Assay Detail
Functional
CHEMBL1780648
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Antiinflammatory activity in human PBMC cells assessed as inhibition of LPS-induced TNFalpha production pretreated 30 mins before LPS challenge measured after 4 hrs by ELISA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | PBMC |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 5.83 | 6.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1779485 | — | — | 1 | 6.37 |
| CHEMBL1779372 | — | — | 1 | 6.35 |
| CHEMBL1779371 | — | — | 1 | 6.04 |
| CHEMBL1779488 | — | — | 1 | 6.03 |
| CHEMBL1779370 | — | — | 1 | 6.00 |
| CHEMBL1779369 | — | — | 1 | 5.96 |
| CHEMBL1779374 | — | — | 1 | 5.89 |
| CHEMBL1779373 | — | — | 1 | 5.52 |
| CHEMBL1779487 | — | — | 1 | 5.48 |
| CHEMBL1779489 | — | — | 1 | 5.37 |
| CHEMBL1779486 | — | — | 1 | 5.16 |
| CHEMBL1779375 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1779485 | — | EC50 | = | 430.0 | nM | 6.37 |
| CHEMBL1779372 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1779371 | — | EC50 | = | 920.0 | nM | 6.04 |
| CHEMBL1779488 | — | EC50 | = | 930.0 | nM | 6.03 |
| CHEMBL1779370 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1779369 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1779374 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1779373 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1779487 | — | EC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL1779489 | — | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL1779486 | — | EC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL1779375 | — | EC50 | > | 10000.0 | nM | - |