Assay Detail
Binding
CHEMBL4189552
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length N-terminal GST-fused human PKC-alpha expressed in baculovirus expression system using (5FAM) RFARKGSLRQKNV as substrate after 60 mins by caliper assay
13
Total Activities
13
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
Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.60 | 7.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4212424 | — | — | 1 | 7.35 |
| CHEMBL4208685 | — | — | 1 | 7.19 |
| CHEMBL4202753 | — | — | 1 | 7.15 |
| CHEMBL4216507 | — | — | 1 | 6.96 |
| CHEMBL4206065 | — | — | 1 | 6.85 |
| CHEMBL4208028 | — | — | 1 | 6.60 |
| CHEMBL4213984 | — | — | 1 | 6.55 |
| CHEMBL4206023 | — | — | 1 | 6.47 |
| CHEMBL4211722 | — | — | 1 | 6.46 |
| CHEMBL4215391 | — | — | 1 | 6.42 |
| CHEMBL4212934 | — | — | 1 | 6.37 |
| CHEMBL4214431 | — | — | 1 | 5.85 |
| CHEMBL4203536 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4212424 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4208685 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4202753 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4216507 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4206065 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4208028 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4213984 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4206023 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4211722 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4215391 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4212934 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4214431 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4203536 | — | IC50 | = | 2500.0 | nM | 5.60 |