Assay Detail
Binding
CHEMBL4220320
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Inhibition of MAPK p38 in human THP1 cells assessed as reduction in LPS-induced TNFalpha production preincubated for 60 mins followed by LPS addition measured after 4 hrs by HTRF assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Intermediate |
Publication
Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.36 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4227523 | — | — | 1 | 8.92 |
| CHEMBL4229137 | — | — | 1 | 8.46 |
| CHEMBL4226320 | — | — | 1 | 7.89 |
| CHEMBL4225003 | — | — | 1 | 7.85 |
| CHEMBL4225173 | — | — | 1 | 7.82 |
| CHEMBL4225133 | — | — | 1 | 7.80 |
| CHEMBL4227050 | — | — | 1 | 7.80 |
| CHEMBL4224940 | — | — | 1 | 7.75 |
| CHEMBL4227582 | — | — | 1 | 7.75 |
| CHEMBL4226563 | — | — | 1 | 7.72 |
| CHEMBL4228109 | — | — | 1 | 7.28 |
| CHEMBL4226206 | — | — | 1 | 7.24 |
| CHEMBL4226302 | — | — | 1 | 7.06 |
| CHEMBL4225547 | — | — | 1 | 6.89 |
| CHEMBL363648 | TAK-715 | 2.0 | 1 | 6.62 |
| CHEMBL4225809 | — | — | 1 | 6.58 |
| CHEMBL4226784 | — | — | 1 | 6.44 |
| CHEMBL4227689 | — | — | 1 | 6.00 |
| CHEMBL4226464 | — | — | 1 | 5.89 |
| CHEMBL4225487 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4227523 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4229137 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4226320 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4225003 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4225173 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4225133 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4227050 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4224940 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4227582 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4226563 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4228109 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4226206 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4226302 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4225547 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL363648 | TAK-715 | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4225809 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4226784 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4227689 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4226464 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4225487 | — | IC50 | > | 10000.0 | nM | - |