Assay Detail
Binding
CHEMBL3412167
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as substrate by LanthaScreen TR-FRET assay
19
Total Activities
19
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 |
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 | 6.82 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3407849 | — | — | 1 | 8.30 |
| CHEMBL3407851 | — | — | 1 | 8.00 |
| CHEMBL3407850 | — | — | 1 | 7.92 |
| CHEMBL3407852 | — | — | 1 | 7.44 |
| CHEMBL3407504 | — | — | 1 | 7.38 |
| CHEMBL3407853 | — | — | 1 | 7.38 |
| CHEMBL3407857 | — | — | 1 | 7.01 |
| CHEMBL3407858 | — | — | 1 | 7.00 |
| CHEMBL3407854 | — | — | 1 | 6.62 |
| CHEMBL3407848 | — | — | 1 | 6.54 |
| CHEMBL3407859 | — | — | 1 | 6.51 |
| CHEMBL3407847 | — | — | 1 | 6.38 |
| CHEMBL3407860 | — | — | 1 | 6.21 |
| CHEMBL3407856 | — | — | 1 | 5.85 |
| CHEMBL3407846 | — | — | 1 | 5.41 |
| CHEMBL3407862 | — | — | 1 | 5.14 |
| CHEMBL3407855 | — | — | 1 | - |
| CHEMBL3407861 | — | — | 1 | - |
| CHEMBL3407863 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3407849 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3407851 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3407850 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3407852 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3407504 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3407853 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3407857 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL3407858 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3407854 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3407848 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3407859 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3407847 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3407860 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL3407856 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3407846 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL3407862 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL3407855 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3407861 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3407863 | — | IC50 | > | 50000.0 | nM | - |