Assay Detail
Binding
CHEMBL4399586
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Inhibition of recombinant full length PKC delta (unknown origin) using ERMRPRKR- QGSVRRRV peptide as substrate measured after 15 mins in presence of ATP by spectrophotometric analysis
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
Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase Cθ (PKCθ) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 6.79 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4453941 | — | — | 1 | 7.92 |
| CHEMBL4589844 | — | — | 1 | 7.22 |
| CHEMBL4590477 | — | — | 1 | 6.87 |
| CHEMBL4457150 | — | — | 1 | 6.74 |
| CHEMBL4539521 | — | — | 1 | 6.62 |
| CHEMBL4461649 | — | — | 1 | 6.41 |
| CHEMBL4587816 | — | — | 1 | 6.27 |
| CHEMBL4559701 | — | — | 1 | 6.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4453941 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4589844 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL4590477 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL4457150 | — | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL4539521 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL4461649 | — | Ki | = | 392.0 | nM | 6.41 |
| CHEMBL4587816 | — | Ki | = | 542.0 | nM | 6.27 |
| CHEMBL4559701 | — | Ki | = | 584.0 | nM | 6.23 |