Assay Detail
Functional
CHEMBL860389
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against human Tpl2 kinase via quantification of MEK phosphorylation
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Mitogen-activated protein kinase kinase kinase 8 (CHEMBL4899) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.16 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL371658 | — | — | 1 | 8.70 |
| CHEMBL199210 | — | — | 1 | 8.22 |
| CHEMBL199230 | — | — | 1 | 7.92 |
| CHEMBL200381 | — | — | 1 | 7.30 |
| CHEMBL200247 | — | — | 1 | 7.14 |
| CHEMBL371095 | — | — | 1 | 6.42 |
| CHEMBL197382 | — | — | 1 | 6.38 |
| CHEMBL197538 | — | — | 1 | 5.92 |
| CHEMBL196919 | — | — | 1 | 5.75 |
| CHEMBL198581 | — | — | 1 | 5.47 |
| CHEMBL425213 | — | — | 1 | 5.45 |
| CHEMBL198905 | — | — | 1 | 5.38 |
| CHEMBL196918 | — | — | 1 | 5.34 |
| CHEMBL197164 | — | — | 1 | 5.00 |
| CHEMBL197006 | — | — | 1 | 5.00 |
| CHEMBL370655 | — | — | 1 | 4.68 |
| CHEMBL370336 | — | — | 1 | 4.57 |
| CHEMBL196771 | — | — | 1 | - |
| CHEMBL198904 | — | — | 1 | - |
| CHEMBL196959 | — | — | 1 | - |
| CHEMBL198577 | — | — | 1 | - |
| CHEMBL371532 | — | — | 1 | - |
| CHEMBL198739 | — | — | 1 | - |
| CHEMBL198647 | — | — | 1 | - |
| CHEMBL199000 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL371658 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL199210 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL199230 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL200381 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL200247 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL371095 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL197382 | — | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL197538 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL196919 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL198581 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL425213 | — | IC50 | = | 3565.0 | nM | 5.45 |
| CHEMBL198905 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL196918 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL197164 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL197006 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL370655 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL370336 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL196771 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL198904 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL196959 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL198577 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL371532 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL198739 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL198647 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL199000 | — | IC50 | > | 40000.0 | nM | - |