Assay Detail
Binding
CHEMBL1768099
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant aggrecanase 1 after 150 mins by fluorescence plate reader
7
Total Activities
7
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
A disintegrin and metalloproteinase with thrombospondin motifs 4 (CHEMBL2318) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of (1S,2R,3R)-2,3-dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates: novel and highly selective aggrecanase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.50 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL179552 | — | — | 1 | 8.96 |
| CHEMBL24398 | — | — | 1 | 8.52 |
| CHEMBL1078281 | — | — | 1 | 8.40 |
| CHEMBL1767014 | — | — | 1 | 7.64 |
| CHEMBL1766896 | — | — | 1 | 6.68 |
| CHEMBL1766897 | — | — | 1 | 6.68 |
| CHEMBL481894 | — | — | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL179552 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL24398 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1078281 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1767014 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1766896 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1766897 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL481894 | — | IC50 | = | 2400.0 | nM | 5.62 |