Assay Detail
Binding
CHEMBL1768095
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant TACE after 60 mins by fluorescence plate reader
43
Total Activities
43
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 17 (CHEMBL3706) ↗| 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 | 43 | 5.68 | 6.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL24398 | — | — | 1 | 6.37 |
| CHEMBL1766904 | — | — | 1 | 5.96 |
| CHEMBL1766899 | — | — | 1 | 5.80 |
| CHEMBL1766905 | — | — | 1 | 5.72 |
| CHEMBL1078279 | — | — | 1 | 5.57 |
| CHEMBL1766903 | — | — | 1 | 5.42 |
| CHEMBL1078281 | — | — | 1 | 5.40 |
| CHEMBL1767010 | — | — | 1 | 5.20 |
| CHEMBL1767011 | — | — | 1 | - |
| CHEMBL1766902 | — | — | 1 | - |
| CHEMBL1767012 | — | — | 1 | - |
| CHEMBL1767013 | — | — | 1 | - |
| CHEMBL1767014 | — | — | 1 | - |
| CHEMBL1767015 | — | — | 1 | - |
| CHEMBL1767016 | — | — | 1 | - |
| CHEMBL1766910 | — | — | 1 | - |
| CHEMBL1766898 | — | — | 1 | - |
| CHEMBL1766900 | — | — | 1 | - |
| CHEMBL1766901 | — | — | 1 | - |
| CHEMBL1767009 | — | — | 1 | - |
| CHEMBL1767008 | — | — | 1 | - |
| CHEMBL1767007 | — | — | 1 | - |
| CHEMBL1767006 | — | — | 1 | - |
| CHEMBL1767005 | — | — | 1 | - |
| CHEMBL1767004 | — | — | 1 | - |
| CHEMBL1767003 | — | — | 1 | - |
| CHEMBL1766920 | — | — | 1 | - |
| CHEMBL1767017 | — | — | 1 | - |
| CHEMBL1766921 | — | — | 1 | - |
| CHEMBL1766922 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL24398 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL1766904 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1766899 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1766905 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1078279 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1766903 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL1078281 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL1767010 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL1766898 | — | IC50 | - | — | - | |
| CHEMBL1766918 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1766900 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1766901 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1766902 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1766906 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1766907 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1766908 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1766909 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1766919 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1766911 | — | IC50 | - | — | - | |
| CHEMBL1766912 | — | IC50 | - | — | - | |
| CHEMBL1766913 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2448145 | — | IC50 | - | — | - | |
| CHEMBL1766915 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1766916 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1766917 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1767007 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1766922 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1766921 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1767017 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1766920 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1767003 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1767004 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1767005 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1767006 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1766910 | — | IC50 | - | — | - | |
| CHEMBL1767008 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1767009 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1767011 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1767012 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1767013 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1767014 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1767015 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1767016 | — | IC50 | > | 10000.0 | nM | - |