Assay Detail
Functional
CHEMBL5500871
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Anti-necroptosis activity against human HT-29 cell assessed as inhibition of TSZ-induced necroptosis by chemiluminescence assay
28
Total Activities
27
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HT-29 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Scaffold hopping derived novel benzoxazepinone receptor-interacting protein kinase 1 (RIP1) inhibitors as anti-necroptosis agents: Anti-inflammatory effect in systemic inflammatory response syndrome (SIRS) and epilepsy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 27 | 6.39 | 8.39 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4071864 | GSK2982772 | 2.0 | 1 | 8.39 |
| CHEMBL5557467 | — | — | 2 | 8.15 |
| CHEMBL5426073 | — | — | 1 | 7.79 |
| CHEMBL5558176 | — | — | 1 | 7.69 |
| CHEMBL5555230 | — | — | 1 | 7.61 |
| CHEMBL5532569 | — | — | 1 | 7.59 |
| CHEMBL5542667 | — | — | 1 | 7.44 |
| CHEMBL5549854 | — | — | 1 | 7.39 |
| CHEMBL5556996 | — | — | 1 | 7.36 |
| CHEMBL5557979 | — | — | 1 | 6.96 |
| CHEMBL5559287 | — | — | 1 | 6.92 |
| CHEMBL5559296 | — | — | 1 | 6.89 |
| CHEMBL5557281 | — | — | 1 | 6.48 |
| CHEMBL5517885 | — | — | 1 | 6.44 |
| CHEMBL5555071 | — | — | 1 | 6.30 |
| CHEMBL5555720 | — | — | 1 | 5.98 |
| CHEMBL5558635 | — | — | 1 | 5.96 |
| CHEMBL5542308 | — | — | 1 | 5.78 |
| CHEMBL5558745 | — | — | 1 | 5.72 |
| CHEMBL5505794 | — | — | 1 | 5.59 |
| CHEMBL5559107 | — | — | 1 | 5.45 |
| CHEMBL5549748 | — | — | 1 | 5.00 |
| CHEMBL5555121 | — | — | 1 | 4.97 |
| CHEMBL5542676 | — | — | 1 | 4.89 |
| CHEMBL5523573 | — | — | 1 | 4.70 |
| CHEMBL5558784 | — | — | 1 | 4.57 |
| CHEMBL5559021 | — | — | 1 | 4.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4071864 | GSK2982772 | EC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5557467 | — | EC50 | = | 7.04 | nM | 8.15 |
| CHEMBL5426073 | — | EC50 | = | 16.17 | nM | 7.79 |
| CHEMBL5558176 | — | EC50 | = | 20.6 | nM | 7.69 |
| CHEMBL5555230 | — | EC50 | = | 24.52 | nM | 7.61 |
| CHEMBL5532569 | — | EC50 | = | 25.46 | nM | 7.59 |
| CHEMBL5542667 | — | EC50 | = | 35.96 | nM | 7.44 |
| CHEMBL5549854 | — | EC50 | = | 40.83 | nM | 7.39 |
| CHEMBL5556996 | — | EC50 | = | 43.4 | nM | 7.36 |
| CHEMBL5557979 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5559287 | — | EC50 | = | 119.0 | nM | 6.92 |
| CHEMBL5559296 | — | EC50 | = | 128.8 | nM | 6.89 |
| CHEMBL5557281 | — | EC50 | = | 330.8 | nM | 6.48 |
| CHEMBL5517885 | — | EC50 | = | 359.5 | nM | 6.44 |
| CHEMBL5555071 | — | EC50 | = | 498.2 | nM | 6.30 |
| CHEMBL5555720 | — | EC50 | = | 1037.0 | nM | 5.98 |
| CHEMBL5558635 | — | EC50 | = | 1089.0 | nM | 5.96 |
| CHEMBL5542308 | — | EC50 | = | 1675.0 | nM | 5.78 |
| CHEMBL5558745 | — | EC50 | = | 1925.0 | nM | 5.72 |
| CHEMBL5505794 | — | EC50 | = | 2541.0 | nM | 5.59 |
| CHEMBL5559107 | — | EC50 | = | 3592.0 | nM | 5.45 |
| CHEMBL5549748 | — | EC50 | = | 9896.0 | nM | 5.00 |
| CHEMBL5555121 | — | EC50 | = | 10610.0 | nM | 4.97 |
| CHEMBL5542676 | — | EC50 | = | 12920.0 | nM | 4.89 |
| CHEMBL5523573 | — | EC50 | = | 19960.0 | nM | 4.70 |
| CHEMBL5558784 | — | EC50 | = | 27220.0 | nM | 4.57 |
| CHEMBL5559021 | — | EC50 | = | 31460.0 | nM | 4.50 |
| CHEMBL5557467 | — | Activity | - | — | - |