Assay Detail
Binding
CHEMBL1002953
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Inhibition of TACE
14
Total Activities
14
Compounds Tested
2
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
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.06 | 8.82 |
| Ki | 5 | 7.36 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL209970 | — | — | 1 | 8.82 |
| CHEMBL484261 | — | — | 1 | 8.70 |
| CHEMBL484262 | — | — | 1 | 8.66 |
| CHEMBL399096 | — | — | 1 | 8.49 |
| CHEMBL318252 | — | — | 1 | 8.22 |
| CHEMBL410462 | — | — | 1 | 8.10 |
| CHEMBL402747 | — | — | 1 | 8.00 |
| CHEMBL270558 | — | — | 1 | 7.92 |
| CHEMBL434567 | — | — | 1 | 7.85 |
| CHEMBL497985 | — | — | 1 | 5.69 |
| CHEMBL483857 | — | — | 1 | 5.43 |
| CHEMBL270083 | — | — | 1 | - |
| CHEMBL507420 | — | — | 1 | - |
| CHEMBL497772 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL209970 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL484261 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL484262 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL399096 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL318252 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL410462 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL402747 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL270558 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL434567 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL497985 | — | IC50 | = | 2045.0 | nM | 5.69 |
| CHEMBL483857 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL270083 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL507420 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL497772 | — | IC50 | > | 25000.0 | nM | - |