Assay Detail
Functional
CHEMBL856248
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration required to inhibit LPS-induced TNFalpha production in human peripheral blood mononuclear cells; n=3
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | PBMC |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
5-Cyanopyrimidine derivatives as a novel class of potent, selective, and orally active inhibitors of p38alpha MAP kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 4.97 | 6.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL196741 | — | — | 1 | 6.48 |
| CHEMBL197351 | — | — | 1 | 5.82 |
| CHEMBL383172 | — | — | 1 | 5.46 |
| CHEMBL274257 | — | — | 1 | 5.39 |
| CHEMBL382954 | — | — | 1 | 5.34 |
| CHEMBL198876 | — | — | 1 | 5.06 |
| CHEMBL363643 | — | — | 1 | 4.77 |
| CHEMBL197206 | — | — | 1 | 4.75 |
| CHEMBL198872 | — | — | 1 | 4.68 |
| CHEMBL195532 | — | — | 1 | 4.38 |
| CHEMBL194813 | — | — | 1 | 4.19 |
| CHEMBL370783 | — | — | 1 | 4.17 |
| CHEMBL198456 | — | — | 1 | 4.14 |
| CHEMBL196230 | — | — | 1 | - |
| CHEMBL198198 | — | — | 1 | - |
| CHEMBL383137 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL196741 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL197351 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL383172 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL274257 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL382954 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL198876 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL363643 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL197206 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL198872 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL195532 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL194813 | — | IC50 | = | 64000.0 | nM | 4.19 |
| CHEMBL370783 | — | IC50 | = | 67000.0 | nM | 4.17 |
| CHEMBL198456 | — | IC50 | = | 72000.0 | nM | 4.14 |
| CHEMBL196230 | — | IC50 | = | 130000.0 | nM | - |
| CHEMBL198198 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL383137 | — | IC50 | = | 158000.0 | nM | - |