Assay Detail
Binding
CHEMBL1019003
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Inhibition of TACE catalytic domain by FRET assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel spirocyclopropyl hydroxamate and carboxylate compounds as TACE inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.49 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL148169 | — | — | 1 | 10.22 |
| CHEMBL461220 | — | — | 1 | 9.85 |
| CHEMBL461221 | — | — | 1 | 9.74 |
| CHEMBL269834 | — | — | 1 | 8.52 |
| CHEMBL517708 | — | — | 1 | 8.17 |
| CHEMBL459747 | — | — | 1 | 7.52 |
| CHEMBL459748 | — | — | 1 | 7.50 |
| CHEMBL468887 | — | — | 1 | 7.50 |
| CHEMBL468888 | — | — | 1 | 7.48 |
| CHEMBL466599 | — | — | 1 | 7.40 |
| CHEMBL467846 | — | — | 1 | 7.28 |
| CHEMBL468689 | — | — | 1 | 7.03 |
| CHEMBL460597 | — | — | 1 | 6.86 |
| CHEMBL468690 | — | — | 1 | 6.84 |
| CHEMBL468896 | — | — | 1 | 6.17 |
| CHEMBL467856 | — | — | 1 | 5.67 |
| CHEMBL467857 | — | — | 1 | 5.51 |
| CHEMBL466813 | — | — | 1 | 5.49 |
| CHEMBL467020 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL148169 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL461220 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL461221 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL269834 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL517708 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL459747 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL459748 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL468887 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL468888 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL466599 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL467846 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL468689 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL460597 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL468690 | — | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL468896 | — | Ki | = | 673.0 | nM | 6.17 |
| CHEMBL467856 | — | Ki | = | 2140.0 | nM | 5.67 |
| CHEMBL467857 | — | Ki | = | 3070.0 | nM | 5.51 |
| CHEMBL466813 | — | Ki | = | 3220.0 | nM | 5.49 |
| CHEMBL467020 | — | Ki | > | 50000.0 | nM | - |