Assay Detail
Binding
CHEMBL1011048
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PKA catalytic subunit alpha using 100 uM ATP and 30 uM TAMRA-kemptide substrate by fluorometric TLC assay
9
Total Activities
9
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 |
|---|---|---|---|
| IC50 | 9 | 6.77 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL525385 | — | — | 1 | 8.27 |
| CHEMBL524516 | — | — | 1 | 7.87 |
| CHEMBL498924 | — | — | 1 | 7.68 |
| CHEMBL297394 | — | — | 1 | 7.27 |
| CHEMBL505949 | — | — | 1 | 7.01 |
| CHEMBL1315166 | — | — | 1 | 7.00 |
| CHEMBL501706 | — | — | 1 | 5.68 |
| CHEMBL450179 | — | — | 1 | 5.58 |
| CHEMBL495766 | — | — | 1 | 4.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL525385 | — | IC50 | = | 5.32 | nM | 8.27 |
| CHEMBL524516 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL498924 | — | IC50 | = | 21.1 | nM | 7.68 |
| CHEMBL297394 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL505949 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL1315166 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL501706 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL450179 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL495766 | — | IC50 | = | 26000.0 | nM | 4.58 |