Assay Detail
Binding
CHEMBL930771
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Inhibition of human MMP13
30
Total Activities
30
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 |
Publication
Quinazolinones and pyrido[3,4-d]pyrimidin-4-ones as orally active and specific matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.70 | 9.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL410029 | — | — | 1 | 9.11 |
| CHEMBL429584 | — | — | 1 | 8.19 |
| CHEMBL273054 | — | — | 1 | 8.01 |
| CHEMBL270502 | — | — | 1 | 7.96 |
| CHEMBL273113 | — | — | 1 | 7.75 |
| CHEMBL272245 | — | — | 1 | 7.75 |
| CHEMBL272007 | — | — | 1 | 7.67 |
| CHEMBL409111 | — | — | 1 | 7.55 |
| CHEMBL270050 | — | — | 1 | 7.52 |
| CHEMBL271997 | — | — | 1 | 7.43 |
| CHEMBL272008 | — | — | 1 | 7.34 |
| CHEMBL429596 | — | — | 1 | 7.32 |
| CHEMBL408646 | — | — | 1 | 7.24 |
| CHEMBL271148 | — | — | 1 | 7.10 |
| CHEMBL406919 | — | — | 1 | 6.92 |
| CHEMBL429247 | — | — | 1 | 6.92 |
| CHEMBL407090 | — | — | 1 | 6.91 |
| CHEMBL272246 | — | — | 1 | 6.85 |
| CHEMBL271535 | — | — | 1 | 6.74 |
| CHEMBL429250 | — | — | 1 | 6.74 |
| CHEMBL272866 | — | — | 1 | 6.61 |
| CHEMBL406831 | — | — | 1 | 6.21 |
| CHEMBL272261 | — | — | 1 | 5.77 |
| CHEMBL410322 | — | — | 1 | 5.72 |
| CHEMBL270481 | — | — | 1 | 5.52 |
| CHEMBL270480 | — | — | 1 | 5.22 |
| CHEMBL409223 | — | — | 1 | 5.00 |
| CHEMBL272188 | — | — | 1 | 4.00 |
| CHEMBL273114 | — | — | 1 | 4.00 |
| CHEMBL271616 | — | — | 1 | 4.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL410029 | — | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL429584 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL273054 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL270502 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL273113 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL272245 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL272007 | — | IC50 | = | 21.2 | nM | 7.67 |
| CHEMBL409111 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL270050 | — | IC50 | = | 30.5 | nM | 7.52 |
| CHEMBL271997 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL272008 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL429596 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL408646 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL271148 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL406919 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL429247 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL407090 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL272246 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL271535 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL429250 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL272866 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL406831 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL272261 | — | IC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL410322 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL270481 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL270480 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL409223 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL272188 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL273114 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL271616 | — | IC50 | = | 100000.0 | nM | 4.00 |