Assay Detail
Binding
CHEMBL1011051
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PKBgamma using 100 uM ATP and 30 uM TAMRA-kemptide substrate by fluorometric TLC assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
RAC-gamma serine/threonine-protein kinase (CHEMBL4816) ↗| 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 | 8 | 6.75 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL498924 | — | — | 1 | 8.62 |
| CHEMBL525385 | — | — | 1 | 7.84 |
| CHEMBL524516 | — | — | 1 | 7.25 |
| CHEMBL1315166 | — | — | 1 | 6.18 |
| CHEMBL297394 | — | — | 1 | 6.11 |
| CHEMBL501706 | — | — | 1 | 5.79 |
| CHEMBL505949 | — | — | 1 | 5.43 |
| CHEMBL495766 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL498924 | — | IC50 | = | 2.38 | nM | 8.62 |
| CHEMBL525385 | — | IC50 | = | 14.6 | nM | 7.84 |
| CHEMBL524516 | — | IC50 | = | 56.6 | nM | 7.25 |
| CHEMBL1315166 | — | IC50 | = | 662.0 | nM | 6.18 |
| CHEMBL297394 | — | IC50 | = | 774.0 | nM | 6.11 |
| CHEMBL501706 | — | IC50 | = | 1610.0 | nM | 5.79 |
| CHEMBL505949 | — | IC50 | = | 3750.0 | nM | 5.43 |
| CHEMBL495766 | — | IC50 | > | 1000000.0 | nM | - |