Assay Detail
Binding
CHEMBL888323
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Inhibition of IKK-beta
52
Total Activities
52
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
Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 52 | 7.20 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL249280 | — | — | 1 | 8.52 |
| CHEMBL249482 | — | — | 1 | 8.15 |
| CHEMBL249104 | — | — | 1 | 8.10 |
| CHEMBL399486 | — | — | 1 | 8.10 |
| CHEMBL400077 | — | — | 1 | 8.07 |
| CHEMBL250106 | — | — | 1 | 8.00 |
| CHEMBL249886 | — | — | 1 | 7.89 |
| CHEMBL398253 | — | — | 1 | 7.89 |
| CHEMBL399689 | — | — | 1 | 7.85 |
| CHEMBL249481 | — | — | 1 | 7.75 |
| CHEMBL399688 | — | — | 1 | 7.72 |
| CHEMBL249515 | — | — | 1 | 7.68 |
| CHEMBL249480 | — | — | 1 | 7.68 |
| CHEMBL249901 | — | — | 1 | 7.66 |
| CHEMBL249899 | — | — | 1 | 7.64 |
| CHEMBL428754 | — | — | 1 | 7.64 |
| CHEMBL249508 | — | — | 1 | 7.64 |
| CHEMBL249887 | — | — | 1 | 7.57 |
| CHEMBL249719 | — | — | 1 | 7.57 |
| CHEMBL249902 | — | — | 1 | 7.54 |
| CHEMBL399368 | — | — | 1 | 7.44 |
| CHEMBL250336 | — | — | 1 | 7.40 |
| CHEMBL400078 | — | — | 1 | 7.37 |
| CHEMBL249102 | — | — | 1 | 7.36 |
| CHEMBL437586 | — | — | 1 | 7.35 |
| CHEMBL249681 | — | — | 1 | 7.29 |
| CHEMBL250337 | — | — | 1 | 7.07 |
| CHEMBL249721 | — | — | 1 | 7.02 |
| CHEMBL249103 | — | — | 1 | 7.02 |
| CHEMBL400389 | — | — | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL249280 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL249482 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL399486 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL249104 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL400077 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL250106 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL249886 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL398253 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL399689 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL249481 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL399688 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL249515 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL249480 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL249901 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL249508 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL428754 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL249899 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL249887 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL249719 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL249902 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL399368 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL250336 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL400078 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL249102 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL437586 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL249681 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL250337 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL249721 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL249103 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL400389 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL250107 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL249697 | BMS-345541 | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL249900 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL398513 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL401301 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL250131 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL398511 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL250105 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL249720 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL398514 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL248899 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL250335 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL249682 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL249929 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL399383 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL249279 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL398512 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL249073 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL250539 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL251724 | — | IC50 | = | 590.0 | nM | 6.23 |