Assay Detail
Binding
CHEMBL2172950
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Inhibition of HRI assessed as EIF2AK1 phosphorylation
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Eukaryotic translation initiation factor 2-alpha kinase 1 (CHEMBL6029) ↗| 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 | 5 | 5.69 | 6.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2171122 | — | — | 1 | 6.67 |
| CHEMBL2171124 | — | — | 1 | 6.38 |
| CHEMBL2171132 | — | — | 1 | 5.73 |
| CHEMBL2171128 | — | — | 1 | 4.92 |
| CHEMBL2171133 | — | — | 1 | 4.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2171122 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL2171124 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2171132 | — | IC50 | = | 1863.0 | nM | 5.73 |
| CHEMBL2171128 | — | IC50 | = | 12080.0 | nM | 4.92 |
| CHEMBL2171133 | — | IC50 | = | 17020.0 | nM | 4.77 |