Assay Detail
Binding
CHEMBL1686372
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Inhibition of recombinant human MMP14 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrs
22
Total Activities
22
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 |
Publication
The design and synthesis of novel N-hydroxyformamide inhibitors of ADAM-TS4 for the treatment of osteoarthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.02 | 8.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1683445 | — | — | 1 | 8.12 |
| CHEMBL1683443 | — | — | 1 | 7.96 |
| CHEMBL1683452 | — | — | 1 | 7.25 |
| CHEMBL1683454 | — | — | 1 | 6.80 |
| CHEMBL1683444 | — | — | 1 | 6.75 |
| CHEMBL1683450 | — | — | 1 | 6.44 |
| CHEMBL1683451 | — | — | 1 | 6.41 |
| CHEMBL1615186 | — | — | 1 | 6.37 |
| CHEMBL1683449 | — | — | 1 | 6.05 |
| CHEMBL1683460 | — | — | 1 | 5.58 |
| CHEMBL1683453 | — | — | 1 | 5.44 |
| CHEMBL1683457 | — | — | 1 | 5.38 |
| CHEMBL1683455 | — | — | 1 | 5.34 |
| CHEMBL1683458 | — | — | 1 | 4.77 |
| CHEMBL1683456 | — | — | 1 | 4.75 |
| CHEMBL1683465 | — | — | 1 | 4.54 |
| CHEMBL1683463 | — | — | 1 | 4.40 |
| CHEMBL1683462 | — | — | 1 | - |
| CHEMBL1683464 | — | — | 1 | - |
| CHEMBL1683461 | — | — | 1 | - |
| CHEMBL1683459 | — | — | 1 | - |
| CHEMBL1615187 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1683445 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL1683443 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1683452 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL1683454 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1683444 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1683450 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL1683451 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL1615186 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL1683449 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL1683460 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1683453 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL1683457 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL1683455 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL1683458 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL1683456 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL1683465 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL1683463 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL1683462 | — | IC50 | > | 18000.0 | nM | - |
| CHEMBL1683464 | — | IC50 | > | 3600.0 | nM | - |
| CHEMBL1683461 | — | IC50 | > | 3700.0 | nM | - |
| CHEMBL1683459 | — | IC50 | > | 8000.0 | nM | - |
| CHEMBL1615187 | — | IC50 | > | 8900.0 | nM | - |