Assay Detail
Binding
CHEMBL4010777
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Inhibition of TACE in NHEK assessed as reduction in LPS/TPA-stimulated TNFalpha production preincubated for 1 hr followed by LPS/TPA stimulation for 24 hrs by HTRF assay
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of novel TACE inhibitors compatible with topical application.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.25 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4065066 | — | — | 1 | 7.22 |
| CHEMBL206815 | APRATASTAT | 2.0 | 2 | 6.92 |
| CHEMBL4102106 | — | — | 1 | 5.89 |
| CHEMBL4069235 | — | — | 1 | 5.51 |
| CHEMBL4096228 | — | — | 1 | 5.04 |
| CHEMBL4076780 | — | — | 1 | - |
| CHEMBL4066243 | — | — | 1 | - |
| CHEMBL4093818 | — | — | 1 | - |
| CHEMBL4078894 | — | — | 1 | - |
| CHEMBL4067012 | — | — | 1 | - |
| CHEMBL4061327 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4065066 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL206815 | APRATASTAT | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL206815 | APRATASTAT | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4102106 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4069235 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4096228 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL4076780 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4066243 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4093818 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4078894 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4067012 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4061327 | — | IC50 | > | 10000.0 | nM | - |