Assay Detail
Binding
CHEMBL3748443
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Inhibition of human recombinant hepsin using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition measured for 15 to 120 mins by plate reader analysis
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 | Autocuration |
Publication
Structure-based design, synthesis, and biological evaluation of Leu-Arg dipeptide analogs as novel hepsin inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.47 | 9.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3745775 | — | — | 1 | 9.08 |
| CHEMBL3747482 | — | — | 1 | 8.98 |
| CHEMBL3356589 | — | — | 1 | 8.84 |
| CHEMBL3747468 | — | — | 1 | 8.54 |
| CHEMBL3746517 | — | — | 1 | 8.54 |
| CHEMBL404190 | — | — | 1 | 8.47 |
| CHEMBL3747618 | — | — | 1 | 7.67 |
| CHEMBL3747575 | — | — | 1 | 7.65 |
| CHEMBL3747752 | — | — | 1 | - |
| CHEMBL3746062 | — | — | 1 | - |
| CHEMBL3746635 | — | — | 1 | - |
| CHEMBL3747693 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3745775 | — | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL3747482 | — | Ki | = | 1.04 | nM | 8.98 |
| CHEMBL3356589 | — | Ki | = | 1.45 | nM | 8.84 |
| CHEMBL3747468 | — | Ki | = | 2.88 | nM | 8.54 |
| CHEMBL3746517 | — | Ki | = | 2.91 | nM | 8.54 |
| CHEMBL404190 | — | Ki | = | 3.38 | nM | 8.47 |
| CHEMBL3747618 | — | Ki | = | 21.5 | nM | 7.67 |
| CHEMBL3747575 | — | Ki | = | 22.4 | nM | 7.65 |
| CHEMBL3747752 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3746062 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3746635 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3747693 | — | Ki | > | 10000.0 | nM | - |