Assay Detail
Functional
CHEMBL4842515
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Anti-necroptotic activity in human HT-29 cells assessed as inhibition of hTNFalpha/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 8 to 10 hrs by celltiter-glo luminescent cell viability assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HT-29 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Structure-based bioisosterism design of thio-benzoxazepinones as novel necroptosis inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 27 | 6.72 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4871408 | — | — | 1 | 8.55 |
| CHEMBL4071864 | GSK2982772 | 2.0 | 1 | 8.44 |
| CHEMBL4850691 | — | — | 1 | 8.13 |
| CHEMBL4866295 | — | — | 1 | 7.86 |
| CHEMBL4861471 | ECLITASERTIB | 2.0 | 1 | 7.81 |
| CHEMBL4866261 | — | — | 1 | 7.73 |
| CHEMBL4872011 | — | — | 1 | 7.65 |
| CHEMBL4848275 | — | — | 1 | 7.12 |
| CHEMBL4874864 | — | — | 1 | 6.91 |
| CHEMBL4860261 | — | — | 1 | 6.84 |
| CHEMBL4849815 | — | — | 1 | 6.67 |
| CHEMBL4874139 | — | — | 1 | 6.61 |
| CHEMBL4090420 | — | — | 1 | 6.55 |
| CHEMBL4872802 | — | — | 1 | 6.44 |
| CHEMBL4861390 | — | — | 1 | 6.13 |
| CHEMBL4853355 | — | — | 1 | 6.09 |
| CHEMBL4865111 | — | — | 1 | 5.82 |
| CHEMBL4863402 | — | — | 1 | 5.70 |
| CHEMBL4869067 | — | — | 1 | 5.47 |
| CHEMBL4873040 | — | — | 1 | 5.19 |
| CHEMBL4864822 | — | — | 1 | 5.17 |
| CHEMBL4854997 | — | — | 1 | 5.05 |
| CHEMBL4871037 | — | — | 1 | - |
| CHEMBL4855090 | — | — | 1 | - |
| CHEMBL4870503 | — | — | 1 | - |
| CHEMBL4847972 | — | — | 1 | - |
| CHEMBL4859911 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4871408 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4071864 | GSK2982772 | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4850691 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4866295 | — | EC50 | = | 13.7 | nM | 7.86 |
| CHEMBL4861471 | ECLITASERTIB | EC50 | = | 15.4 | nM | 7.81 |
| CHEMBL4866261 | — | EC50 | = | 18.6 | nM | 7.73 |
| CHEMBL4872011 | — | EC50 | = | 22.6 | nM | 7.65 |
| CHEMBL4848275 | — | EC50 | = | 76.3 | nM | 7.12 |
| CHEMBL4874864 | — | EC50 | = | 121.8 | nM | 6.91 |
| CHEMBL4860261 | — | EC50 | = | 143.8 | nM | 6.84 |
| CHEMBL4849815 | — | EC50 | = | 211.2 | nM | 6.67 |
| CHEMBL4874139 | — | EC50 | = | 243.0 | nM | 6.61 |
| CHEMBL4090420 | — | EC50 | = | 279.2 | nM | 6.55 |
| CHEMBL4872802 | — | EC50 | = | 363.0 | nM | 6.44 |
| CHEMBL4861390 | — | EC50 | = | 735.6 | nM | 6.13 |
| CHEMBL4853355 | — | EC50 | = | 810.5 | nM | 6.09 |
| CHEMBL4865111 | — | EC50 | = | 1513.0 | nM | 5.82 |
| CHEMBL4863402 | — | EC50 | = | 2017.5 | nM | 5.70 |
| CHEMBL4869067 | — | EC50 | = | 3402.5 | nM | 5.47 |
| CHEMBL4873040 | — | EC50 | = | 6496.0 | nM | 5.19 |
| CHEMBL4864822 | — | EC50 | = | 6677.0 | nM | 5.17 |
| CHEMBL4854997 | — | EC50 | = | 8837.0 | nM | 5.05 |
| CHEMBL4871037 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4855090 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4870503 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4847972 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4859911 | — | EC50 | > | 10000.0 | nM | - |