Assay Detail
Binding
CHEMBL2393916
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of atypical PKCzeta in bovine retinal endothelial cells assessed as TNFalpha/VEGF-induced endothelial permeability preincubated for 30 mins followed by TNFalpha induction for 1 hr and VEGF induction for 30 mins measured every 30 mins for 4 hrs by Transwell assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Cell Type | Endothelial cell |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 7.70 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2393423 | — | — | 1 | 9.00 |
| CHEMBL200027 | — | — | 1 | 8.70 |
| CHEMBL2393450 | — | — | 1 | 7.70 |
| CHEMBL2393447 | — | — | 1 | 6.57 |
| CHEMBL2393448 | — | — | 1 | 6.55 |
| CHEMBL2393451 | — | — | 1 | - |
| CHEMBL2393431 | — | — | 1 | - |
| CHEMBL2393427 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2393423 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL200027 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2393450 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2393447 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL2393448 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2393451 | — | EC50 | - | — | - | |
| CHEMBL2393431 | — | EC50 | > | 100.0 | nM | - |
| CHEMBL2393427 | — | EC50 | - | — | - |