Assay Detail
Binding
CHEMBL3412166
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal His-tagged PERK expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as substrate by LanthaScreen TR-FRET assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 20 | 8.14 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3407849 | — | — | 1 | 9.00 |
| CHEMBL3407846 | — | — | 1 | 9.00 |
| CHEMBL3407863 | — | — | 1 | 8.70 |
| CHEMBL3407504 | — | — | 1 | 8.52 |
| CHEMBL3407850 | — | — | 1 | 8.52 |
| CHEMBL3407848 | — | — | 1 | 8.40 |
| CHEMBL3407856 | — | — | 1 | 8.40 |
| CHEMBL3407852 | — | — | 1 | 8.40 |
| CHEMBL3407854 | — | — | 1 | 8.30 |
| CHEMBL3407851 | — | — | 1 | 8.30 |
| CHEMBL3407859 | — | — | 1 | 8.22 |
| CHEMBL3407853 | — | — | 1 | 8.22 |
| CHEMBL3407862 | — | — | 1 | 8.22 |
| CHEMBL3407857 | — | — | 1 | 8.05 |
| CHEMBL3407860 | — | — | 1 | 7.96 |
| CHEMBL3407858 | — | — | 1 | 7.96 |
| CHEMBL3407847 | — | — | 1 | 7.39 |
| CHEMBL3407864 | — | — | 1 | 7.38 |
| CHEMBL3407861 | — | — | 1 | 7.28 |
| CHEMBL3407855 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3407849 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3407846 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3407863 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3407504 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3407850 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3407848 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3407856 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3407852 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3407854 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3407851 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3407859 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3407853 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3407862 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3407857 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3407860 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3407858 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3407847 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3407864 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3407861 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3407855 | — | IC50 | = | 240.0 | nM | 6.62 |