Assay Detail
Binding
CHEMBL911347
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Inhibition of human recombinant IKKepsilon by TR-FRET assay
18
Total Activities
18
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
Inhibitor of nuclear factor kappa-B kinase subunit epsilon (CHEMBL3529) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-epsilon kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.95 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL220090 | — | — | 1 | 7.60 |
| CHEMBL373751 | GSK-319347A | — | 1 | 7.40 |
| CHEMBL222318 | — | — | 1 | 7.30 |
| CHEMBL374440 | — | — | 1 | 6.60 |
| CHEMBL375787 | — | — | 1 | 6.10 |
| CHEMBL221063 | — | — | 1 | 6.00 |
| CHEMBL376262 | — | — | 1 | 5.80 |
| CHEMBL219845 | — | — | 1 | 5.80 |
| CHEMBL219992 | — | — | 1 | 5.60 |
| CHEMBL375379 | — | — | 1 | 5.50 |
| CHEMBL220145 | — | — | 1 | 5.40 |
| CHEMBL223425 | — | — | 1 | 5.30 |
| CHEMBL219711 | — | — | 1 | 5.30 |
| CHEMBL375115 | — | — | 1 | 4.90 |
| CHEMBL222419 | GSK-237701A | — | 1 | 4.70 |
| CHEMBL219899 | — | — | 1 | - |
| CHEMBL220032 | — | — | 1 | - |
| CHEMBL222312 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL220090 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL373751 | GSK-319347A | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL222318 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL374440 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL375787 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL221063 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL376262 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL219845 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL219992 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL375379 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL220145 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL223425 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL219711 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL375115 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL222419 | GSK-237701A | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL219899 | — | IC50 | < | 15848.93 | nM | - |
| CHEMBL220032 | — | IC50 | < | 15848.93 | nM | - |
| CHEMBL222312 | — | IC50 | < | 15848.93 | nM | - |