Assay Detail
Binding
CHEMBL717441
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50 percent inhibition of human Matrix metalloprotease-13 by the cleavage of fluorogenic peptide MCA-Pro-Leu-Gly-Leu-Dpa-ala-Arg-NH2
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and activity of selective MMP inhibitors with an aryl backbone.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.93 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL75094 | PRINOMASTAT | 3.0 | 1 | 9.30 |
| CHEMBL440498 | CTS-1027 | 2.0 | 1 | 9.22 |
| CHEMBL279785 | MARIMASTAT | 3.0 | 1 | 8.70 |
| CHEMBL309465 | — | — | 1 | 7.91 |
| CHEMBL83209 | — | — | 1 | 7.55 |
| CHEMBL310008 | — | — | 1 | 7.48 |
| CHEMBL94872 | — | — | 1 | 6.28 |
| CHEMBL94467 | — | — | 1 | 6.05 |
| CHEMBL319055 | — | — | 1 | 6.00 |
| CHEMBL330078 | — | — | 1 | 5.70 |
| CHEMBL97478 | — | — | 1 | 5.66 |
| CHEMBL433415 | — | — | 1 | 5.17 |
| CHEMBL94324 | — | — | 1 | 5.05 |
| CHEMBL421372 | — | — | 1 | - |
| CHEMBL94828 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL75094 | PRINOMASTAT | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL440498 | CTS-1027 | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL279785 | MARIMASTAT | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL309465 | — | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL83209 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL310008 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL94872 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL94467 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL319055 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL330078 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL97478 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL433415 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL94324 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL421372 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL94828 | — | IC50 | > | 10000.0 | nM | - |