Assay Detail
Binding
CHEMBL5140187
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Inhibition of C-terminal poly-His-tagged human recombinant KLK7 (30 to 253 residues) transfected in CHO cells assessed as inhibition constant using KHLY-pNA as fluorogenic substrate incubated for 30 mins by fluorescence plate reader assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Phage Display Selected Cyclic Peptide Inhibitors of Kallikrein-Related Peptidases 5 and 7 and Their <i>In Vivo</i> Delivery to the Skin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 7.41 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5185665 | — | — | 1 | 8.15 |
| CHEMBL5198206 | — | — | 1 | 8.06 |
| CHEMBL5173572 | — | — | 1 | 8.05 |
| CHEMBL5173148 | — | — | 1 | 8.00 |
| CHEMBL5179139 | — | — | 1 | 7.92 |
| CHEMBL5204039 | — | — | 1 | 7.80 |
| CHEMBL5189873 | — | — | 1 | 7.76 |
| CHEMBL5191378 | — | — | 1 | 7.72 |
| CHEMBL5185516 | — | — | 1 | 7.54 |
| CHEMBL5175658 | — | — | 1 | 7.53 |
| CHEMBL5204199 | — | — | 1 | 7.51 |
| CHEMBL5177855 | — | — | 1 | 7.50 |
| CHEMBL5177530 | — | — | 1 | 7.44 |
| CHEMBL5180009 | — | — | 1 | 7.30 |
| CHEMBL5177117 | — | — | 1 | 7.28 |
| CHEMBL5191079 | — | — | 1 | 7.28 |
| CHEMBL5175954 | — | — | 1 | 7.18 |
| CHEMBL5192988 | — | — | 1 | 7.05 |
| CHEMBL5190884 | — | — | 1 | 7.03 |
| CHEMBL5172075 | — | — | 1 | 7.02 |
| CHEMBL5183937 | — | — | 1 | 6.97 |
| CHEMBL5194521 | — | — | 1 | 6.70 |
| CHEMBL5206546 | — | — | 1 | 6.66 |
| CHEMBL5207509 | — | — | 1 | 6.36 |
| CHEMBL5185478 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5185665 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL5198206 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL5173572 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL5173148 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL5179139 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5204039 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL5189873 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL5191378 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL5185516 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL5175658 | — | Ki | = | 29.4 | nM | 7.53 |
| CHEMBL5204199 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL5177855 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL5177530 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL5180009 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL5177117 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL5191079 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL5175954 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL5192988 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL5190884 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL5172075 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL5183937 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL5194521 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL5206546 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL5207509 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL5185478 | — | Ki | > | 1000.0 | nM | - |