | 9.20 |
| CHEMBL314782 | — | — | 1 | 9.10 |
| CHEMBL263811 | — | — | 1 | 9.00 |
| CHEMBL84556 | — | — | 1 | 9.00 |
| CHEMBL421347 | — | — | 1 | 8.90 |
| CHEMBL430831 | — | — | 1 | 8.80 |
| CHEMBL83869 | — | — | 1 | 8.70 |
| CHEMBL315273 | — | — | 1 | 8.60 |
| CHEMBL84657 | — | — | 1 | 8.60 |
| CHEMBL315453 | — | — | 1 | 8.40 |
| CHEMBL310143 | — | — | 1 | 8.30 |
| CHEMBL85158 | — | — | 1 | 8.10 |
| CHEMBL81960 | — | — | 1 | 8.10 |
| CHEMBL84689 | — | — | 1 | 8.00 |
| CHEMBL313750 | — | — | 1 | 8.00 |
| CHEMBL85706 | — | — | 1 | 8.00 |
| CHEMBL86229 | — | — | 1 | 7.80 |
| CHEMBL84614 | — | — | 1 | 7.80 |
| CHEMBL84601 | — | — | 1 | 7.60 |
| CHEMBL312185 | — | — | 1 | 7.40 |
| CHEMBL83398 | — | — | 1 | 7.40 |
| CHEMBL430893 | (-)-ROLIPRAM | — | 1 | 7.30 |
| CHEMBL420408 | — | — | 1 | 7.20 |
| CHEMBL315042 | — | — | 1 | 7.20 |
| CHEMBL511115 | CILOMILAST | 3.0 | 1 | 7.00 |
| CHEMBL313881 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL314936 | — | IC50 | = | 0.1995 | nM | 9.70 |
| CHEMBL82399 | — | IC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL312886 | — | IC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL315762 | — | IC50 | = | 0.631 | nM | 9.20 |
| CHEMBL85005 | — | IC50 | = | 0.631 | nM | 9.20 |
| CHEMBL314782 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL263811 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL84556 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL421347 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL430831 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL83869 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL315273 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL84657 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL315453 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL310143 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL85158 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL81960 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL85706 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL313750 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL84689 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL86229 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL84614 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL84601 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL312185 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL83398 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL430893 | (-)-ROLIPRAM | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL315042 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL420408 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL511115 | CILOMILAST | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL313881 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL85611 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL431602 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL86208 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL82500 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL84688 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL86170 | — | IC50 | > | 10000.0 | nM | - |