Assay Detail
Binding
CHEMBL855484
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human eosinophil phosphodiesterase
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.43 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | 2.0 | 1 | 8.05 |
| CHEMBL373810 | — | — | 1 | 7.52 |
| CHEMBL219418 | — | — | 1 | 7.52 |
| CHEMBL386902 | — | — | 1 | 7.40 |
| CHEMBL376441 | — | — | 1 | 7.40 |
| CHEMBL218103 | — | — | 1 | 7.10 |
| CHEMBL374995 | — | — | 1 | 7.05 |
| CHEMBL218641 | — | — | 1 | 7.05 |
| CHEMBL439000 | — | — | 1 | 6.92 |
| CHEMBL376440 | — | — | 1 | 6.92 |
| CHEMBL376857 | — | — | 1 | 6.89 |
| CHEMBL376489 | — | — | 1 | 6.85 |
| CHEMBL217899 | TOFIMILAST | 2.0 | 1 | 6.85 |
| CHEMBL219192 | — | — | 1 | 6.80 |
| CHEMBL511115 | CILOMILAST | 3.0 | 1 | 6.77 |
| CHEMBL218221 | — | — | 1 | 6.75 |
| CHEMBL434741 | — | — | 1 | 6.64 |
| CHEMBL387479 | — | — | 1 | 6.58 |
| CHEMBL218696 | — | — | 1 | 6.55 |
| CHEMBL218653 | — | — | 1 | 6.54 |
| CHEMBL425987 | — | — | 1 | 6.40 |
| CHEMBL219223 | — | — | 1 | 6.37 |
| CHEMBL218053 | — | — | 1 | 6.24 |
| CHEMBL374220 | — | — | 1 | 6.04 |
| CHEMBL219157 | — | — | 1 | 6.00 |
| CHEMBL218990 | — | — | 1 | 5.92 |
| CHEMBL218793 | — | — | 1 | 5.89 |
| CHEMBL219571 | — | — | 1 | 5.85 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 5.48 |
| CHEMBL217953 | — | — | 1 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL373810 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL219418 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL386902 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL376441 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL218103 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL374995 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL218641 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL439000 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL376440 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL376857 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL376489 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL217899 | TOFIMILAST | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL219192 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL511115 | CILOMILAST | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL218221 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL434741 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL387479 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL218696 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL218653 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL425987 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL219223 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL218053 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL374220 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL219157 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL218990 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL218793 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL219571 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 3340.0 | nM | 5.48 |
| CHEMBL217953 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL218938 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL387173 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL384329 | — | IC50 | = | 57000.0 | nM | 4.24 |