Assay Detail
Binding
CHEMBL5032467
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human C-terminal 10-His tagged hepsin (Arg45 to Leu417) expressed in mouse myeloma cells using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition by fluorescence based assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Multiple myeloma cancer stem cell |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Macrocyclic Inhibitors of HGF-Activating Serine Proteases Overcome Resistance to Receptor Tyrosine Kinase Inhibitors and Block Lung Cancer Progression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.14 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5081575 | — | — | 1 | 10.10 |
| CHEMBL5074750 | — | — | 1 | 9.42 |
| CHEMBL5083517 | — | — | 1 | 8.77 |
| CHEMBL5092327 | — | — | 1 | 8.27 |
| CHEMBL5088958 | — | — | 1 | 8.24 |
| CHEMBL5086585 | — | — | 1 | 8.23 |
| CHEMBL5081090 | — | — | 1 | 8.23 |
| CHEMBL5084226 | — | — | 1 | 8.11 |
| CHEMBL5081335 | — | — | 1 | 8.08 |
| CHEMBL5077855 | — | — | 1 | 8.06 |
| CHEMBL5078472 | — | — | 1 | 8.00 |
| CHEMBL5081508 | — | — | 1 | 7.96 |
| CHEMBL5091091 | — | — | 1 | 7.82 |
| CHEMBL5075134 | — | — | 1 | 7.77 |
| CHEMBL5091578 | — | — | 1 | 7.66 |
| CHEMBL5075263 | — | — | 1 | 7.60 |
| CHEMBL5081851 | — | — | 1 | 7.36 |
| CHEMBL5091873 | — | — | 1 | 6.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5081575 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL5074750 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL5083517 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5092327 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL5088958 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5086585 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL5081090 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL5084226 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL5081335 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL5077855 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL5078472 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5081508 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5091091 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5075134 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5091578 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5075263 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5081851 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5091873 | — | IC50 | = | 136.0 | nM | 6.87 |