Assay Detail
Functional
CHEMBL1780646
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production pretreated 30 mins before LPS challenge measured after 4 hrs
36
Total Activities
36
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 selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 36 | 5.59 | 6.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1779352 | — | — | 1 | 6.55 |
| CHEMBL1779353 | — | — | 1 | 6.33 |
| CHEMBL1779372 | — | — | 1 | 6.07 |
| CHEMBL1738702 | — | — | 1 | 6.04 |
| CHEMBL1779485 | — | — | 1 | 6.01 |
| CHEMBL1779370 | — | — | 1 | 5.85 |
| CHEMBL1779369 | — | — | 1 | 5.85 |
| CHEMBL1779350 | — | — | 1 | 5.85 |
| CHEMBL1779371 | — | — | 1 | 5.82 |
| CHEMBL1779488 | — | — | 1 | 5.80 |
| CHEMBL1779354 | — | — | 1 | 5.80 |
| CHEMBL1779375 | — | — | 1 | 5.66 |
| CHEMBL1779374 | — | — | 1 | 5.62 |
| CHEMBL1779367 | — | — | 1 | 5.58 |
| CHEMBL1779487 | — | — | 1 | 5.52 |
| CHEMBL1779359 | — | — | 1 | 5.44 |
| CHEMBL1779349 | — | — | 1 | 5.38 |
| CHEMBL1779356 | — | — | 1 | 5.38 |
| CHEMBL1779361 | — | — | 1 | 5.32 |
| CHEMBL1779347 | — | — | 1 | 5.31 |
| CHEMBL1779346 | — | — | 1 | 5.30 |
| CHEMBL1779358 | — | — | 1 | 5.23 |
| CHEMBL1779355 | — | — | 1 | 5.21 |
| CHEMBL1779360 | — | — | 1 | 5.20 |
| CHEMBL1779357 | — | — | 1 | 5.20 |
| CHEMBL1779373 | — | — | 1 | 5.08 |
| CHEMBL1779489 | — | — | 1 | 5.06 |
| CHEMBL226471 | — | — | 1 | 5.04 |
| CHEMBL1779366 | — | — | 1 | - |
| CHEMBL1779365 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1779352 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1779353 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL1779372 | — | EC50 | = | 850.0 | nM | 6.07 |
| CHEMBL1738702 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL1779485 | — | EC50 | = | 980.0 | nM | 6.01 |
| CHEMBL1779370 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1779369 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1779350 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1779371 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1779354 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1779488 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1779375 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1779374 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1779367 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1779487 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1779359 | — | EC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL1779349 | — | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL1779356 | — | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL1779361 | — | EC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL1779347 | — | EC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL1779346 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL1779358 | — | EC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL1779355 | — | EC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL1779360 | — | EC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL1779357 | — | EC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL1779373 | — | EC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL1779489 | — | EC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL226471 | — | EC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL1779366 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1779365 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1779364 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1779363 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1779362 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1779486 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1779348 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1779351 | — | EC50 | > | 10000.0 | nM | - |