Assay Detail
Functional
CHEMBL4734695
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Anti-necroptotic activity in mouse L929 cells assessed as inhibition of TNFalpha/Z-VAD-fmk (TZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay
15
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | L929 |
| 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 | 5.88 | 6.21 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4800694 | — | — | 1 | 6.21 |
| CHEMBL4751151 | — | — | 1 | 6.21 |
| CHEMBL4764330 | — | — | 1 | 6.09 |
| CHEMBL4747957 | — | — | 2 | 6.07 |
| CHEMBL4786387 | — | — | 1 | 5.99 |
| CHEMBL1720855 | — | — | 1 | 5.84 |
| CHEMBL4756694 | — | — | 1 | 5.83 |
| CHEMBL3105688 | — | — | 1 | 5.38 |
| CHEMBL4303525 | OMAVELOXOLONE | 4.0 | 1 | 5.28 |
| CHEMBL1093059 | BARDOXOLONE | 2.0 | 1 | - |
| CHEMBL168 | OLEANOLIC_ACID | — | 1 | - |
| CHEMBL230128 | — | — | 1 | - |
| CHEMBL1762621 | BARDOXOLONE METHYL | 3.0 | 1 | - |
| CHEMBL3582242 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4800694 | — | EC50 | = | 620.0 | nM | 6.21 |
| CHEMBL4751151 | — | EC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4764330 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4747957 | — | EC50 | = | 860.0 | nM | 6.07 |
| CHEMBL4786387 | — | EC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL1720855 | — | EC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL4756694 | — | EC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL3105688 | — | EC50 | = | 4150.0 | nM | 5.38 |
| CHEMBL4303525 | OMAVELOXOLONE | EC50 | = | 5250.0 | nM | 5.28 |
| CHEMBL1093059 | BARDOXOLONE | EC50 | > | 10000.0 | nM | - |
| CHEMBL168 | OLEANOLIC_ACID | EC50 | - | — | - | |
| CHEMBL230128 | — | EC50 | - | — | - | |
| CHEMBL1762621 | BARDOXOLONE METHYL | EC50 | > | 10000.0 | nM | - |
| CHEMBL3582242 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4747957 | — | Inhibition | - | % | - |