Assay Detail
Binding
CHEMBL868588
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TACE by FRET assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
Design and synthesis of butynyloxyphenyl beta-sulfone piperidine hydroxamates as TACE inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 8.66 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL212481 | — | — | 1 | 9.00 |
| CHEMBL425251 | — | — | 1 | 9.00 |
| CHEMBL385821 | — | — | 1 | 8.85 |
| CHEMBL379287 | — | — | 1 | 8.85 |
| CHEMBL377862 | — | — | 1 | 8.85 |
| CHEMBL209970 | — | — | 1 | 8.82 |
| CHEMBL212411 | — | — | 1 | 8.77 |
| CHEMBL212205 | — | — | 1 | 8.74 |
| CHEMBL211726 | — | — | 1 | 8.70 |
| CHEMBL377317 | — | — | 1 | 8.68 |
| CHEMBL380049 | — | — | 1 | 8.68 |
| CHEMBL387079 | — | — | 1 | 8.68 |
| CHEMBL379763 | — | — | 1 | 8.66 |
| CHEMBL211487 | — | — | 1 | 8.66 |
| CHEMBL211274 | — | — | 1 | 8.66 |
| CHEMBL210084 | — | — | 1 | 8.64 |
| CHEMBL212469 | — | — | 1 | 8.64 |
| CHEMBL214287 | — | — | 1 | 8.60 |
| CHEMBL208841 | — | — | 1 | 8.47 |
| CHEMBL212920 | — | — | 1 | 8.40 |
| CHEMBL209490 | — | — | 1 | 8.32 |
| CHEMBL425783 | — | — | 1 | 8.31 |
| CHEMBL377272 | — | — | 1 | 8.22 |
| CHEMBL211770 | — | — | 1 | - |
| CHEMBL210133 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL212481 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL425251 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL385821 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL379287 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL377862 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL209970 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL212411 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL212205 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL211726 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL377317 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL380049 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL387079 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL379763 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL211487 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL211274 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL210084 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL212469 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL214287 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL208841 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL212920 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL209490 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL425783 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL377272 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL211770 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL210133 | — | IC50 | < | 1.0 | nM | - |