Basic Information
ID: ALA3706116
Type: Binding
Description: Luminescence-Based Kinase Assay: IC50 values were determined using an in vitro luminescence-based kinase assay against aPKCζ to elucidate a pharmacophore. The IC50 values determined for isopropyl 2-amino-4-(3,4-dimethoxyphenyl)thiophene-3-carboxylate (also referred to as PKCl-diMeO, PKCζl-diMeO, or PKCzl3), and compounds described herein and illustrated in FIGS. 1, 3, and 7 are described in Table 1. The IC50 values were determined using an ADP Quest assay with 500 ng/ml aPKCζ, 10 μM CREBtide, and 10 μM ATP. In PKCζ kinase activity assays using 30 μM of candidate compound, PKCl-diMeO and the compounds illustrated in FIG. 7 resulted in a 55-100% inhibition in kinase activity.
Format: BAO_0000357
Organism: Homo sapiens
Target: Protein kinase C zeta(ALA3438)
Document: ALA3638452
BindingDB Source: 6568
Activity Charts
Bioactivity
Activity Types for Assay ALA3706116
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 321.40 | 3.58 | 3.58 |
| 369.44 | 4.37 | 4.37 |
| 399.47 | 4.38 | 4.38 |
| 387.43 | 4.51 | 4.51 |
| 306.39 | 2.76 | 2.76 |
| 260.32 | 2.89 | 2.89 |
| 262.33 | 2.76 | 2.76 |
| 290.39 | 3.24 | 3.24 |
| 291.33 | 2.90 | 2.90 |
| 295.33 | 3.32 | 3.32 |
| 295.33 | 3.32 | 3.32 |
| 353.40 | 4.08 | 4.08 |
| 304.37 | 3.13 | 3.13 |
| 382.44 | 3.46 | 3.46 |
| 352.42 | 3.45 | 3.45 |
| 305.36 | 3.29 | 3.29 |
| 348.42 | 2.49 | 2.49 |
| 329.25 | 4.44 | 4.44 |
| 357.26 | 3.78 | 3.78 |
| 315.23 | 4.05 | 4.05 |