Assay Detail
Binding
CHEMBL3107055
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant ADAMTS-5 using interglobular domain peptide of aggrecan after 60 mins by FRET assay
28
Total Activities
28
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 5 (CHEMBL2285) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a benzimidazole series of ADAMTS-5 (aggrecanase-2) inhibitors by scaffold hopping.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 5.97 | 6.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3104658 | — | — | 1 | 6.77 |
| CHEMBL2348091 | — | — | 1 | 6.64 |
| CHEMBL3104666 | — | — | 1 | 6.42 |
| CHEMBL3104659 | — | — | 1 | 6.39 |
| CHEMBL3104657 | — | — | 1 | 6.38 |
| CHEMBL3104660 | — | — | 1 | 6.37 |
| CHEMBL3104667 | — | — | 1 | 6.33 |
| CHEMBL3104673 | — | — | 1 | 6.33 |
| CHEMBL3104661 | — | — | 1 | 6.32 |
| CHEMBL3104650 | — | — | 1 | 6.32 |
| CHEMBL3104662 | — | — | 1 | 6.30 |
| CHEMBL3104649 | — | — | 1 | 6.30 |
| CHEMBL3104676 | — | — | 1 | 6.16 |
| CHEMBL3104672 | — | — | 1 | 5.89 |
| CHEMBL3104663 | — | — | 1 | 5.89 |
| CHEMBL3104668 | — | — | 1 | 5.85 |
| CHEMBL3104664 | — | — | 1 | 5.85 |
| CHEMBL3104656 | — | — | 1 | 5.82 |
| CHEMBL3104652 | — | — | 1 | 5.77 |
| CHEMBL3104674 | — | — | 1 | 5.77 |
| CHEMBL3104675 | — | — | 1 | 5.77 |
| CHEMBL3104654 | — | — | 1 | 5.60 |
| CHEMBL3104653 | — | — | 1 | 5.57 |
| CHEMBL3104665 | — | — | 1 | 5.40 |
| CHEMBL3104670 | — | — | 1 | 5.30 |
| CHEMBL3104671 | — | — | 1 | 5.27 |
| CHEMBL3104669 | — | — | 1 | 5.22 |
| CHEMBL3104655 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3104658 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2348091 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3104666 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3104659 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3104657 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3104660 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL3104667 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3104673 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3104661 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3104650 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3104662 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3104649 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3104676 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3104672 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3104663 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3104668 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3104664 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3104656 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3104652 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3104674 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3104675 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3104654 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3104653 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3104665 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3104670 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3104671 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL3104669 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3104655 | — | IC50 | = | 6000.0 | nM | 5.22 |