Assay Detail
Binding
CHEMBL4251843
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-c-AMP from His-Tb-tagged human PDE4D2 (86 to 413 residues) preincubated for 10 mins followed by [3H]-c-AMP addition measured after 1 hr by scintillation proximity assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
3',5'-cyclic-AMP phosphodiesterase 4D (CHEMBL288) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of imidazo[1,2-<i>b</i>]pyridazine TYK2 pseudokinase ligands as potent and selective allosteric inhibitors of TYK2 signalling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.14 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4293907 | — | — | 1 | 8.22 |
| CHEMBL4291200 | — | — | 1 | 7.89 |
| CHEMBL4289426 | — | — | 1 | 7.82 |
| CHEMBL4278757 | — | — | 1 | 7.75 |
| CHEMBL4285841 | — | — | 1 | 7.62 |
| CHEMBL4287761 | — | — | 1 | 7.50 |
| CHEMBL4279883 | — | — | 1 | 7.37 |
| CHEMBL4279157 | — | — | 1 | 7.21 |
| CHEMBL4295039 | — | — | 1 | 7.06 |
| CHEMBL4291611 | — | — | 1 | 6.42 |
| CHEMBL4283351 | — | — | 1 | 5.62 |
| CHEMBL4290130 | — | — | 1 | 5.25 |
| CHEMBL4281304 | — | — | 1 | - |
| CHEMBL4293510 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4293907 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4291200 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4289426 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4278757 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4285841 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4287761 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4279883 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4279157 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4295039 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4291611 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4283351 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4290130 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4281304 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4293510 | — | IC50 | > | 33000.0 | nM | - |