Assay Detail
Binding
CHEMBL5111583
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Inhibition of GCN2 (unknown origin)
46
Total Activities
46
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
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 | 46 | 7.40 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5200118 | — | — | 1 | 8.70 |
| CHEMBL5202342 | — | — | 1 | 8.52 |
| CHEMBL5190023 | — | — | 1 | 8.30 |
| CHEMBL5209076 | — | — | 1 | 8.30 |
| CHEMBL5179922 | — | — | 1 | 8.30 |
| CHEMBL5196751 | — | — | 1 | 8.10 |
| CHEMBL5208600 | — | — | 1 | 8.10 |
| CHEMBL5193210 | — | — | 1 | 8.00 |
| CHEMBL5202445 | — | — | 1 | 7.96 |
| CHEMBL5201930 | — | — | 1 | 7.82 |
| CHEMBL5172690 | — | — | 1 | 7.80 |
| CHEMBL5170361 | — | — | 1 | 7.80 |
| CHEMBL5199369 | — | — | 1 | 7.77 |
| CHEMBL5195519 | — | — | 1 | 7.68 |
| CHEMBL5180017 | — | — | 1 | 7.68 |
| CHEMBL5199283 | — | — | 1 | 7.64 |
| CHEMBL5201758 | — | — | 1 | 7.57 |
| CHEMBL5195933 | — | — | 1 | 7.54 |
| CHEMBL5197413 | — | — | 1 | 7.40 |
| CHEMBL5199088 | — | — | 1 | 7.37 |
| CHEMBL5175719 | — | — | 1 | 7.26 |
| CHEMBL5183235 | — | — | 1 | 7.25 |
| CHEMBL5183990 | — | — | 1 | 7.21 |
| CHEMBL5176674 | — | — | 1 | 7.21 |
| CHEMBL5200952 | — | — | 1 | 7.13 |
| CHEMBL5188650 | — | — | 1 | 7.12 |
| CHEMBL5189372 | — | — | 1 | 7.11 |
| CHEMBL5178602 | — | — | 1 | 7.09 |
| CHEMBL5189317 | — | — | 1 | 7.05 |
| CHEMBL5177614 | — | — | 1 | 7.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5200118 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5202342 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5209076 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5179922 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5190023 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5196751 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5208600 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5193210 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5202445 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5201930 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5172690 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5170361 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5199369 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5195519 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5180017 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5199283 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5201758 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5195933 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5197413 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5199088 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5175719 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5183235 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5176674 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL5183990 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL5200952 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL5188650 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL5189372 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5178602 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL5189317 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5177614 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL5180483 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL5194671 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL5208897 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL5196192 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL5172627 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL5205311 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL5180106 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL5207062 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL5194718 | — | IC50 | = | 359.0 | nM | 6.45 |
| CHEMBL5178135 | — | IC50 | = | 405.0 | nM | 6.39 |
| CHEMBL5192014 | — | IC50 | = | 923.0 | nM | 6.04 |
| CHEMBL5188269 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5208898 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5204720 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5204967 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5176845 | — | IC50 | > | 1000.0 | nM | - |