Assay Detail
Functional
CHEMBL654358
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of human recombinant IL-1-beta-induced breakdown of bovine cartilage in a cartilage organ culture assay
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Bos taurus |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Heteroaryl-fused 2-phenylisothiazolone inhibitors of cartilage breakdown.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 4.98 | 5.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL421398 | — | — | 1 | 5.54 |
| CHEMBL105189 | — | — | 1 | 5.52 |
| CHEMBL102387 | — | — | 1 | 5.46 |
| CHEMBL103470 | — | — | 1 | 5.40 |
| CHEMBL316658 | — | — | 1 | 5.36 |
| CHEMBL105757 | — | — | 1 | 5.36 |
| CHEMBL321809 | — | — | 1 | 5.31 |
| CHEMBL104863 | — | — | 1 | 5.27 |
| CHEMBL322881 | — | — | 1 | 5.22 |
| CHEMBL105373 | — | — | 1 | 5.16 |
| CHEMBL105200 | — | — | 1 | 5.16 |
| CHEMBL318098 | — | — | 1 | 5.11 |
| CHEMBL320843 | — | — | 1 | 5.10 |
| CHEMBL433167 | — | — | 1 | 5.10 |
| CHEMBL100470 | — | — | 1 | 5.10 |
| CHEMBL101422 | — | — | 1 | 5.09 |
| CHEMBL104736 | — | — | 1 | 5.09 |
| CHEMBL318367 | — | — | 1 | 5.07 |
| CHEMBL262554 | — | — | 1 | 5.05 |
| CHEMBL105588 | — | — | 1 | 5.05 |
| CHEMBL321373 | — | — | 1 | 5.05 |
| CHEMBL104611 | — | — | 1 | 5.02 |
| CHEMBL322629 | — | — | 1 | 5.02 |
| CHEMBL317848 | — | — | 1 | 4.96 |
| CHEMBL101858 | — | — | 1 | 4.92 |
| CHEMBL106011 | — | — | 1 | 4.92 |
| CHEMBL104542 | — | — | 1 | 4.89 |
| CHEMBL95284 | — | — | 1 | 4.87 |
| CHEMBL105418 | — | — | 1 | 4.85 |
| CHEMBL321535 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL421398 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL105189 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL102387 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL103470 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL316658 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL105757 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL321809 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL104863 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL322881 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL105373 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL105200 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL318098 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL320843 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL100470 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL433167 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL101422 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL104736 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL318367 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL262554 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL105588 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL321373 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL322629 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL104611 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL317848 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL101858 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL106011 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL104542 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL95284 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL105418 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL321535 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL263279 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL319633 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL102855 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL105190 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL99137 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL318167 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL105482 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL105419 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL102496 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL106835 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL105959 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL1440 | TETRACYCLINE | IC50 | > | 30000.0 | nM | - |
| CHEMBL6 | INDOMETHACIN | IC50 | > | 30000.0 | nM | - |
| CHEMBL154 | NAPROXEN | IC50 | > | 30000.0 | nM | - |
| CHEMBL7660 | PHENIDONE | IC50 | > | 30000.0 | nM | - |