Assay Detail
Binding
CHEMBL5111584
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GCN2 in human SK-OV-3 cells assessed as reduction in phosphorylation of eIF2alpha by cellular assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SK-OV-3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 7.07 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5200118 | — | — | 1 | 8.05 |
| CHEMBL5190023 | — | — | 1 | 7.80 |
| CHEMBL5170361 | — | — | 1 | 7.80 |
| CHEMBL5179922 | — | — | 1 | 7.70 |
| CHEMBL5199369 | — | — | 1 | 7.68 |
| CHEMBL5172690 | — | — | 1 | 7.60 |
| CHEMBL5180017 | — | — | 1 | 7.60 |
| CHEMBL5193210 | — | — | 1 | 7.54 |
| CHEMBL5208600 | — | — | 1 | 7.48 |
| CHEMBL5196751 | — | — | 1 | 7.46 |
| CHEMBL5197413 | — | — | 1 | 7.07 |
| CHEMBL5199088 | — | — | 1 | 6.97 |
| CHEMBL5183990 | — | — | 1 | 6.81 |
| CHEMBL5200952 | — | — | 1 | 6.80 |
| CHEMBL5196192 | — | — | 1 | 6.74 |
| CHEMBL5201930 | — | — | 1 | 6.62 |
| CHEMBL5175719 | — | — | 1 | 6.58 |
| CHEMBL5189317 | — | — | 1 | 6.42 |
| CHEMBL5195519 | — | — | 1 | 6.26 |
| CHEMBL5202342 | — | — | 1 | 6.21 |
| CHEMBL5172627 | — | — | 1 | 6.20 |
| CHEMBL5180106 | — | — | 1 | 6.12 |
| CHEMBL5204720 | — | — | 1 | - |
| CHEMBL5201758 | — | — | 1 | - |
| CHEMBL5188650 | — | — | 1 | - |
| CHEMBL5194718 | — | — | 1 | - |
| CHEMBL5192014 | — | — | 1 | - |
| CHEMBL5177614 | — | — | 1 | - |
| CHEMBL5208898 | — | — | 1 | - |
| CHEMBL5176674 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5200118 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5190023 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5170361 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5179922 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5199369 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5172690 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5180017 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5193210 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5208600 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5196751 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5197413 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL5199088 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL5183990 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL5200952 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL5196192 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL5201930 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5175719 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL5189317 | — | IC50 | = | 378.0 | nM | 6.42 |
| CHEMBL5195519 | — | IC50 | = | 545.0 | nM | 6.26 |
| CHEMBL5202342 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL5172627 | — | IC50 | = | 628.0 | nM | 6.20 |
| CHEMBL5180106 | — | IC50 | = | 763.0 | nM | 6.12 |
| CHEMBL5189372 | — | IC50 | - | — | - | |
| CHEMBL5195933 | — | IC50 | - | — | - | |
| CHEMBL5180483 | — | IC50 | - | — | - | |
| CHEMBL5194671 | — | IC50 | - | — | - | |
| CHEMBL5205311 | — | IC50 | - | — | - | |
| CHEMBL5207062 | — | IC50 | - | — | - | |
| CHEMBL5176674 | — | IC50 | - | — | - | |
| CHEMBL5208898 | — | IC50 | - | — | - | |
| CHEMBL5177614 | — | IC50 | - | — | - | |
| CHEMBL5192014 | — | IC50 | - | — | - | |
| CHEMBL5194718 | — | IC50 | - | — | - | |
| CHEMBL5188650 | — | IC50 | - | — | - | |
| CHEMBL5201758 | — | IC50 | - | — | - | |
| CHEMBL5204720 | — | IC50 | - | — | - |