Assay Detail
Binding
CHEMBL1780647
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Inhibition of MK2 in LPS-stimulated human THP1 cells assessed as inhibition of Hsp27 phosphorylation pretreated 60 mins before LPS challenge measured after 10 mins
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
MAP kinase-activated protein kinase 2 (CHEMBL2208) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 5.85 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1779485 | — | — | 1 | 6.40 |
| CHEMBL1779372 | — | — | 1 | 6.30 |
| CHEMBL1738702 | — | — | 1 | 6.21 |
| CHEMBL1779370 | — | — | 1 | 6.05 |
| CHEMBL1779369 | — | — | 1 | 6.03 |
| CHEMBL1779374 | — | — | 1 | 5.96 |
| CHEMBL1779352 | — | — | 1 | 5.92 |
| CHEMBL1779488 | — | — | 1 | 5.92 |
| CHEMBL1779371 | — | — | 1 | 5.85 |
| CHEMBL1779353 | — | — | 1 | 5.80 |
| CHEMBL1779487 | — | — | 1 | 5.68 |
| CHEMBL1779375 | — | — | 1 | 5.64 |
| CHEMBL226471 | — | — | 1 | 5.57 |
| CHEMBL1779489 | — | — | 1 | 5.24 |
| CHEMBL1779373 | — | — | 1 | 5.11 |
| CHEMBL1779354 | — | — | 1 | - |
| CHEMBL1779351 | — | — | 1 | - |
| CHEMBL1779486 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1779485 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1779372 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1738702 | — | EC50 | = | 620.0 | nM | 6.21 |
| CHEMBL1779370 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL1779369 | — | EC50 | = | 930.0 | nM | 6.03 |
| CHEMBL1779374 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1779352 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1779488 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1779371 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1779353 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1779487 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL1779375 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL226471 | — | EC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1779489 | — | EC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL1779373 | — | EC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL1779354 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1779351 | — | EC50 | - | — | - | |
| CHEMBL1779486 | — | EC50 | > | 10000.0 | nM | - |