Assay Detail
Binding
CHEMBL5142534
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ARC-1063 fluorescent probe binding to recombinant human PKAC-alpha incubated for 1 hr by time-gated luminescence intensity based displacement assay
6
Total Activities
6
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
cAMP-dependent protein kinase catalytic subunit alpha (CHEMBL4101) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Construction of Covalent Bisubstrate Inhibitor of Protein Kinase Reacting with Cysteine Residue at Substrate-Binding Site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.58 | 8.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5188777 | — | — | 1 | 8.25 |
| CHEMBL5201435 | — | — | 1 | 7.62 |
| CHEMBL5174274 | — | — | 1 | 6.40 |
| CHEMBL5189362 | — | — | 1 | 6.10 |
| CHEMBL5174535 | — | — | 1 | 5.92 |
| CHEMBL5179913 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5188777 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL5201435 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5174274 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5189362 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL5174535 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5179913 | — | IC50 | = | 6100.0 | nM | 5.21 |