Assay Detail
Functional
CHEMBL4734690
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Anti-necroptotic activity in human HT-29 cells assessed as inhibition of TNFalpha/SM-164/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay
16
Total Activities
14
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
Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 5.87 | 6.54 |
| Inhibition | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4751151 | — | — | 1 | 6.54 |
| CHEMBL4747957 | — | — | 2 | 6.51 |
| CHEMBL1093059 | BARDOXOLONE | 2.0 | 2 | 5.89 |
| CHEMBL3582242 | — | — | 1 | 5.89 |
| CHEMBL3105688 | — | — | 1 | 5.86 |
| CHEMBL4303525 | OMAVELOXOLONE | 4.0 | 1 | 5.85 |
| CHEMBL4786387 | — | — | 1 | 5.79 |
| CHEMBL4800694 | — | — | 1 | 5.74 |
| CHEMBL4764330 | — | — | 1 | 5.72 |
| CHEMBL1720855 | — | — | 1 | 5.68 |
| CHEMBL4756694 | — | — | 1 | 5.55 |
| CHEMBL1762621 | BARDOXOLONE METHYL | 3.0 | 1 | 5.36 |
| CHEMBL168 | OLEANOLIC_ACID | — | 1 | - |
| CHEMBL230128 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4751151 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4747957 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1093059 | BARDOXOLONE | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3582242 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3105688 | — | EC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL4303525 | OMAVELOXOLONE | EC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL4786387 | — | EC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL4800694 | — | EC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL4764330 | — | EC50 | = | 1910.0 | nM | 5.72 |
| CHEMBL1720855 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4756694 | — | EC50 | = | 2810.0 | nM | 5.55 |
| CHEMBL1762621 | BARDOXOLONE METHYL | EC50 | = | 4340.0 | nM | 5.36 |
| CHEMBL1093059 | BARDOXOLONE | Inhibition | - | % | - | |
| CHEMBL168 | OLEANOLIC_ACID | EC50 | > | 10000.0 | nM | - |
| CHEMBL230128 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4747957 | — | Inhibition | - | % | - |