Assay Detail
Binding
CHEMBL5553697
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Binding affinity to recombinant human TMPRSS6 using Boc-QAR-AMC as substrate assessed as inhibition constant by fluorescence based analysis
14
Total Activities
14
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
Rational <i>In Silico</i> Design of Selective TMPRSS6 Peptidomimetic Inhibitors via Exploitation of the S2 Subpocket.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.50 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5562941 | — | — | 1 | 8.92 |
| CHEMBL4081543 | — | — | 1 | 8.92 |
| CHEMBL5590035 | — | — | 1 | 8.85 |
| CHEMBL5573803 | — | — | 1 | 8.85 |
| CHEMBL5574204 | — | — | 1 | 8.82 |
| CHEMBL5575948 | — | — | 1 | 8.66 |
| CHEMBL5569457 | — | — | 1 | 8.47 |
| CHEMBL5571372 | — | — | 1 | 8.43 |
| CHEMBL5569773 | — | — | 1 | 8.41 |
| CHEMBL5592173 | — | — | 1 | 8.34 |
| CHEMBL5595012 | — | — | 1 | 8.25 |
| CHEMBL5574444 | — | — | 1 | 8.10 |
| CHEMBL5566155 | — | — | 1 | 8.08 |
| CHEMBL5596033 | — | — | 1 | 7.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5562941 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL4081543 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL5590035 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL5573803 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL5574204 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL5575948 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL5569457 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL5571372 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL5569773 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL5592173 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL5595012 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL5574444 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL5566155 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL5596033 | — | Ki | = | 12.5 | nM | 7.90 |