Assay Detail
Binding
CHEMBL2393915
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of atypical PKCzeta (unknown origin) using CREBtide as substrate incubated for 1 hr measured every 2.5 mins by ADP Quest assay
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and structure-activity relationships of 2-amino-3-carboxy-4-phenylthiophenes as novel atypical protein kinase C inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.58 | 6.10 |
| INH | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2393448 | — | — | 1 | 6.10 |
| CHEMBL2393450 | — | — | 1 | 5.70 |
| CHEMBL2393447 | — | — | 1 | 5.70 |
| CHEMBL2393431 | — | — | 1 | 5.70 |
| CHEMBL2393451 | — | — | 1 | 5.40 |
| CHEMBL2393427 | — | — | 1 | 5.22 |
| CHEMBL2393423 | — | — | 1 | 5.22 |
| CHEMBL2393417 | — | — | 1 | - |
| CHEMBL2393416 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2393448 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL2393450 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2393447 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2393431 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2393451 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2393427 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL2393423 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL2393417 | — | INH | = | 13.0 | uM | - |
| CHEMBL2393416 | — | INH | = | 23.0 | uM | - |