Assay Detail
Binding
CHEMBL4407366
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Inhibition of recombinant His-tagged human PKA expressed in Escherichia coli using Ser/Thr 01 as substrate after 1 hr by Z-lyte assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 9.15 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4441825 | — | — | 1 | 9.70 |
| CHEMBL4440965 | — | — | 1 | 9.52 |
| CHEMBL3137336 | UPROSERTIB | 2.0 | 1 | 9.22 |
| CHEMBL4457064 | — | — | 1 | 8.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4441825 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4440965 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3137336 | UPROSERTIB | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4457064 | — | IC50 | = | 7.0 | nM | 8.15 |