Assay Detail
Binding
CHEMBL5546197
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Activation of GCN2 in HEK293 cells transfected with ATF4 response element preincubated for 30 mins followed by halofuginone addition and measured after 6 hrs by One-Glo reagent based plate reader assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of HC-7366: An Orally Bioavailable and Efficacious GCN2 Kinase Activator.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 6.85 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5571568 | — | — | 1 | 7.89 |
| CHEMBL5574976 | — | — | 1 | 7.34 |
| CHEMBL5569981 | — | — | 1 | 7.14 |
| CHEMBL5591595 | — | — | 1 | 6.96 |
| CHEMBL5593998 | — | — | 1 | 6.92 |
| CHEMBL5590796 | — | — | 1 | 6.85 |
| CHEMBL5579682 | — | — | 1 | 6.80 |
| CHEMBL5571377 | — | — | 1 | 6.80 |
| CHEMBL5593039 | — | — | 1 | 6.62 |
| CHEMBL5574193 | — | — | 1 | 6.36 |
| CHEMBL5575532 | — | — | 1 | 6.34 |
| CHEMBL5574769 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5571568 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5574976 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL5569981 | — | EC50 | = | 72.0 | nM | 7.14 |
| CHEMBL5591595 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5593998 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5590796 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5579682 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5571377 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5593039 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5574193 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5575532 | — | EC50 | = | 460.0 | nM | 6.34 |
| CHEMBL5574769 | — | EC50 | = | 750.0 | nM | 6.12 |