Assay Detail
Binding
CHEMBL1000656
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Inhibition of Tpl2 kinase by ELISA
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Mitogen-activated protein kinase kinase kinase 8 (CHEMBL4899) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Selective inhibitors of tumor progression loci-2 (Tpl2) kinase with potent inhibition of TNF-alpha production in human whole blood.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.68 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL527026 | — | — | 1 | 8.80 |
| CHEMBL498071 | — | — | 1 | 8.70 |
| CHEMBL498029 | — | — | 1 | 8.66 |
| CHEMBL482863 | — | — | 1 | 8.52 |
| CHEMBL498070 | — | — | 1 | 8.40 |
| CHEMBL498028 | — | — | 1 | 8.28 |
| CHEMBL495867 | — | — | 1 | 8.15 |
| CHEMBL498072 | — | — | 1 | 8.12 |
| CHEMBL496595 | — | — | 1 | 8.10 |
| CHEMBL495617 | — | — | 1 | 8.09 |
| CHEMBL523059 | — | — | 1 | 8.04 |
| CHEMBL495584 | — | — | 1 | 8.02 |
| CHEMBL501709 | — | — | 1 | 8.00 |
| CHEMBL498222 | — | — | 1 | 8.00 |
| CHEMBL483685 | — | — | 1 | 7.89 |
| CHEMBL482864 | — | — | 1 | 7.77 |
| CHEMBL499853 | — | — | 1 | 7.75 |
| CHEMBL230232 | — | — | 1 | 7.75 |
| CHEMBL220037 | — | — | 1 | 7.72 |
| CHEMBL524638 | — | — | 1 | 7.70 |
| CHEMBL483484 | — | — | 1 | 7.70 |
| CHEMBL497228 | — | — | 1 | 7.66 |
| CHEMBL524069 | — | — | 1 | 7.66 |
| CHEMBL497883 | — | — | 1 | 7.64 |
| CHEMBL496594 | — | — | 1 | 7.55 |
| CHEMBL230761 | — | — | 1 | 7.52 |
| CHEMBL496388 | — | — | 1 | 7.40 |
| CHEMBL495585 | — | — | 1 | 7.40 |
| CHEMBL495866 | — | — | 1 | 7.21 |
| CHEMBL496591 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL527026 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL498071 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL498029 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL482863 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL498070 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL498028 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL495867 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL498072 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL496595 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL495617 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL523059 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL495584 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL501709 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL498222 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL483685 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL482864 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL230232 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL499853 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL220037 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL524638 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL483484 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL497228 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL524069 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL497883 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL496594 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL230761 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL496388 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL495585 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL495866 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL496591 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL526840 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL496590 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL197538 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL522217 | — | IC50 | = | 40000.0 | nM | 4.40 |