Assay Detail
Binding
CHEMBL715366
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In vitro inhibitory activity against truncated collagenase-1 (matrix metalloprotease-1).
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 7.81 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL141080 | — | — | 1 | 9.40 |
| CHEMBL139886 | — | — | 1 | 9.30 |
| CHEMBL140511 | — | — | 1 | 9.15 |
| CHEMBL140970 | — | — | 1 | 9.10 |
| CHEMBL344633 | — | — | 1 | 9.00 |
| CHEMBL337594 | — | — | 1 | 9.00 |
| CHEMBL334909 | — | — | 1 | 8.92 |
| CHEMBL342210 | — | — | 1 | 8.72 |
| CHEMBL421932 | — | — | 1 | 8.72 |
| CHEMBL341570 | — | — | 1 | 8.72 |
| CHEMBL140569 | — | — | 1 | 8.64 |
| CHEMBL140152 | — | — | 1 | 8.62 |
| CHEMBL344634 | — | — | 1 | 8.54 |
| CHEMBL441662 | — | — | 1 | 8.52 |
| CHEMBL75094 | PRINOMASTAT | 3.0 | 1 | 8.31 |
| CHEMBL140004 | — | — | 1 | 8.24 |
| CHEMBL342248 | — | — | 1 | 7.89 |
| CHEMBL139884 | — | — | 1 | 7.75 |
| CHEMBL436205 | — | — | 1 | 7.72 |
| CHEMBL140720 | — | — | 1 | 7.66 |
| CHEMBL140575 | — | — | 1 | 7.64 |
| CHEMBL344828 | — | — | 1 | 7.38 |
| CHEMBL140788 | — | — | 1 | 7.31 |
| CHEMBL514138 | CGS-27023A | — | 1 | 7.30 |
| CHEMBL357233 | — | — | 1 | 7.30 |
| CHEMBL345054 | — | — | 1 | 7.21 |
| CHEMBL343082 | — | — | 1 | 7.21 |
| CHEMBL140568 | — | — | 1 | 7.19 |
| CHEMBL124680 | — | — | 1 | 6.76 |
| CHEMBL141451 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL141080 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL139886 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL140511 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL140970 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL344633 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL337594 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL334909 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL342210 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL421932 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL341570 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL140569 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL140152 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL344634 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL441662 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL75094 | PRINOMASTAT | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL140004 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL342248 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL139884 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL436205 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL140720 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL140575 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL344828 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL140788 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL514138 | CGS-27023A | IC50 | = | 49.5 | nM | 7.30 |
| CHEMBL357233 | — | IC50 | = | 49.5 | nM | 7.30 |
| CHEMBL345054 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL343082 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL140568 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL124680 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL141451 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL2111965 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL2112796 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL139609 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL343718 | — | IC50 | = | 638.0 | nM | 6.20 |
| CHEMBL344453 | — | IC50 | = | 688.0 | nM | 6.16 |
| CHEMBL1234370 | — | IC50 | = | 7780.0 | nM | 5.11 |
| CHEMBL342172 | — | IC50 | < | 1.0 | nM | - |