Assay Detail
Binding
CHEMBL1011049
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Binding affinity to PKA catalytic subunit alpha by fluorescence polarization assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
cAMP-dependent protein kinase catalytic subunit alpha (CHEMBL4101) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structural analysis of ARC-type inhibitor (ARC-1034) binding to protein kinase A catalytic subunit and rational design of bisubstrate analogue inhibitors of basophilic protein kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 27 | 6.36 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL524516 | — | — | 1 | 9.30 |
| CHEMBL498924 | — | — | 1 | 8.74 |
| CHEMBL505949 | — | — | 1 | 8.24 |
| CHEMBL297394 | — | — | 1 | 8.12 |
| CHEMBL506331 | — | — | 1 | 8.06 |
| CHEMBL495088 | — | — | 1 | 8.02 |
| CHEMBL500989 | — | — | 1 | 7.90 |
| CHEMBL449834 | — | — | 1 | 7.08 |
| CHEMBL509411 | — | — | 1 | 7.02 |
| CHEMBL465518 | — | — | 1 | 6.61 |
| CHEMBL501706 | — | — | 1 | 6.60 |
| CHEMBL450179 | — | — | 1 | 6.50 |
| CHEMBL523738 | — | — | 1 | 6.35 |
| CHEMBL447678 | — | — | 1 | 6.23 |
| CHEMBL496141 | — | — | 1 | 5.79 |
| CHEMBL454225 | — | — | 1 | 5.71 |
| CHEMBL495766 | — | — | 1 | 5.66 |
| CHEMBL497800 | — | — | 1 | 5.22 |
| CHEMBL523401 | — | — | 1 | 5.08 |
| CHEMBL522899 | — | — | 1 | 4.87 |
| CHEMBL510221 | — | — | 1 | 4.73 |
| CHEMBL1315166 | — | — | 1 | 4.64 |
| CHEMBL521551 | — | — | 1 | 4.28 |
| CHEMBL496365 | — | — | 1 | 4.25 |
| CHEMBL495767 | — | — | 1 | 4.01 |
| CHEMBL450260 | — | — | 1 | - |
| CHEMBL525385 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL524516 | — | Kd | = | 0.5 | nM | 9.30 |
| CHEMBL498924 | — | Kd | = | 1.8 | nM | 8.74 |
| CHEMBL505949 | — | Kd | = | 5.8 | nM | 8.24 |
| CHEMBL297394 | — | Kd | = | 7.6 | nM | 8.12 |
| CHEMBL506331 | — | Kd | = | 8.7 | nM | 8.06 |
| CHEMBL495088 | — | Kd | = | 9.5 | nM | 8.02 |
| CHEMBL500989 | — | Kd | = | 12.6 | nM | 7.90 |
| CHEMBL449834 | — | Kd | = | 83.0 | nM | 7.08 |
| CHEMBL509411 | — | Kd | = | 95.4 | nM | 7.02 |
| CHEMBL465518 | — | Kd | = | 247.0 | nM | 6.61 |
| CHEMBL501706 | — | Kd | = | 249.0 | nM | 6.60 |
| CHEMBL450179 | — | Kd | = | 319.0 | nM | 6.50 |
| CHEMBL523738 | — | Kd | = | 443.0 | nM | 6.35 |
| CHEMBL447678 | — | Kd | = | 594.0 | nM | 6.23 |
| CHEMBL496141 | — | Kd | = | 1640.0 | nM | 5.79 |
| CHEMBL454225 | — | Kd | = | 1960.0 | nM | 5.71 |
| CHEMBL495766 | — | Kd | = | 2180.0 | nM | 5.66 |
| CHEMBL497800 | — | Kd | = | 6050.0 | nM | 5.22 |
| CHEMBL523401 | — | Kd | = | 8230.0 | nM | 5.08 |
| CHEMBL522899 | — | Kd | = | 13500.0 | nM | 4.87 |
| CHEMBL510221 | — | Kd | = | 18700.0 | nM | 4.73 |
| CHEMBL1315166 | — | Kd | = | 23000.0 | nM | 4.64 |
| CHEMBL521551 | — | Kd | = | 52100.0 | nM | 4.28 |
| CHEMBL496365 | — | Kd | = | 55800.0 | nM | 4.25 |
| CHEMBL495767 | — | Kd | = | 98700.0 | nM | 4.01 |
| CHEMBL450260 | — | Kd | > | 100000.0 | nM | - |
| CHEMBL525385 | — | Kd | < | 0.5 | nM | - |