Assay Detail
Binding
CHEMBL3388709
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Inhibition of human recombinant MMP2 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.45 | 10.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL440498 | CTS-1027 | 2.0 | 1 | 10.54 |
| CHEMBL3337869 | — | — | 1 | 6.52 |
| CHEMBL3359091 | — | — | 1 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL440498 | CTS-1027 | IC50 | = | 0.029 | nM | 10.54 |
| CHEMBL3337869 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3359091 | — | IC50 | = | 5300.0 | nM | 5.28 |