Assay Detail
Binding
CHEMBL3588573
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human active MMP2 using (7-methoxycoumarin-4-yl) acetyl pro-Leu-Gly-Leu-[3-(2,4-dinitrophenyl)-L-2,3-diamino-propionyl]-Ala-Arg-NH2 fluorogenic substrate assessed as fluorescent product release
18
Total Activities
18
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
New matrix metalloproteinase inhibitors based on γ-fluorinated α-aminocarboxylic and α-aminohydroxamic acids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.88 | 8.70 |
| Ki | 2 | 7.83 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3585761 | — | — | 1 | 8.70 |
| CHEMBL3585769 | — | — | 1 | 8.41 |
| CHEMBL3585770 | — | — | 1 | 8.20 |
| CHEMBL3585765 | — | — | 1 | 8.19 |
| CHEMBL3585774 | — | — | 1 | 8.14 |
| CHEMBL3585773 | — | — | 1 | 8.03 |
| CHEMBL85030 | — | — | 1 | 7.96 |
| CHEMBL514138 | CGS-27023A | — | 1 | 7.70 |
| CHEMBL3585766 | — | — | 1 | 7.48 |
| CHEMBL3585762 | — | — | 1 | 5.85 |
| CHEMBL3585767 | — | — | 1 | 5.68 |
| CHEMBL3585759 | — | — | 1 | 4.99 |
| CHEMBL3585764 | — | — | 1 | 4.46 |
| CHEMBL3585771 | — | — | 1 | 4.45 |
| CHEMBL3585768 | — | — | 1 | - |
| CHEMBL3585772 | — | — | 1 | - |
| CHEMBL3585763 | — | — | 1 | - |
| CHEMBL3585760 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3585761 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3585769 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3585770 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3585765 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL3585774 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL3585773 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL85030 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL514138 | CGS-27023A | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL3585766 | — | IC50 | = | 32.8 | nM | 7.48 |
| CHEMBL3585762 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3585767 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3585759 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL3585764 | — | IC50 | = | 34700.0 | nM | 4.46 |
| CHEMBL3585771 | — | IC50 | = | 35700.0 | nM | 4.45 |
| CHEMBL3585768 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3585772 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3585763 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3585760 | — | IC50 | > | 100000.0 | nM | - |