Assay Detail
Binding
CHEMBL4372230
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human proMMP2 using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate preincubated for 3 hrs followed by substrate addition and measured every 10 secs for 15 mins in presence of APMA by fluorometric assay
7
Total Activities
7
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
Design, synthesis and biological evaluation of bifunctional inhibitors of membrane type 1 matrix metalloproteinase (MT1-MMP).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.56 | 9.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3617407 | — | — | 1 | 9.17 |
| CHEMBL1090647 | — | — | 1 | 9.15 |
| CHEMBL4442617 | — | — | 1 | 8.92 |
| CHEMBL4466038 | — | — | 1 | 8.80 |
| CHEMBL4584813 | — | — | 1 | 8.39 |
| CHEMBL4518217 | — | — | 1 | 7.89 |
| CHEMBL267178 | — | — | 1 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3617407 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL1090647 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4442617 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4466038 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4584813 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4518217 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL267178 | — | IC50 | = | 25.0 | nM | 7.60 |