Assay Detail
Binding
CHEMBL2317231
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Inhibition of p38alpha MAP kinase in whole blood (unknown origin) assessed as lipopolysaccharide-stimulated TNF-alpha release by ELISA
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dibenzosuberones as p38 mitogen-activated protein kinase inhibitors with low ATP competitiveness and outstanding whole blood activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 6.89 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2316466 | — | — | 1 | 7.92 |
| CHEMBL2316480 | — | — | 1 | 7.77 |
| CHEMBL2316481 | — | — | 1 | 7.75 |
| CHEMBL2316197 | — | — | 1 | 7.75 |
| CHEMBL2316469 | — | — | 1 | 7.72 |
| CHEMBL2316195 | — | — | 1 | 7.72 |
| CHEMBL2316490 | — | — | 1 | 7.58 |
| CHEMBL2316478 | — | — | 1 | 7.57 |
| CHEMBL2316194 | — | — | 1 | 7.57 |
| CHEMBL2316479 | — | — | 1 | 7.54 |
| CHEMBL2316477 | — | — | 1 | 7.54 |
| CHEMBL2316207 | FS-694 | — | 1 | 7.51 |
| CHEMBL2316494 | — | — | 1 | 7.50 |
| CHEMBL2316474 | — | — | 1 | 7.44 |
| CHEMBL2316470 | — | — | 1 | 7.43 |
| CHEMBL2152944 | Skepinone-L | — | 1 | 7.40 |
| CHEMBL2316493 | — | — | 1 | 7.38 |
| CHEMBL2316476 | — | — | 1 | 7.30 |
| CHEMBL2316475 | — | — | 1 | 7.27 |
| CHEMBL2316473 | — | — | 1 | 7.19 |
| CHEMBL2316198 | — | — | 1 | 7.19 |
| CHEMBL2316472 | — | — | 1 | 7.08 |
| CHEMBL2316491 | — | — | 1 | 7.02 |
| CHEMBL2316196 | — | — | 1 | 7.02 |
| CHEMBL2316489 | — | — | 1 | 6.96 |
| CHEMBL2316496 | — | — | 1 | 6.82 |
| CHEMBL2316201 | — | — | 1 | 6.80 |
| CHEMBL2316205 | — | — | 1 | 6.68 |
| CHEMBL2316497 | — | — | 1 | 6.66 |
| CHEMBL2316203 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2316466 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2316480 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2316197 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2316481 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2316469 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2316195 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2316490 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2316478 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2316194 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2316479 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2316477 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2316207 | FS-694 | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL2316494 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2316474 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL2316470 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2152944 | Skepinone-L | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2316493 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2316476 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2316475 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL2316473 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2316198 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2316472 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL2316196 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL2316491 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL2316489 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2316496 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2316201 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2316205 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL2316497 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2316203 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2316206 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2316485 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL2316202 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL2316486 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2316208 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2316492 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2316484 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL2316199 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL2316468 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL2316495 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL2316487 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2316204 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL2316483 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2316482 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL2316471 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL2316488 | — | IC50 | = | 9000.0 | nM | 5.05 |