Assay Detail
Binding
CHEMBL2393917
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of atypical PKCzeta in HEK293 cells assessed as TNF-induced NFkappaB activation incubated for 3 hrs prior to TNF induction measured after 5 hrs by bright-glo luciferase reporter gene assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 |
|---|---|---|---|
| EC50 | 8 | 8.68 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2393448 | — | — | 1 | 9.00 |
| CHEMBL2393447 | — | — | 1 | 9.00 |
| CHEMBL2393431 | — | — | 1 | 9.00 |
| CHEMBL2393450 | — | — | 1 | 8.70 |
| CHEMBL2393427 | — | — | 1 | 8.70 |
| CHEMBL200027 | — | — | 1 | 8.52 |
| CHEMBL2393423 | — | — | 1 | 8.52 |
| CHEMBL2393451 | — | — | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2393448 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2393447 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2393431 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2393450 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2393427 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL200027 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2393423 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2393451 | — | EC50 | = | 10.0 | nM | 8.00 |