Assay Detail
Binding
CHEMBL1646312
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Inhibition of IKK2
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Inhibitor of nuclear factor kappa-B kinase subunit beta (CHEMBL1991) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.47 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL521643 | — | — | 1 | 8.22 |
| CHEMBL1642545 | — | — | 1 | 8.22 |
| CHEMBL1642549 | — | — | 1 | 8.05 |
| CHEMBL1642564 | — | — | 1 | 8.00 |
| CHEMBL1642547 | — | — | 1 | 7.89 |
| CHEMBL1642559 | — | — | 1 | 7.80 |
| CHEMBL1642546 | — | — | 1 | 7.72 |
| CHEMBL1642565 | — | — | 1 | 7.70 |
| CHEMBL454973 | — | — | 1 | 7.66 |
| CHEMBL1642560 | — | — | 1 | 7.57 |
| CHEMBL1642550 | — | — | 1 | 7.55 |
| CHEMBL1642558 | — | — | 1 | 7.47 |
| CHEMBL1642557 | — | — | 1 | 7.44 |
| CHEMBL1642561 | — | — | 1 | 7.41 |
| CHEMBL1642563 | — | — | 1 | 7.39 |
| CHEMBL1642552 | — | — | 1 | 7.31 |
| CHEMBL1642556 | — | — | 1 | 7.26 |
| CHEMBL1642551 | — | — | 1 | 7.24 |
| CHEMBL1642548 | — | — | 1 | 7.22 |
| CHEMBL1642562 | — | — | 1 | 7.11 |
| CHEMBL1642554 | — | — | 1 | 7.00 |
| CHEMBL1642553 | — | — | 1 | 6.89 |
| CHEMBL249697 | BMS-345541 | — | 1 | 6.70 |
| CHEMBL523189 | — | — | 1 | 6.55 |
| CHEMBL1642555 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL521643 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1642545 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1642549 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1642564 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1642547 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1642559 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1642546 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1642565 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL454973 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1642560 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1642550 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1642558 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1642557 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1642561 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL1642563 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL1642552 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL1642556 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL1642551 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL1642548 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1642562 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL1642554 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1642553 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL249697 | BMS-345541 | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL523189 | — | IC50 | = | 279.0 | nM | 6.55 |
| CHEMBL1642555 | — | IC50 | > | 500.0 | nM | - |