Assay Detail
Binding
CHEMBL1014534
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Inhibition of IKK-beta by TR-FRET assay
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Inhibitor of nuclear factor kappa-B kinase subunit beta (CHEMBL1991) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
IKKbeta inhibitors identification part I: homology model assisted structure based virtual screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.12 | 8.10 |
| Ki | 1 | 8.70 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL516203 | — | — | 1 | 8.70 |
| CHEMBL474802 | — | — | 1 | 8.10 |
| CHEMBL129857 | AS-602868 | 1.0 | 1 | 8.10 |
| CHEMBL257167 | — | — | 1 | 7.75 |
| CHEMBL514980 | — | — | 1 | 7.40 |
| CHEMBL514334 | — | — | 1 | 7.16 |
| CHEMBL473619 | — | — | 1 | 6.50 |
| CHEMBL361862 | — | — | 1 | 6.17 |
| CHEMBL474389 | — | — | 1 | 5.75 |
| CHEMBL520813 | — | — | 1 | - |
| CHEMBL452967 | — | — | 1 | - |
| CHEMBL483617 | — | — | 1 | - |
| CHEMBL483816 | — | — | 1 | - |
| CHEMBL474783 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL516203 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL474802 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL129857 | AS-602868 | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL257167 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL514980 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL514334 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL473619 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL361862 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL474389 | — | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL520813 | — | IC50 | - | — | - | |
| CHEMBL452967 | — | IC50 | - | — | - | |
| CHEMBL483617 | — | IC50 | - | — | - | |
| CHEMBL483816 | — | IC50 | - | — | - | |
| CHEMBL474783 | — | IC50 | - | — | - |