Assay Detail
Binding
CHEMBL1025323
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IKK1-catalyzed phosphorylation of GST-tagged IkappaBalpha fusion protein by fluorescence polarization assay
16
Total Activities
16
Compounds Tested
1
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 alpha (CHEMBL3476) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.34 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL549478 | — | — | 1 | 8.15 |
| CHEMBL558491 | — | — | 1 | 8.15 |
| CHEMBL551773 | — | — | 1 | 8.10 |
| CHEMBL562720 | — | — | 1 | 7.96 |
| CHEMBL562971 | — | — | 1 | 7.92 |
| CHEMBL552183 | — | — | 1 | 7.85 |
| CHEMBL562370 | — | — | 1 | 7.66 |
| CHEMBL561447 | — | — | 1 | 7.60 |
| CHEMBL560708 | — | — | 1 | 7.41 |
| CHEMBL565076 | — | — | 1 | 7.40 |
| CHEMBL549479 | — | — | 1 | 7.37 |
| CHEMBL556806 | — | — | 1 | 7.36 |
| CHEMBL563554 | — | — | 1 | 7.10 |
| CHEMBL493940 | — | — | 1 | 6.57 |
| CHEMBL521643 | — | — | 1 | 5.46 |
| CHEMBL522011 | — | — | 1 | 5.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL549478 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL558491 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL551773 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL562720 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL562971 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL552183 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL562370 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL561447 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL560708 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL565076 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL549479 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL556806 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL563554 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL493940 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL521643 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL522011 | — | IC50 | = | 4280.0 | nM | 5.37 |