Assay Detail
Binding
CHEMBL3888015
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Inhibition Assay: The molecules are tested in dose-response studies on the following enzymes MMP1, MMP3, MMP9, ADAM9 and ADAM10 according to the same protocol as that described for the TACE enzyme in example 28 but with different substrates (MMP R&D system reference: P126-990 and ADAM R&D system reference: ES003).
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Disintegrin and metalloproteinase domain-containing protein 10 (CHEMBL5028) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
4-alkoxy-N-(2-hydroxycarbamoyl-2-piperidinyl-ethyl)-benzamide compounds as selective TACE-inhibitors for the treatment of inflammatory diseases
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.95 | 7.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL206815 | APRATASTAT | 2.0 | 1 | 7.15 |
| CHEMBL3935135 | — | — | 1 | 5.51 |
| CHEMBL3897740 | — | — | 1 | 5.19 |
| CHEMBL3941484 | — | — | 1 | - |
| CHEMBL3966632 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL206815 | APRATASTAT | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3935135 | — | IC50 | = | 3091.0 | nM | 5.51 |
| CHEMBL3897740 | — | IC50 | = | 6405.0 | nM | 5.19 |
| CHEMBL3941484 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3966632 | — | IC50 | > | 10000.0 | nM | - |