Assay Detail
Functional
CHEMBL1114702
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Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production by PLAP reporter assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.83 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1099077 | — | — | 1 | 7.64 |
| CHEMBL1096417 | — | — | 1 | 7.58 |
| CHEMBL1098080 | — | — | 1 | 7.37 |
| CHEMBL1097999 | E-6201 | 2.0 | 1 | 7.25 |
| CHEMBL1097699 | — | — | 1 | 7.15 |
| CHEMBL1097700 | — | — | 1 | 7.07 |
| CHEMBL1097280 | — | — | 1 | 6.97 |
| CHEMBL1097698 | — | — | 1 | 6.89 |
| CHEMBL1096741 | — | — | 1 | 6.46 |
| CHEMBL1097653 | — | — | 1 | 6.44 |
| CHEMBL1096740 | — | — | 1 | 6.36 |
| CHEMBL1097413 | — | — | 1 | 5.90 |
| CHEMBL1098081 | — | — | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1099077 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1096417 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1098080 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1097999 | E-6201 | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL1097699 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL1097700 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL1097280 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL1097698 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL1096741 | — | IC50 | = | 351.0 | nM | 6.46 |
| CHEMBL1097653 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL1096740 | — | IC50 | = | 437.0 | nM | 6.36 |
| CHEMBL1097413 | — | IC50 | = | 1251.0 | nM | 5.90 |
| CHEMBL1098081 | — | IC50 | = | 2066.0 | nM | 5.68 |