Assay Detail
Binding
CHEMBL3373430
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant MMP2 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay
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
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 8.27 | 10.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL440498 | CTS-1027 | 2.0 | 1 | 10.54 |
| CHEMBL3337894 | T-26c | — | 1 | 7.75 |
| CHEMBL3337869 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL440498 | CTS-1027 | IC50 | = | 0.029 | nM | 10.54 |
| CHEMBL3337894 | T-26c | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3337869 | — | IC50 | = | 300.0 | nM | 6.52 |