Assay Detail
Binding
CHEMBL5142544
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Irreversible inhibition of ARC-1063 fluorescent probe binding to recombinant human PKAC-alpha incubated for 22 hrs followed by probe addition at 20 nM and further incubated for 1 hr by time-gated luminescence intensity based displacement assay
2
Total Activities
2
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 | 2 | 5.69 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5174535 | — | — | 1 | 6.10 |
| CHEMBL5174274 | — | — | 1 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5174535 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL5174274 | — | IC50 | = | 5300.0 | nM | 5.28 |