Assay Detail
Binding
CHEMBL4400465
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human C-terminal 10-His-tagged KLK8 (Gln29 to Gly260 residues) expressed in mouse NS0 cells using BOC-VPR-AMC as substrate incubated for 40 mins by FLINT assay
15
Total Activities
15
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
Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.30 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4558285 | — | — | 1 | 8.20 |
| CHEMBL4447752 | — | — | 1 | 7.60 |
| CHEMBL4465265 | — | — | 1 | 7.50 |
| CHEMBL4517343 | — | — | 1 | 7.00 |
| CHEMBL4436048 | — | — | 1 | 6.70 |
| CHEMBL4535907 | — | — | 1 | 6.60 |
| CHEMBL4461533 | — | — | 1 | 6.60 |
| CHEMBL4543039 | — | — | 1 | 6.50 |
| CHEMBL4579813 | — | — | 1 | 6.40 |
| CHEMBL4460168 | — | — | 1 | 5.80 |
| CHEMBL4473069 | — | — | 1 | 5.70 |
| CHEMBL4464120 | — | — | 1 | 5.10 |
| CHEMBL4536142 | — | — | 1 | 5.00 |
| CHEMBL4448315 | — | — | 1 | 4.90 |
| CHEMBL4547455 | — | — | 1 | 4.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4558285 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4447752 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4465265 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4517343 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4436048 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4535907 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4461533 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4543039 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4579813 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4460168 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4473069 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4464120 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4536142 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4448315 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL4547455 | — | IC50 | = | 12589.25 | nM | 4.90 |