Assay Detail
Binding
CHEMBL768312
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Inhibition of cAMP-dependent protein kinase (PKA).
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
cAMP-dependent protein kinase (PKA) (CHEMBL2094138) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Design of potent protein kinase inhibitors using the bisubstrate approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.10 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL436718 | — | — | 1 | 8.52 |
| CHEMBL415414 | — | — | 1 | 6.52 |
| CHEMBL428973 | — | — | 1 | 5.92 |
| CHEMBL407100 | — | — | 1 | 5.92 |
| CHEMBL265876 | — | — | 1 | 5.92 |
| CHEMBL351282 | — | — | 1 | 5.70 |
| CHEMBL344314 | — | — | 1 | 5.70 |
| CHEMBL540848 | — | — | 1 | 5.46 |
| CHEMBL75773 | — | — | 1 | 5.22 |
| CHEMBL410778 | — | — | 1 | - |
| CHEMBL263188 | — | — | 1 | - |
| CHEMBL437640 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL436718 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL415414 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL428973 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL407100 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL265876 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL351282 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL344314 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL540848 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL75773 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL410778 | — | IC50 | > | 75000.0 | nM | - |
| CHEMBL263188 | — | IC50 | > | 75000.0 | nM | - |
| CHEMBL437640 | — | IC50 | > | 75000.0 | nM | - |