Assay Detail
Functional
CHEMBL1805902
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Antiinflammatory activity against LPS-induced TNFalpha release in human PBMC preincubated for 30 mins measured after 3 hrs of LPS stimulation
29
Total Activities
29
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
In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.67 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1801374 | — | — | 1 | 8.30 |
| CHEMBL1801384 | — | — | 1 | 8.05 |
| CHEMBL1801373 | — | — | 1 | 7.85 |
| CHEMBL1801375 | — | — | 1 | 7.85 |
| CHEMBL1801376 | — | — | 1 | 7.82 |
| CHEMBL1801385 | — | — | 1 | 7.50 |
| CHEMBL1801315 | — | — | 1 | 7.34 |
| CHEMBL1801386 | — | — | 1 | 7.01 |
| CHEMBL1801391 | — | — | 1 | 6.85 |
| CHEMBL1801377 | — | — | 1 | 6.70 |
| CHEMBL1801390 | — | — | 1 | 6.70 |
| CHEMBL1614995 | — | — | 1 | 6.58 |
| CHEMBL1801388 | — | — | 1 | 6.55 |
| CHEMBL1801380 | — | — | 1 | 6.55 |
| CHEMBL1801387 | — | — | 1 | 6.53 |
| CHEMBL1801382 | — | — | 1 | 6.38 |
| CHEMBL1801381 | — | — | 1 | 6.25 |
| CHEMBL1801091 | — | — | 1 | 6.24 |
| CHEMBL1801313 | — | — | 1 | 6.13 |
| CHEMBL1801378 | — | — | 1 | 6.04 |
| CHEMBL1801314 | — | — | 1 | 5.91 |
| CHEMBL1801389 | — | — | 1 | 5.85 |
| CHEMBL1801316 | — | — | 1 | 5.63 |
| CHEMBL1801090 | — | — | 1 | 5.08 |
| CHEMBL1801089 | — | — | 1 | 5.07 |
| CHEMBL1801392 | — | — | 1 | - |
| CHEMBL1801383 | — | — | 1 | - |
| CHEMBL1801088 | — | — | 1 | - |
| CHEMBL1801379 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1801374 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1801384 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1801373 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1801375 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1801376 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1801385 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1801315 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL1801386 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL1801391 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1801377 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL1801390 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL1614995 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1801388 | — | IC50 | = | 283.0 | nM | 6.55 |
| CHEMBL1801380 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1801387 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL1801382 | — | IC50 | = | 416.0 | nM | 6.38 |
| CHEMBL1801381 | — | IC50 | = | 556.0 | nM | 6.25 |
| CHEMBL1801091 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL1801313 | — | IC50 | = | 735.0 | nM | 6.13 |
| CHEMBL1801378 | — | IC50 | = | 912.0 | nM | 6.04 |
| CHEMBL1801314 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL1801389 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1801316 | — | IC50 | = | 2359.0 | nM | 5.63 |
| CHEMBL1801090 | — | IC50 | = | 8380.0 | nM | 5.08 |
| CHEMBL1801089 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL1801392 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1801383 | — | IC50 | - | — | - | |
| CHEMBL1801088 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL1801379 | — | IC50 | - | — | - |