Assay Detail
ADMET
CHEMBL4400467
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal Met and 6-His-tagged matriptase (G596 to V855 residues) expressed in Escherichia coli using Boc-QAR-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 | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Suppressor of tumorigenicity 14 protein (CHEMBL3018) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 5.24 | 7.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4517343 | — | — | 1 | 7.90 |
| CHEMBL4460168 | — | — | 1 | 5.90 |
| CHEMBL4558285 | — | — | 1 | 5.90 |
| CHEMBL4447752 | — | — | 1 | 5.70 |
| CHEMBL4465265 | — | — | 1 | 5.70 |
| CHEMBL4579813 | — | — | 1 | 5.20 |
| CHEMBL4535907 | — | — | 1 | 5.10 |
| CHEMBL4436048 | — | — | 1 | 5.10 |
| CHEMBL4543039 | — | — | 1 | 5.00 |
| CHEMBL4461533 | — | — | 1 | 4.80 |
| CHEMBL4536142 | — | — | 1 | 4.60 |
| CHEMBL4547455 | — | — | 1 | 4.60 |
| CHEMBL4473069 | — | — | 1 | 4.50 |
| CHEMBL4448315 | — | — | 1 | 4.40 |
| CHEMBL4464120 | — | — | 1 | 4.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4517343 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4460168 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4558285 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4447752 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4465265 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4579813 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL4535907 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4436048 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4543039 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4461533 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL4536142 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL4547455 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL4473069 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL4448315 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL4464120 | — | IC50 | = | 63095.73 | nM | 4.20 |