Assay Detail
Binding
CHEMBL1106705
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Inhibition of ADAMTS5
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
A disintegrin and metalloproteinase with thrombospondin motifs 5 (CHEMBL2285) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.08 | 8.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1078281 | — | — | 1 | 8.13 |
| CHEMBL1078454 | — | — | 1 | 8.00 |
| CHEMBL1078279 | — | — | 1 | 7.68 |
| CHEMBL1078280 | — | — | 1 | 7.50 |
| CHEMBL1078167 | — | — | 1 | 7.22 |
| CHEMBL448604 | — | — | 1 | 7.14 |
| CHEMBL1077893 | — | — | 1 | 7.10 |
| CHEMBL1079173 | — | — | 1 | 7.08 |
| CHEMBL1078168 | — | — | 1 | 7.03 |
| CHEMBL1077892 | — | — | 1 | 7.00 |
| CHEMBL1077579 | — | — | 1 | 6.92 |
| CHEMBL1079172 | — | — | 1 | 6.68 |
| CHEMBL1078625 | — | — | 1 | 6.44 |
| CHEMBL1078624 | — | — | 1 | 6.11 |
| CHEMBL1078322 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1078281 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL1078454 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1078279 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1078280 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1078167 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL448604 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL1077893 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1079173 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL1078168 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL1077892 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1077579 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1079172 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1078625 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL1078624 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL1078322 | — | IC50 | = | 800.0 | nM | 6.10 |