Assay Detail
ADMET
CHEMBL4009364
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human matriptase (596 to 855 residues) expressed in Escherichia coli using Boc-Gln-Ala-ArgAMC as substrate measured for 1200 mins by fluorescence assay
29
Total Activities
29
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
Modulating the selectivity of matriptase-2 inhibitors with unnatural amino acids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 7.17 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4081543 | — | — | 1 | 8.40 |
| CHEMBL4103673 | — | — | 1 | 8.25 |
| CHEMBL4093487 | — | — | 1 | 8.15 |
| CHEMBL4089262 | — | — | 1 | 7.92 |
| CHEMBL4085747 | — | — | 1 | 7.72 |
| CHEMBL4101897 | — | — | 1 | 7.70 |
| CHEMBL4085021 | — | — | 1 | 7.70 |
| CHEMBL4083908 | — | — | 1 | 7.58 |
| CHEMBL4065964 | — | — | 1 | 7.55 |
| CHEMBL3354684 | — | — | 1 | 7.50 |
| CHEMBL4103740 | — | — | 1 | 7.47 |
| CHEMBL4099552 | — | — | 1 | 7.47 |
| CHEMBL4093566 | — | — | 1 | 7.41 |
| CHEMBL4091809 | — | — | 1 | 7.37 |
| CHEMBL4065870 | — | — | 1 | 7.36 |
| CHEMBL4062334 | — | — | 1 | 7.32 |
| CHEMBL4104560 | — | — | 1 | 7.29 |
| CHEMBL4070960 | — | — | 1 | 7.20 |
| CHEMBL4100506 | — | — | 1 | 7.19 |
| CHEMBL4073691 | — | — | 1 | 7.15 |
| CHEMBL4073533 | — | — | 1 | 6.92 |
| CHEMBL4084785 | — | — | 1 | 6.92 |
| CHEMBL4074504 | — | — | 1 | 6.82 |
| CHEMBL4086405 | — | — | 1 | 6.70 |
| CHEMBL4101235 | — | — | 1 | 6.64 |
| CHEMBL4063137 | — | — | 1 | 6.62 |
| CHEMBL4084047 | — | — | 1 | 5.86 |
| CHEMBL4080327 | — | — | 1 | 4.92 |
| CHEMBL4094168 | — | — | 1 | 4.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4081543 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4103673 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL4093487 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4089262 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4085747 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4101897 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4085021 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4083908 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL4065964 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL3354684 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL4103740 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL4099552 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL4093566 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL4091809 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL4065870 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL4062334 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL4104560 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL4070960 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL4100506 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL4073691 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL4073533 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4084785 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4074504 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL4086405 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL4101235 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL4063137 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL4084047 | — | Ki | = | 1380.0 | nM | 5.86 |
| CHEMBL4080327 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL4094168 | — | Ki | = | 15000.0 | nM | 4.82 |