Assay Detail
Binding
CHEMBL897707
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Inhibition of human TACE expressed in CHO cells by FRET assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.33 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL236573 | — | — | 1 | 8.80 |
| CHEMBL237467 | — | — | 1 | 8.70 |
| CHEMBL236572 | — | — | 1 | 8.70 |
| CHEMBL235559 | — | — | 1 | 8.64 |
| CHEMBL238081 | — | — | 1 | 8.64 |
| CHEMBL236400 | — | — | 1 | 8.60 |
| CHEMBL209970 | — | — | 1 | 8.52 |
| CHEMBL236574 | — | — | 1 | 8.48 |
| CHEMBL400430 | — | — | 1 | 8.46 |
| CHEMBL236806 | — | — | 1 | 8.40 |
| CHEMBL237468 | — | — | 1 | 8.19 |
| CHEMBL207729 | — | — | 1 | 8.10 |
| CHEMBL399400 | — | — | 1 | 8.00 |
| CHEMBL394003 | — | — | 1 | 7.57 |
| CHEMBL237466 | — | — | 1 | 7.19 |
| CHEMBL399401 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL236573 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL237467 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL236572 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL235559 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL238081 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL236400 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL209970 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL236574 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL400430 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL236806 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL237468 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL207729 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL399400 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL394003 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL237466 | — | IC50 | = | 64.5 | nM | 7.19 |
| CHEMBL399401 | — | IC50 | < | 1.0 | nM | - |