Assay Detail
Binding
CHEMBL1008370
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Inhibition of human recombinant ADAM10
19
Total Activities
19
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 10 (CHEMBL5028) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.93 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL496628 | — | — | 1 | 7.82 |
| CHEMBL495596 | — | — | 1 | 7.72 |
| CHEMBL496829 | — | — | 1 | 7.68 |
| CHEMBL497222 | — | — | 1 | 7.52 |
| CHEMBL497026 | — | — | 1 | 7.24 |
| CHEMBL523076 | — | — | 1 | 7.19 |
| CHEMBL496211 | — | — | 1 | 7.11 |
| CHEMBL496825 | — | — | 1 | 7.08 |
| CHEMBL497032 | — | — | 1 | 6.96 |
| CHEMBL221857 | — | — | 1 | 6.92 |
| CHEMBL495797 | — | — | 1 | 6.79 |
| CHEMBL496629 | — | — | 1 | 6.78 |
| CHEMBL496018 | — | — | 1 | 6.78 |
| CHEMBL521719 | — | — | 1 | 6.71 |
| CHEMBL445717 | — | — | 1 | 6.52 |
| CHEMBL387202 | — | — | 1 | 6.51 |
| CHEMBL252246 | — | — | 1 | 6.49 |
| CHEMBL497645 | — | — | 1 | 6.04 |
| CHEMBL496212 | — | — | 1 | 5.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL496628 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL495596 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL496829 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL497222 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL497026 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL523076 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL496211 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL496825 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL497032 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL221857 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL495797 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL496629 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL496018 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL521719 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL445717 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL387202 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL252246 | — | IC50 | = | 323.0 | nM | 6.49 |
| CHEMBL497645 | — | IC50 | = | 915.0 | nM | 6.04 |
| CHEMBL496212 | — | IC50 | = | 1545.0 | nM | 5.81 |