Assay Detail
Binding
CHEMBL709097
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Inhibition of human fibroblast collagenase, matrix metalloprotease-1
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design, synthesis, activity, and structure of a novel class of matrix metalloproteinase inhibitors containing a heterocyclic P2-P3 amide bond isostere
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.50 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL40351 | — | — | 1 | 8.52 |
| CHEMBL288649 | — | — | 1 | 8.22 |
| CHEMBL288896 | — | — | 1 | 8.16 |
| CHEMBL289513 | — | — | 1 | 8.15 |
| CHEMBL298033 | — | — | 1 | 8.05 |
| CHEMBL43403 | — | — | 1 | 7.75 |
| CHEMBL40589 | — | — | 1 | 7.66 |
| CHEMBL296874 | — | — | 1 | 7.54 |
| CHEMBL42311 | — | — | 1 | 7.40 |
| CHEMBL40237 | — | — | 1 | 6.77 |
| CHEMBL41497 | — | — | 1 | 6.32 |
| CHEMBL289842 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL40351 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL288649 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL288896 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL289513 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL298033 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL43403 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL40589 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL296874 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL42311 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL40237 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL41497 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL289842 | — | IC50 | = | 3500.0 | nM | 5.46 |