Assay Detail
Functional
CHEMBL1228243
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Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production after 4 hrs by ELISA
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of imidazo[1,2-b]pyridazine derivatives as IKKbeta inhibitors. Part 1: Hit-to-lead study and structure-activity relationship.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 54 | 5.48 | 6.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1221431 | — | — | 1 | 6.31 |
| CHEMBL1223203 | — | — | 1 | 6.16 |
| CHEMBL1222990 | — | — | 1 | 6.16 |
| CHEMBL1223204 | — | — | 1 | 5.92 |
| CHEMBL1223355 | — | — | 1 | 5.89 |
| CHEMBL1223289 | — | — | 1 | 5.82 |
| CHEMBL1223206 | — | — | 1 | 5.82 |
| CHEMBL1223288 | — | — | 1 | 5.80 |
| CHEMBL1222928 | — | — | 1 | 5.77 |
| CHEMBL1222925 | — | — | 1 | 5.77 |
| CHEMBL1223287 | — | — | 1 | 5.68 |
| CHEMBL1223207 | — | — | 1 | 5.68 |
| CHEMBL1223564 | — | — | 1 | 5.62 |
| CHEMBL1223205 | — | — | 1 | 5.62 |
| CHEMBL1222992 | — | — | 1 | 5.57 |
| CHEMBL1222929 | — | — | 1 | 5.50 |
| CHEMBL1222991 | — | — | 1 | 5.43 |
| CHEMBL1222565 | — | — | 1 | 5.40 |
| CHEMBL1222638 | — | — | 1 | 5.36 |
| CHEMBL1222477 | — | — | 1 | 5.33 |
| CHEMBL1222563 | — | — | 1 | 5.19 |
| CHEMBL1222637 | — | — | 1 | 5.19 |
| CHEMBL1222789 | — | — | 1 | 4.92 |
| CHEMBL1222786 | — | — | 1 | 4.82 |
| CHEMBL1222635 | — | — | 1 | 4.77 |
| CHEMBL1223137 | — | — | 1 | 4.70 |
| CHEMBL1222854 | — | — | 1 | 4.57 |
| CHEMBL1222927 | — | — | 1 | 4.54 |
| CHEMBL1223139 | — | — | 1 | - |
| CHEMBL1223138 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1221431 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL1223203 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL1222990 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL1223204 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1223355 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1223289 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1223206 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1223288 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1222928 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1222925 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1223287 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL1223207 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL1223564 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1223205 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1222992 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1222929 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL1222991 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL1222565 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL1222638 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL1222477 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL1222563 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL1222637 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL1222789 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL1222786 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL1222635 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL1223137 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL1222854 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL1222927 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL1222788 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1222851 | — | IC50 | - | — | - | |
| CHEMBL1222852 | — | IC50 | - | — | - | |
| CHEMBL1222853 | — | IC50 | - | — | - | |
| CHEMBL1222926 | — | IC50 | - | — | - | |
| CHEMBL1222636 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1222705 | — | IC50 | - | — | - | |
| CHEMBL1223060 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1223061 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1223062 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1223063 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL588573 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1222474 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1222475 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1222476 | — | IC50 | - | — | - | |
| CHEMBL1223286 | — | IC50 | - | — | - | |
| CHEMBL1221423 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1222564 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1223136 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1222993 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1223138 | — | IC50 | - | — | - | |
| CHEMBL1223139 | — | IC50 | - | — | - |