Assay Detail
Binding
CHEMBL3706116
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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.
21
Total Activities
20
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
Compounds, formulations, and methods of protein kinase C inhibition
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 5.23 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2393448 | — | — | 1 | 6.00 |
| CHEMBL2393447 | — | — | 1 | 5.70 |
| CHEMBL2393450 | — | — | 1 | 5.70 |
| CHEMBL3702549 | — | — | 1 | 5.52 |
| CHEMBL2393451 | — | — | 1 | 5.40 |
| CHEMBL2393437 | — | — | 1 | 5.40 |
| CHEMBL3702547 | — | — | 1 | 5.40 |
| CHEMBL3702550 | — | — | 1 | 5.30 |
| CHEMBL3702548 | — | — | 1 | 5.30 |
| CHEMBL2393431 | — | — | 1 | 5.30 |
| CHEMBL2393427 | — | — | 1 | 5.22 |
| CHEMBL2393423 | — | — | 2 | 5.22 |
| CHEMBL3702543 | — | — | 1 | 5.22 |
| CHEMBL3702544 | — | — | 1 | 5.22 |
| CHEMBL2393441 | — | — | 1 | 5.16 |
| CHEMBL2393432 | — | — | 1 | 5.16 |
| CHEMBL3702545 | — | — | 1 | 4.96 |
| CHEMBL2393452 | — | — | 1 | 4.77 |
| CHEMBL2393461 | — | — | 1 | 4.70 |
| CHEMBL3702546 | — | — | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2393448 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2393447 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2393450 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3702549 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL2393451 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2393437 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3702547 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3702550 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3702548 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2393431 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2393427 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL2393423 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3702543 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3702544 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL2393441 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL2393432 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3702545 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2393452 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL2393461 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL3702546 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL2393423 | — | IC50 | = | 35000.0 | nM | 4.46 |