Assay Detail
Binding
CHEMBL974340
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Inhibition of MMP13 in presence of 1% bovine serum albumin
64
Total Activities
64
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 64 | 6.94 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL440498 | CTS-1027 | 2.0 | 1 | 8.70 |
| CHEMBL514138 | CGS-27023A | — | 1 | 8.36 |
| CHEMBL115653 | CIPEMASTAT | 2.0 | 1 | 8.33 |
| CHEMBL466237 | — | — | 1 | 8.15 |
| CHEMBL512081 | — | — | 1 | 8.05 |
| CHEMBL468101 | — | — | 1 | 8.01 |
| CHEMBL253680 | — | — | 1 | 7.96 |
| CHEMBL512061 | — | — | 1 | 7.92 |
| CHEMBL466249 | — | — | 1 | 7.87 |
| CHEMBL466024 | — | — | 1 | 7.84 |
| CHEMBL466052 | — | — | 1 | 7.71 |
| CHEMBL494167 | — | — | 1 | 7.70 |
| CHEMBL467687 | — | — | 1 | 7.60 |
| CHEMBL512613 | — | — | 1 | 7.60 |
| CHEMBL466059 | — | — | 1 | 7.42 |
| CHEMBL466045 | — | — | 1 | 7.33 |
| CHEMBL511895 | — | — | 1 | 7.32 |
| CHEMBL466060 | — | — | 1 | 7.24 |
| CHEMBL469138 | — | — | 1 | 7.22 |
| CHEMBL468731 | — | — | 1 | 7.22 |
| CHEMBL466656 | — | — | 1 | 7.20 |
| CHEMBL513655 | — | — | 1 | 7.19 |
| CHEMBL493989 | — | — | 1 | 7.19 |
| CHEMBL499159 | — | — | 1 | 7.17 |
| CHEMBL467257 | — | — | 1 | 7.14 |
| CHEMBL492384 | — | — | 1 | 7.10 |
| CHEMBL512275 | — | — | 1 | 7.09 |
| CHEMBL468096 | — | — | 1 | 7.05 |
| CHEMBL468737 | — | — | 1 | 7.00 |
| CHEMBL467262 | — | — | 1 | 6.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL440498 | CTS-1027 | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL514138 | CGS-27023A | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL115653 | CIPEMASTAT | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL466237 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL512081 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL468101 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL253680 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL512061 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL466249 | — | IC50 | = | 13.5 | nM | 7.87 |
| CHEMBL466024 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL466052 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL494167 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL467687 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL512613 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL466059 | — | IC50 | = | 37.8 | nM | 7.42 |
| CHEMBL466045 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL511895 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL466060 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL469138 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL468731 | — | IC50 | = | 60.6 | nM | 7.22 |
| CHEMBL466656 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL513655 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL493989 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL499159 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL467257 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL492384 | — | IC50 | = | 79.5 | nM | 7.10 |
| CHEMBL512275 | — | IC50 | = | 81.2 | nM | 7.09 |
| CHEMBL468096 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL468737 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL467262 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL513645 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL512237 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL466657 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL468095 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL466445 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL492383 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL511433 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL494824 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL466460 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL493177 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL467482 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL513823 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL493178 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL493179 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL512243 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL468739 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL466461 | — | IC50 | = | 325.0 | nM | 6.49 |
| CHEMBL466208 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL494823 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL467459 | — | IC50 | = | 1160.0 | nM | 5.94 |