Assay Detail
Binding
CHEMBL893771
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Inhibition of PDE4 in U937 cells
17
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U-937 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Dual M3 antagonists-PDE4 inhibitors. Part 2: Synthesis and SAR of 3-substituted azetidinyl derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.16 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL396761 | — | — | 2 | 7.30 |
| CHEMBL232417 | — | — | 1 | 6.70 |
| CHEMBL232419 | — | — | 2 | 6.60 |
| CHEMBL436814 | — | — | 1 | 6.30 |
| CHEMBL205654 | — | — | 2 | 6.20 |
| CHEMBL242822 | — | — | 1 | 6.20 |
| CHEMBL232416 | — | — | 1 | 6.10 |
| CHEMBL232860 | — | — | 1 | 6.10 |
| CHEMBL245137 | — | — | 1 | 6.00 |
| CHEMBL389992 | — | — | 1 | 5.70 |
| CHEMBL242823 | — | — | 1 | 5.70 |
| CHEMBL234099 | — | — | 1 | 5.50 |
| CHEMBL232208 | — | — | 1 | 5.40 |
| CHEMBL434388 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL396761 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL396761 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL232417 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL232419 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL232419 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL436814 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL242822 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL205654 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL232416 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL205654 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL232860 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL245137 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL389992 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL242823 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL234099 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL232208 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL434388 | — | IC50 | = | 5000.0 | nM | 5.30 |