Assay Detail
Functional
CHEMBL2172921
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production after 20 hrs
14
Total Activities
14
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
Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.60 | 9.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2170284 | — | — | 1 | 9.43 |
| CHEMBL2170297 | — | — | 1 | 9.34 |
| CHEMBL2170294 | AS1940477 | — | 1 | 9.22 |
| CHEMBL2170292 | — | — | 1 | 9.07 |
| CHEMBL2170295 | — | — | 1 | 9.02 |
| CHEMBL2170290 | — | — | 1 | 9.00 |
| CHEMBL2170296 | — | — | 1 | 8.96 |
| CHEMBL2170288 | — | — | 1 | 8.96 |
| CHEMBL2170293 | — | — | 1 | 8.74 |
| CHEMBL2170287 | — | — | 1 | 8.22 |
| CHEMBL2170291 | — | — | 1 | 8.00 |
| CHEMBL2170286 | — | — | 1 | 7.85 |
| CHEMBL2170285 | — | — | 1 | 7.64 |
| CHEMBL2170289 | — | — | 1 | 6.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2170284 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL2170297 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL2170294 | AS1940477 | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL2170292 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL2170295 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL2170290 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2170296 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2170288 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2170293 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL2170287 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2170291 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2170286 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2170285 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2170289 | — | IC50 | = | 106.0 | nM | 6.97 |