Assay Detail
Functional
CHEMBL885084
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory activity against lipopolysaccharide-stimulated release of tumor necrosis factor alpha from human monocytic THP-1 cells
29
Total Activities
29
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 | Expert |
Publication
Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.10 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL197912 | — | — | 1 | 8.29 |
| CHEMBL199160 | — | — | 1 | 8.21 |
| CHEMBL197581 | — | — | 1 | 7.89 |
| CHEMBL194201 | — | — | 1 | 7.72 |
| CHEMBL196576 | — | — | 1 | 7.55 |
| CHEMBL383569 | — | — | 1 | 7.48 |
| CHEMBL197545 | — | — | 1 | 7.43 |
| CHEMBL196575 | — | — | 1 | 7.38 |
| CHEMBL382103 | — | — | 1 | 7.37 |
| CHEMBL363648 | TAK-715 | 2.0 | 1 | 7.32 |
| CHEMBL195942 | — | — | 1 | 7.31 |
| CHEMBL197799 | — | — | 1 | 7.21 |
| CHEMBL371716 | — | — | 1 | 7.16 |
| CHEMBL198334 | — | — | 1 | 7.14 |
| CHEMBL198383 | — | — | 1 | 7.11 |
| CHEMBL425909 | — | — | 1 | 7.03 |
| CHEMBL369936 | — | — | 1 | 6.96 |
| CHEMBL371188 | — | — | 1 | 6.96 |
| CHEMBL381864 | — | — | 1 | 6.92 |
| CHEMBL197753 | — | — | 1 | 6.89 |
| CHEMBL194595 | — | — | 1 | 6.89 |
| CHEMBL198323 | — | — | 1 | 6.89 |
| CHEMBL197983 | — | — | 1 | 6.89 |
| CHEMBL196386 | — | — | 1 | 6.66 |
| CHEMBL364441 | — | — | 1 | 6.36 |
| CHEMBL196247 | — | — | 1 | 6.35 |
| CHEMBL371209 | — | — | 1 | 6.35 |
| CHEMBL197517 | — | — | 1 | 6.16 |
| CHEMBL197776 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL197912 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL199160 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL197581 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL194201 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL196576 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL383569 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL197545 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL196575 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL382103 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL363648 | TAK-715 | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL195942 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL197799 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL371716 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL198334 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL198383 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL425909 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL369936 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL371188 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL381864 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL197753 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL194595 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL198323 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL197983 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL196386 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL364441 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL196247 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL371209 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL197517 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL197776 | — | IC50 | = | 890.0 | nM | 6.05 |