Assay Detail
Binding
CHEMBL877754
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In vitro inhibitory activity against collagenase-3 (matrix metalloprotease-13).
34
Total Activities
34
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 | 34 | 8.54 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL342172 | — | — | 1 | 9.70 |
| CHEMBL436205 | — | — | 1 | 9.40 |
| CHEMBL140575 | — | — | 1 | 9.30 |
| CHEMBL140970 | — | — | 1 | 9.05 |
| CHEMBL441662 | — | — | 1 | 9.00 |
| CHEMBL141080 | — | — | 1 | 9.00 |
| CHEMBL357233 | — | — | 1 | 9.00 |
| CHEMBL345054 | — | — | 1 | 9.00 |
| CHEMBL341570 | — | — | 1 | 8.89 |
| CHEMBL140511 | — | — | 1 | 8.89 |
| CHEMBL337594 | — | — | 1 | 8.85 |
| CHEMBL124680 | — | — | 1 | 8.77 |
| CHEMBL140788 | — | — | 1 | 8.74 |
| CHEMBL140568 | — | — | 1 | 8.72 |
| CHEMBL343082 | — | — | 1 | 8.68 |
| CHEMBL342210 | — | — | 1 | 8.68 |
| CHEMBL139884 | — | — | 1 | 8.64 |
| CHEMBL2112796 | — | — | 1 | 8.60 |
| CHEMBL334909 | — | — | 1 | 8.57 |
| CHEMBL421932 | — | — | 1 | 8.48 |
| CHEMBL141451 | — | — | 1 | 8.40 |
| CHEMBL342248 | — | — | 1 | 8.37 |
| CHEMBL514138 | CGS-27023A | — | 1 | 8.37 |
| CHEMBL344828 | — | — | 1 | 8.25 |
| CHEMBL140720 | — | — | 1 | 8.12 |
| CHEMBL139886 | — | — | 1 | 8.04 |
| CHEMBL344453 | — | — | 1 | 7.74 |
| CHEMBL2111965 | — | — | 1 | 6.86 |
| CHEMBL1234370 | — | — | 1 | 5.63 |
| CHEMBL140569 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL342172 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL436205 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL140575 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL140970 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL441662 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL141080 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL357233 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL345054 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL341570 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL140511 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL337594 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL124680 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL140788 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL140568 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL342210 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL343082 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL139884 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2112796 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL334909 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL421932 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL141451 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL342248 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL514138 | CGS-27023A | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL344828 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL140720 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL139886 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL344453 | — | IC50 | = | 18.4 | nM | 7.74 |
| CHEMBL2111965 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL1234370 | — | IC50 | = | 2330.0 | nM | 5.63 |
| CHEMBL140569 | — | IC50 | < | 0.4 | nM | - |
| CHEMBL344634 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL75094 | PRINOMASTAT | IC50 | < | 0.4 | nM | - |
| CHEMBL140004 | — | IC50 | < | 0.4 | nM | - |
| CHEMBL344633 | — | IC50 | < | 0.2 | nM | - |