Assay Detail
Binding
CHEMBL4372252
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of enterokinase activated recombinant mouse C-terminal His6-tagged KLK7 (Gln22 to Arg249 residues) using MOCAc-Arg-Pro-Lys-Pro-Val-Glu-Nva-Trp-Arg-Lys(Dnp)-NH2 as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence analysis
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and structure-activity relationship of imidazolinylindole derivatives as kallikrein 7 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.30 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4554224 | — | — | 1 | 6.40 |
| CHEMBL4517387 | — | — | 1 | 5.89 |
| CHEMBL4575145 | — | — | 1 | 5.82 |
| CHEMBL4467792 | — | — | 1 | 5.19 |
| CHEMBL4444444 | — | — | 1 | 5.00 |
| CHEMBL4528949 | — | — | 1 | 5.00 |
| CHEMBL4557205 | — | — | 1 | 4.96 |
| CHEMBL4520107 | — | — | 1 | 4.82 |
| CHEMBL4438568 | — | — | 1 | 4.66 |
| CHEMBL4567825 | — | — | 1 | - |
| CHEMBL4442779 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4554224 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4517387 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4575145 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4467792 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL4444444 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4528949 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4557205 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4520107 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4438568 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL4567825 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4442779 | — | IC50 | > | 30000.0 | nM | - |