Assay Detail
Binding
CHEMBL4020950
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [20-3H]phorbol 12,13-dibutyrate from RasGRP1 (unknown origin) in the presence of porcine brain phosphatidylserine by scintillation counting
8
Total Activities
8
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 |
Publication
Exploring the influence of indololactone structure on selectivity for binding to the C1 domains of PKCα, PKCε, and RasGRP.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.46 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL519741 | — | — | 1 | 9.24 |
| CHEMBL4097154 | — | — | 1 | 7.65 |
| CHEMBL4070999 | — | — | 1 | 7.65 |
| CHEMBL4075373 | — | — | 1 | 7.50 |
| CHEMBL4069954 | — | — | 1 | 7.40 |
| CHEMBL4099579 | — | — | 1 | 7.20 |
| CHEMBL4081576 | — | — | 1 | 6.88 |
| CHEMBL4066764 | — | — | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL519741 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL4097154 | — | Ki | = | 22.6 | nM | 7.65 |
| CHEMBL4070999 | — | Ki | = | 22.6 | nM | 7.65 |
| CHEMBL4075373 | — | Ki | = | 31.3 | nM | 7.50 |
| CHEMBL4069954 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4099579 | — | Ki | = | 63.3 | nM | 7.20 |
| CHEMBL4081576 | — | Ki | = | 133.0 | nM | 6.88 |
| CHEMBL4066764 | — | Ki | = | 666.0 | nM | 6.18 |