Assay Detail
Binding
CHEMBL3412175
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Inhibition of PERK in human HT1080 cells assessed as inhibition of thapsigargin-induced CHoP mRNA expression preincubated for 1 hr followed by thapsigargin-induction measured after 2 hrs by bDNA assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HT-1080 |
| 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 | 6.19 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3407846 | — | — | 1 | 7.70 |
| CHEMBL3407863 | — | — | 1 | 7.05 |
| CHEMBL3407850 | — | — | 1 | 6.50 |
| CHEMBL3407856 | — | — | 1 | 6.50 |
| CHEMBL3407852 | — | — | 1 | 6.40 |
| CHEMBL3407504 | — | — | 1 | 6.32 |
| CHEMBL3407849 | — | — | 1 | 6.32 |
| CHEMBL3407853 | — | — | 1 | 6.19 |
| CHEMBL3407857 | — | — | 1 | 6.12 |
| CHEMBL3407862 | — | — | 1 | 6.11 |
| CHEMBL3407851 | — | — | 1 | 6.00 |
| CHEMBL3407858 | — | — | 1 | 5.96 |
| CHEMBL3407847 | — | — | 1 | 5.92 |
| CHEMBL3407859 | — | — | 1 | 5.68 |
| CHEMBL3407854 | — | — | 1 | 5.64 |
| CHEMBL3407861 | — | — | 1 | 5.52 |
| CHEMBL3407860 | — | — | 1 | 5.32 |
| CHEMBL3407855 | — | — | 1 | - |
| CHEMBL3407848 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3407846 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3407863 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3407850 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3407856 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3407852 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3407504 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3407849 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3407853 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL3407857 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL3407862 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL3407851 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3407858 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3407847 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3407859 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3407854 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3407861 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3407860 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL3407855 | — | IC50 | - | — | - | |
| CHEMBL3407848 | — | IC50 | - | — | - |