Assay Detail
Binding
CHEMBL897091
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Inhibition of ADAMTS5 by FRET assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
A disintegrin and metalloproteinase with thrombospondin motifs 5 (CHEMBL2285) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.24 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL231740 | — | — | 1 | 5.96 |
| CHEMBL442073 | — | — | 1 | 5.68 |
| CHEMBL393113 | — | — | 1 | 5.66 |
| CHEMBL232364 | — | — | 1 | 5.60 |
| CHEMBL231752 | — | — | 1 | 5.43 |
| CHEMBL232565 | — | — | 1 | 5.38 |
| CHEMBL233132 | — | — | 1 | 5.38 |
| CHEMBL231962 | — | — | 1 | 5.34 |
| CHEMBL393991 | — | — | 1 | 5.34 |
| CHEMBL231780 | — | — | 1 | 5.24 |
| CHEMBL394026 | — | — | 1 | 5.17 |
| CHEMBL391928 | — | — | 1 | 5.15 |
| CHEMBL391299 | — | — | 1 | 5.10 |
| CHEMBL231755 | — | — | 1 | 5.08 |
| CHEMBL391693 | — | — | 1 | 5.05 |
| CHEMBL233333 | — | — | 1 | 5.04 |
| CHEMBL231990 | — | — | 1 | 4.93 |
| CHEMBL231754 | — | — | 1 | 4.85 |
| CHEMBL400198 | — | — | 1 | 4.77 |
| CHEMBL392264 | — | — | 1 | 4.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL231740 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL442073 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL393113 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL232364 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL231752 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL232565 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL233132 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL231962 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL393991 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL231780 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL394026 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL391928 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL391299 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL231755 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL391693 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL233333 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL231990 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL231754 | — | IC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL400198 | — | IC50 | = | 16900.0 | nM | 4.77 |
| CHEMBL392264 | — | IC50 | = | 23200.0 | nM | 4.63 |