Assay Detail
Functional
CHEMBL831580
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Inhibitory concentration against TNF-alpha release in LPS treated whole blood
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 3-OH-3-methylpipecolic hydroxamates: potent orally active inhibitors of aggrecanase and MMP-13.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.11 | 9.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL446697 | — | — | 1 | 9.32 |
| CHEMBL363126 | — | — | 1 | 8.80 |
| CHEMBL186500 | — | — | 1 | 8.72 |
| CHEMBL186663 | — | — | 1 | 8.66 |
| CHEMBL365283 | — | — | 1 | 8.60 |
| CHEMBL436277 | — | — | 1 | 8.60 |
| CHEMBL186743 | — | — | 1 | 8.48 |
| CHEMBL187474 | — | — | 1 | 8.19 |
| CHEMBL365247 | — | — | 1 | 8.15 |
| CHEMBL183995 | — | — | 1 | 8.14 |
| CHEMBL183474 | — | — | 1 | 8.08 |
| CHEMBL187852 | — | — | 1 | 7.85 |
| CHEMBL369115 | — | — | 1 | 7.82 |
| CHEMBL187245 | — | — | 1 | 7.77 |
| CHEMBL182306 | — | — | 1 | 7.48 |
| CHEMBL187141 | — | — | 1 | 7.22 |
| CHEMBL360854 | — | — | 1 | 7.14 |
| CHEMBL426975 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL446697 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL363126 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL186500 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL186663 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL365283 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL436277 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL186743 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL187474 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL365247 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL183995 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL183474 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL187852 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL369115 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL187245 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL182306 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL187141 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL360854 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL426975 | — | IC50 | = | 100.0 | nM | 7.00 |