Assay Detail
Binding
CHEMBL960916
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IKK2-mediated phosphorylation of GST-IkappaBalpha fusion protein afterr 60 mins by fluorescence polarization assay
32
Total Activities
32
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 beta (CHEMBL1991) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel tricyclic inhibitors of IkappaB kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.20 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL493974 | — | — | 1 | 8.30 |
| CHEMBL521643 | — | — | 1 | 8.22 |
| CHEMBL493940 | — | — | 1 | 7.96 |
| CHEMBL492755 | — | — | 1 | 7.82 |
| CHEMBL492527 | — | — | 1 | 7.82 |
| CHEMBL504727 | — | — | 1 | 7.82 |
| CHEMBL522014 | — | — | 1 | 7.80 |
| CHEMBL249901 | — | — | 1 | 7.72 |
| CHEMBL454973 | — | — | 1 | 7.66 |
| CHEMBL494162 | — | — | 1 | 7.60 |
| CHEMBL538910 | — | — | 1 | 7.58 |
| CHEMBL505943 | — | — | 1 | 7.55 |
| CHEMBL494154 | — | — | 1 | 7.50 |
| CHEMBL523692 | — | — | 1 | 7.48 |
| CHEMBL492331 | — | — | 1 | 7.48 |
| CHEMBL493745 | — | — | 1 | 7.47 |
| CHEMBL493161 | — | — | 1 | 7.41 |
| CHEMBL494153 | — | — | 1 | 7.28 |
| CHEMBL521679 | — | — | 1 | 7.25 |
| CHEMBL450835 | — | — | 1 | 7.12 |
| CHEMBL447603 | — | — | 1 | 7.09 |
| CHEMBL522318 | — | — | 1 | 6.89 |
| CHEMBL492754 | — | — | 1 | 6.80 |
| CHEMBL522331 | — | — | 1 | 6.75 |
| CHEMBL492332 | — | — | 1 | 6.68 |
| CHEMBL523189 | — | — | 1 | 6.55 |
| CHEMBL506895 | — | — | 1 | 6.52 |
| CHEMBL249697 | BMS-345541 | — | 1 | 6.52 |
| CHEMBL522011 | — | — | 1 | 6.28 |
| CHEMBL454470 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL493974 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL521643 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL493940 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL492755 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL492527 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL504727 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL522014 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL249901 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL454973 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL494162 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL538910 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL505943 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL494154 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL523692 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL492331 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL493745 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL493161 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL494153 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL521679 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL450835 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL447603 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL522318 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL492754 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL522331 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL492332 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL523189 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL506895 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL249697 | BMS-345541 | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL522011 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL454470 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL522171 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL523002 | — | IC50 | = | 2500.0 | nM | 5.60 |