Assay Detail
Binding
CHEMBL2066798
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MMP9 using (7-methoxycoumarin-4-yl)acetyl-Pro-Leu-Gly-Leu-(3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl)Ala-Arg-NH2 as substrate incubated for 30 mins prior to substrate addition measured for 10 mins by fluorometry
17
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A new class of highly potent matrix metalloproteinase inhibitors based on triazole-substituted hydroxamates: (radio)synthesis and in vitro and first in vivo evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.86 | 10.52 |
| Ki | 1 | 7.57 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2064547 | — | — | 1 | 10.52 |
| CHEMBL2064549 | — | — | 1 | 10.30 |
| CHEMBL2064548 | — | — | 1 | 10.22 |
| CHEMBL2064542 | — | — | 1 | 9.43 |
| CHEMBL2064552 | — | — | 1 | 9.22 |
| CHEMBL2064541 | — | — | 1 | 9.22 |
| CHEMBL2064550 | — | — | 1 | 9.05 |
| CHEMBL2064545 | — | — | 1 | 8.70 |
| CHEMBL2064544 | — | — | 1 | 8.52 |
| CHEMBL2064551 | — | — | 1 | 8.40 |
| CHEMBL2064540 | — | — | 1 | 8.30 |
| CHEMBL514138 | CGS-27023A | — | 1 | 8.22 |
| CHEMBL2064546 | — | — | 1 | 8.15 |
| CHEMBL85030 | — | — | 1 | 7.57 |
| CHEMBL2064543 | — | — | 1 | 7.37 |
| CHEMBL429800 | — | — | 1 | 7.30 |
| CHEMBL2064553 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2064547 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL2064549 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL2064548 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL2064542 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL2064552 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL2064541 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL2064550 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL2064545 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2064544 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2064551 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2064540 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL514138 | CGS-27023A | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2064546 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL85030 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL2064543 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL429800 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2064553 | — | IC50 | > | 100000.0 | nM | - |