Assay Detail
Binding
CHEMBL927855
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Inhibition of ADAM10
30
Total Activities
30
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 10 (CHEMBL5028) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.45 | 8.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL400528 | — | — | 1 | 8.11 |
| CHEMBL253021 | — | — | 1 | 8.04 |
| CHEMBL251820 | — | — | 1 | 8.00 |
| CHEMBL253230 | — | — | 1 | 7.96 |
| CHEMBL254492 | — | — | 1 | 7.96 |
| CHEMBL253665 | — | — | 1 | 7.92 |
| CHEMBL399351 | — | — | 1 | 7.82 |
| CHEMBL442432 | — | — | 1 | 7.80 |
| CHEMBL253035 | — | — | 1 | 7.75 |
| CHEMBL252023 | — | — | 1 | 7.75 |
| CHEMBL252612 | — | — | 1 | 7.75 |
| CHEMBL253020 | — | — | 1 | 7.72 |
| CHEMBL439405 | — | — | 1 | 7.66 |
| CHEMBL398743 | — | — | 1 | 7.62 |
| CHEMBL252024 | — | — | 1 | 7.58 |
| CHEMBL404409 | — | — | 1 | 7.55 |
| CHEMBL253019 | — | — | 1 | 7.47 |
| CHEMBL253652 | — | — | 1 | 7.47 |
| CHEMBL253890 | — | — | 1 | 7.41 |
| CHEMBL252627 | — | — | 1 | 7.36 |
| CHEMBL254295 | — | — | 1 | 7.24 |
| CHEMBL442291 | — | — | 1 | 7.04 |
| CHEMBL251823 | — | — | 1 | 6.97 |
| CHEMBL251830 | — | — | 1 | 6.97 |
| CHEMBL254715 | — | — | 1 | 6.58 |
| CHEMBL254510 | — | — | 1 | 6.54 |
| CHEMBL254508 | — | — | 1 | 6.48 |
| CHEMBL427717 | — | — | 1 | 5.99 |
| CHEMBL252830 | — | — | 1 | - |
| CHEMBL253452 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400528 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL253021 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL251820 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL253230 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL254492 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL253665 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL399351 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL442432 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL253035 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL252023 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL252612 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL253020 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL439405 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL398743 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL252024 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL404409 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL253019 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL253652 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL253890 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL252627 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL254295 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL442291 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL251823 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL251830 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL254715 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL254510 | — | IC50 | = | 286.0 | nM | 6.54 |
| CHEMBL254508 | — | IC50 | = | 332.0 | nM | 6.48 |
| CHEMBL427717 | — | IC50 | = | 1036.0 | nM | 5.99 |
| CHEMBL252830 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL253452 | — | IC50 | > | 2000.0 | nM | - |