Assay Detail
Binding
CHEMBL2172954
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells after 2 hrs by Western blotting
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Eukaryotic translation initiation factor 2-alpha kinase 3 (CHEMBL6030) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.31 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2171132 | — | — | 1 | 7.52 |
| CHEMBL2171126 | — | — | 1 | 7.52 |
| CHEMBL2171139 | — | — | 1 | 7.52 |
| CHEMBL2171128 | — | — | 1 | 7.00 |
| CHEMBL2171142 | — | — | 1 | 7.00 |
| CHEMBL2171133 | — | — | 1 | - |
| CHEMBL2171124 | — | — | 1 | - |
| CHEMBL2171122 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2171132 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2171126 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2171139 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2171128 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2171142 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2171133 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL2171124 | — | IC50 | < | 30.0 | nM | - |
| CHEMBL2171122 | — | IC50 | < | 30.0 | nM | - |