Assay Detail
Binding
CHEMBL5032465
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human HGFA serine protease domain using Boc-QLR-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 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Hepatocyte growth factor activator (CHEMBL3351190) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 5.36 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5074750 | — | — | 1 | 7.58 |
| CHEMBL5084226 | — | — | 1 | 5.74 |
| CHEMBL5075134 | — | — | 1 | 5.50 |
| CHEMBL5086585 | — | — | 1 | 5.49 |
| CHEMBL5081090 | — | — | 1 | 5.37 |
| CHEMBL5083517 | — | — | 1 | 5.35 |
| CHEMBL5081575 | — | — | 1 | 5.30 |
| CHEMBL5092327 | — | — | 1 | 5.27 |
| CHEMBL5081508 | — | — | 1 | 5.07 |
| CHEMBL5088958 | — | — | 1 | 4.93 |
| CHEMBL5091091 | — | — | 1 | 4.92 |
| CHEMBL5077855 | — | — | 1 | 4.86 |
| CHEMBL5078472 | — | — | 1 | 4.80 |
| CHEMBL5091578 | — | — | 1 | 4.79 |
| CHEMBL5091873 | — | — | 1 | - |
| CHEMBL5081335 | — | — | 1 | - |
| CHEMBL5081851 | — | — | 1 | - |
| CHEMBL5075263 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5074750 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5084226 | — | IC50 | = | 1832.0 | nM | 5.74 |
| CHEMBL5075134 | — | IC50 | = | 3173.0 | nM | 5.50 |
| CHEMBL5086585 | — | IC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL5081090 | — | IC50 | = | 4312.0 | nM | 5.37 |
| CHEMBL5083517 | — | IC50 | = | 4466.0 | nM | 5.35 |
| CHEMBL5081575 | — | IC50 | = | 5046.0 | nM | 5.30 |
| CHEMBL5092327 | — | IC50 | = | 5378.0 | nM | 5.27 |
| CHEMBL5081508 | — | IC50 | = | 8610.0 | nM | 5.07 |
| CHEMBL5088958 | — | IC50 | = | 11777.0 | nM | 4.93 |
| CHEMBL5091091 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL5077855 | — | IC50 | = | 13705.0 | nM | 4.86 |
| CHEMBL5078472 | — | IC50 | = | 15837.0 | nM | 4.80 |
| CHEMBL5091578 | — | IC50 | = | 16108.0 | nM | 4.79 |
| CHEMBL5091873 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5081335 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5081851 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5075263 | — | IC50 | > | 20000.0 | nM | - |