Assay Detail
Binding
CHEMBL888322
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Inhibition of IKKalpha
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 alpha (CHEMBL3476) ↗| 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 | 5.88 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL249481 | — | — | 1 | 6.89 |
| CHEMBL249280 | — | — | 1 | 6.77 |
| CHEMBL249887 | — | — | 1 | 6.72 |
| CHEMBL400077 | — | — | 1 | 6.66 |
| CHEMBL399689 | — | — | 1 | 6.58 |
| CHEMBL400078 | — | — | 1 | 6.58 |
| CHEMBL399368 | — | — | 1 | 6.48 |
| CHEMBL398253 | — | — | 1 | 6.41 |
| CHEMBL249899 | — | — | 1 | 6.38 |
| CHEMBL249482 | — | — | 1 | 6.36 |
| CHEMBL249104 | — | — | 1 | 6.35 |
| CHEMBL428754 | — | — | 1 | 6.29 |
| CHEMBL437586 | — | — | 1 | 6.19 |
| CHEMBL399486 | — | — | 1 | 6.17 |
| CHEMBL249102 | — | — | 1 | 6.16 |
| CHEMBL249279 | — | — | 1 | 6.11 |
| CHEMBL249480 | — | — | 1 | 6.09 |
| CHEMBL249515 | — | — | 1 | 6.04 |
| CHEMBL249901 | — | — | 1 | 6.04 |
| CHEMBL249902 | — | — | 1 | 6.03 |
| CHEMBL251724 | — | — | 1 | 6.00 |
| CHEMBL249681 | — | — | 1 | 5.97 |
| CHEMBL398511 | — | — | 1 | 5.96 |
| CHEMBL249719 | — | — | 1 | 5.96 |
| CHEMBL249721 | — | — | 1 | 5.93 |
| CHEMBL399688 | — | — | 1 | 5.92 |
| CHEMBL398513 | — | — | 1 | 5.91 |
| CHEMBL250105 | — | — | 1 | 5.90 |
| CHEMBL249886 | — | — | 1 | 5.90 |
| CHEMBL249683 | — | — | 1 | 5.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL249481 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL249280 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL249887 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL400077 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL399689 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL400078 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL399368 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL398253 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL249899 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL249482 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL249104 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL428754 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL437586 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL399486 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL249102 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL249279 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL249480 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL249515 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL249901 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL249902 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL251724 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL249681 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL398511 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL249719 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL249721 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL399688 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL398513 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL250105 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL249886 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL249683 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL250106 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL249720 | — | IC50 | = | 1990.0 | nM | 5.70 |
| CHEMBL249508 | — | IC50 | = | 2330.0 | nM | 5.63 |
| CHEMBL250107 | — | IC50 | = | 2570.0 | nM | 5.59 |
| CHEMBL249103 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL398514 | — | IC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL250336 | — | IC50 | = | 3130.0 | nM | 5.50 |
| CHEMBL250337 | — | IC50 | = | 3480.0 | nM | 5.46 |
| CHEMBL398512 | — | IC50 | = | 3860.0 | nM | 5.41 |
| CHEMBL250539 | — | IC50 | = | 4120.0 | nM | 5.38 |
| CHEMBL400389 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL399383 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL250335 | — | IC50 | = | 7030.0 | nM | 5.15 |
| CHEMBL249697 | BMS-345541 | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL249073 | — | IC50 | = | 7830.0 | nM | 5.11 |
| CHEMBL250131 | — | IC50 | = | 7990.0 | nM | 5.10 |
| CHEMBL249900 | — | IC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL248899 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL401301 | — | IC50 | = | 14400.0 | nM | 4.84 |
| CHEMBL249682 | — | IC50 | > | 30000.0 | nM | - |