Assay Detail
Binding
CHEMBL4372250
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of thermolysin activated recombinant human C-terminal 10-His tagged KLK7 (E23 to H252 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
21
Total Activities
21
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
Discovery and structure-activity relationship of imidazolinylindole derivatives as kallikrein 7 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 5.16 | 6.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4554224 | — | — | 1 | 6.41 |
| CHEMBL4517387 | — | — | 1 | 6.00 |
| CHEMBL4575145 | — | — | 1 | 5.92 |
| CHEMBL4567825 | — | — | 1 | 5.72 |
| CHEMBL4467792 | — | — | 1 | 5.39 |
| CHEMBL4453721 | — | — | 1 | 5.33 |
| CHEMBL4572471 | — | — | 1 | 5.24 |
| CHEMBL4557205 | — | — | 1 | 5.17 |
| CHEMBL4442779 | — | — | 1 | 5.03 |
| CHEMBL4566954 | — | — | 1 | 5.00 |
| CHEMBL4438568 | — | — | 1 | 4.96 |
| CHEMBL4528949 | — | — | 1 | 4.85 |
| CHEMBL4520107 | — | — | 1 | 4.77 |
| CHEMBL4567713 | — | — | 1 | 4.66 |
| CHEMBL4571184 | — | — | 1 | 4.62 |
| CHEMBL4444444 | — | — | 1 | 4.52 |
| CHEMBL4540373 | — | — | 1 | 4.16 |
| CHEMBL4549943 | — | — | 1 | - |
| CHEMBL4577042 | — | — | 1 | - |
| CHEMBL4535920 | — | — | 1 | - |
| CHEMBL4438651 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4554224 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4517387 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4575145 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4567825 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4467792 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4453721 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4572471 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4557205 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL4442779 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL4566954 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4438568 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4528949 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4520107 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4567713 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL4571184 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL4444444 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL4540373 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL4549943 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4577042 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4535920 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4438651 | — | IC50 | > | 30000.0 | nM | - |