Assay Detail
Functional
CHEMBL5165543
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Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells preincubated for 2 hrs followed by LPS treatment for 24 hrs by RT-qPCR analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | RAW264.7 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of First-in-Class TAK1-MKK3 Protein-Protein Interaction (PPI) Inhibitor <b>(<i>R</i>)-STU104</b> for the Treatment of Ulcerative Colitis through Modulating TNF-α Production.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.04 | 6.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5178905 | — | — | 1 | 6.24 |
| CHEMBL5206351 | — | — | 1 | 5.90 |
| CHEMBL5209411 | — | — | 1 | 5.45 |
| CHEMBL5203831 | — | — | 1 | 5.41 |
| CHEMBL5199979 | — | — | 1 | 5.40 |
| CHEMBL5200314 | — | — | 1 | 5.35 |
| CHEMBL5205909 | — | — | 1 | 4.36 |
| CHEMBL5206866 | — | — | 1 | 4.34 |
| CHEMBL5191781 | — | — | 1 | 4.33 |
| CHEMBL5209842 | — | — | 1 | 4.32 |
| CHEMBL5179422 | — | — | 1 | 4.29 |
| CHEMBL5173925 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5178905 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL5206351 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL5209411 | — | IC50 | = | 3520.0 | nM | 5.45 |
| CHEMBL5203831 | — | IC50 | = | 3920.0 | nM | 5.41 |
| CHEMBL5199979 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5200314 | — | IC50 | = | 4510.0 | nM | 5.35 |
| CHEMBL5205909 | — | IC50 | = | 43600.0 | nM | 4.36 |
| CHEMBL5206866 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL5191781 | — | IC50 | = | 47300.0 | nM | 4.33 |
| CHEMBL5209842 | — | IC50 | = | 48300.0 | nM | 4.32 |
| CHEMBL5179422 | — | IC50 | = | 51500.0 | nM | 4.29 |
| CHEMBL5173925 | — | IC50 | > | 50000.0 | nM | - |