Assay Detail
Binding
CHEMBL3706019
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding Assay: Human recombinant PDE4 (Gene bank accession no NM006203) was incubated for 1 hour with the test compound at concentrations up to 10 μM, with cAMP (1x10-5M), and with a low amount (0.021 MBq) of radioactively labelled cAMP. At the end of the incubation, the cleavage of the substrate was evaluated by the binding of the AMP product to SPA beads, which generate chemo luminescence when bound to the radioactive tracer. The AMP product inhibited the binding of the radioactive tracer to the beads, and the luminescent signal was competed.
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
3',5'-cyclic-AMP phosphodiesterase 4A (CHEMBL254) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Triazolopyridines as phosphodiesterase inhibitors for treatment of dermal diseases
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.88 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3676245 | — | — | 1 | 10.00 |
| CHEMBL3676246 | — | — | 1 | 9.70 |
| CHEMBL3676244 | — | — | 1 | 9.70 |
| CHEMBL3639751 | — | — | 1 | 9.52 |
| CHEMBL3676243 | — | — | 1 | 9.40 |
| CHEMBL3676240 | — | — | 1 | 9.30 |
| CHEMBL3676242 | — | — | 1 | 9.15 |
| CHEMBL3676241 | — | — | 1 | 9.00 |
| CHEMBL3676231 | — | — | 1 | 8.70 |
| CHEMBL3676257 | — | — | 1 | 8.52 |
| CHEMBL3676247 | — | — | 1 | 8.52 |
| CHEMBL3676236 | — | — | 1 | 8.40 |
| CHEMBL3676233 | — | — | 1 | 8.15 |
| CHEMBL3676248 | — | — | 1 | 8.10 |
| CHEMBL3676239 | — | — | 1 | 7.62 |
| CHEMBL3676234 | — | — | 1 | 7.58 |
| CHEMBL3676237 | — | — | 1 | 7.35 |
| CHEMBL3676256 | — | — | 1 | 7.34 |
| CHEMBL3676253 | — | — | 1 | 7.28 |
| CHEMBL3676238 | — | — | 1 | 7.26 |
| CHEMBL3676252 | — | — | 1 | 7.17 |
| CHEMBL3676232 | — | — | 1 | 6.87 |
| CHEMBL3676251 | — | — | 1 | 6.58 |
| CHEMBL3676235 | — | — | 1 | 6.52 |
| CHEMBL3676255 | — | — | 1 | 6.26 |
| CHEMBL3676249 | — | — | 1 | 5.60 |
| CHEMBL3676254 | — | — | 1 | 5.51 |
| CHEMBL3676250 | — | — | 1 | 5.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3676245 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3676246 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3676244 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3639751 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3676243 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3676240 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3676242 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3676241 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3676231 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3676257 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3676247 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3676236 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3676233 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3676248 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3676239 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3676234 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3676237 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3676256 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3676253 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3676238 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3676252 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3676232 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL3676251 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL3676235 | — | IC50 | = | 305.0 | nM | 6.52 |
| CHEMBL3676255 | — | IC50 | = | 548.0 | nM | 6.26 |
| CHEMBL3676249 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3676254 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3676250 | — | IC50 | = | 3600.0 | nM | 5.44 |