Assay Detail
Binding
CHEMBL3412176
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GCN2 phosphorylation in human U2OS cells preincubated for 1 hr followed by drug wash out and incubated for 2 hrs by MSD assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| 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 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.18 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3407504 | — | — | 1 | 7.77 |
| CHEMBL3407858 | — | — | 1 | 7.36 |
| CHEMBL3407857 | — | — | 1 | 7.30 |
| CHEMBL3407859 | — | — | 1 | 7.28 |
| CHEMBL3407860 | — | — | 1 | 7.10 |
| CHEMBL3407856 | — | — | 1 | 6.28 |
| CHEMBL3407847 | — | — | 1 | - |
| CHEMBL3407848 | — | — | 1 | - |
| CHEMBL3407849 | — | — | 1 | - |
| CHEMBL3407850 | — | — | 1 | - |
| CHEMBL3407851 | — | — | 1 | - |
| CHEMBL3407852 | — | — | 1 | - |
| CHEMBL3407853 | — | — | 1 | - |
| CHEMBL3407846 | — | — | 1 | - |
| CHEMBL3407855 | — | — | 1 | - |
| CHEMBL3407861 | — | — | 1 | - |
| CHEMBL3407862 | — | — | 1 | - |
| CHEMBL3407863 | — | — | 1 | - |
| CHEMBL3407854 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3407504 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3407858 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3407857 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3407859 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3407860 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3407856 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL3407847 | — | IC50 | - | — | - | |
| CHEMBL3407848 | — | IC50 | - | — | - | |
| CHEMBL3407849 | — | IC50 | - | — | - | |
| CHEMBL3407850 | — | IC50 | - | — | - | |
| CHEMBL3407851 | — | IC50 | - | — | - | |
| CHEMBL3407852 | — | IC50 | - | — | - | |
| CHEMBL3407853 | — | IC50 | - | — | - | |
| CHEMBL3407846 | — | IC50 | - | — | - | |
| CHEMBL3407855 | — | IC50 | - | — | - | |
| CHEMBL3407861 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3407862 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3407863 | — | IC50 | - | — | - | |
| CHEMBL3407854 | — | IC50 | - | — | - |