Assay Detail
Binding
CHEMBL855706
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Inhibition of Tpl2 kinase by ELISA
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 TNFalpha production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.53 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL219682 | — | — | 1 | 8.52 |
| CHEMBL221221 | — | — | 1 | 8.52 |
| CHEMBL219628 | — | — | 1 | 7.85 |
| CHEMBL220037 | — | — | 1 | 7.72 |
| CHEMBL221269 | — | — | 1 | 7.51 |
| CHEMBL221005 | — | — | 1 | 7.22 |
| CHEMBL220233 | — | — | 1 | 7.13 |
| CHEMBL374482 | — | — | 1 | 7.05 |
| CHEMBL221274 | — | — | 1 | 7.00 |
| CHEMBL223011 | — | — | 1 | 6.96 |
| CHEMBL222666 | — | — | 1 | 6.96 |
| CHEMBL376501 | — | — | 1 | 6.89 |
| CHEMBL200247 | — | — | 1 | 6.85 |
| CHEMBL222954 | — | — | 1 | 6.85 |
| CHEMBL426924 | — | — | 1 | 6.75 |
| CHEMBL375813 | — | — | 1 | 6.70 |
| CHEMBL373480 | — | — | 1 | 6.68 |
| CHEMBL222467 | — | — | 1 | 6.62 |
| CHEMBL223088 | — | — | 1 | 6.58 |
| CHEMBL374241 | — | — | 1 | 6.19 |
| CHEMBL221330 | — | — | 1 | 6.00 |
| CHEMBL197538 | — | — | 1 | 5.92 |
| CHEMBL374071 | — | — | 1 | 5.66 |
| CHEMBL426886 | — | — | 1 | 5.16 |
| CHEMBL223877 | — | — | 1 | 5.04 |
| CHEMBL376288 | — | — | 1 | 4.96 |
| CHEMBL374852 | — | — | 1 | 4.94 |
| CHEMBL223587 | — | — | 1 | 4.72 |
| CHEMBL220685 | — | — | 1 | 4.52 |
| CHEMBL222882 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL219682 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL221221 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL219628 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL220037 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL221269 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL221005 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL220233 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL374482 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL221274 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL223011 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL222666 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL376501 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL200247 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL222954 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL426924 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL375813 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL373480 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL222467 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL223088 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL374241 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL221330 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL197538 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL374071 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL426886 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL223877 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL376288 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL374852 | — | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL223587 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL220685 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL374210 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL222202 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL222468 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL374785 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL374258 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL222829 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL373557 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL221006 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL222882 | — | IC50 | > | 40000.0 | nM | - |