Assay Detail
Binding
CHEMBL2352585
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Inhibition of human His-tagged ADAMTS-5 using QF-peptide as substrate by FRET method
27
Total Activities
27
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
A series of thiazole derivatives bearing thiazolidin-4-one as non-competitive ADAMTS-5 (aggrecanase-2) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 5.95 | 6.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2348091 | — | — | 1 | 6.64 |
| CHEMBL2348077 | — | — | 1 | 6.40 |
| CHEMBL2348090 | — | — | 1 | 6.38 |
| CHEMBL2348087 | — | — | 1 | 6.38 |
| CHEMBL2348089 | — | — | 1 | 6.37 |
| CHEMBL2348073 | — | — | 1 | 6.37 |
| CHEMBL2348076 | — | — | 1 | 6.33 |
| CHEMBL2348088 | — | — | 1 | 6.30 |
| CHEMBL2348092 | — | — | 1 | 6.20 |
| CHEMBL2348086 | — | — | 1 | 6.14 |
| CHEMBL2348071 | — | — | 1 | 6.14 |
| CHEMBL2348082 | — | — | 1 | 6.08 |
| CHEMBL2348078 | — | — | 1 | 6.08 |
| CHEMBL2348072 | — | — | 1 | 6.00 |
| CHEMBL2347847 | — | — | 1 | 5.92 |
| CHEMBL2348080 | — | — | 1 | 5.92 |
| CHEMBL2348081 | — | — | 1 | 5.92 |
| CHEMBL2348085 | — | — | 1 | 5.92 |
| CHEMBL2348083 | — | — | 1 | 5.85 |
| CHEMBL2348084 | — | — | 1 | 5.66 |
| CHEMBL2348067 | — | — | 1 | 5.55 |
| CHEMBL2348068 | — | — | 1 | 5.54 |
| CHEMBL2348075 | — | — | 1 | 5.52 |
| CHEMBL2348074 | — | — | 1 | 5.40 |
| CHEMBL2348069 | — | — | 1 | 5.38 |
| CHEMBL2348070 | — | — | 1 | 5.19 |
| CHEMBL2348079 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2348091 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2348077 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2348090 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2348087 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2348089 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL2348073 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL2348076 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL2348088 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2348092 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL2348086 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL2348071 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL2348082 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL2348078 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL2348072 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2347847 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2348080 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2348081 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2348085 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2348083 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2348084 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2348067 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL2348068 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL2348075 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL2348074 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2348069 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL2348070 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL2348079 | — | IC50 | = | 7000.0 | nM | 5.16 |