Assay Detail
Binding
CHEMBL4189735
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human MMP-12 using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate preincubated for 3 hrs followed by substrate addition measured every 10 secs for 15 mins by fluorometric assay
16
Total Activities
16
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
Development of Thioaryl-Based Matrix Metalloproteinase-12 Inhibitors with Alternative Zinc-Binding Groups: Synthesis, Potentiometric, NMR, and Crystallographic Studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.73 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4210206 | — | — | 1 | 8.40 |
| CHEMBL584365 | — | — | 1 | 8.32 |
| CHEMBL4209100 | — | — | 1 | 7.58 |
| CHEMBL4203044 | — | — | 1 | 7.48 |
| CHEMBL4214269 | — | — | 1 | 7.40 |
| CHEMBL4214626 | — | — | 1 | 7.40 |
| CHEMBL573936 | — | — | 1 | 6.85 |
| CHEMBL4206329 | — | — | 1 | 6.60 |
| CHEMBL4213983 | — | — | 1 | 6.29 |
| CHEMBL4218036 | — | — | 1 | 6.22 |
| CHEMBL4212208 | — | — | 1 | 5.68 |
| CHEMBL4207046 | — | — | 1 | 5.48 |
| CHEMBL4213651 | — | — | 1 | 5.46 |
| CHEMBL4216008 | — | — | 1 | 5.12 |
| CHEMBL4202548 | — | — | 1 | - |
| CHEMBL4206259 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4210206 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL584365 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4209100 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4203044 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4214269 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4214626 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL573936 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4206329 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4213983 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4218036 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4212208 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4207046 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4213651 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4216008 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL4202548 | — | IC50 | = | 230000.0 | nM | - |
| CHEMBL4206259 | — | IC50 | > | 10000.0 | nM | - |