Assay Detail
Binding
CHEMBL5032447
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant thrombin (unknown origin) using D-Phe-Pip-Arg-pNA as substrate preincubated for 30 mins followed by substrate addition by chromogenic 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 |
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 | 5.45 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5092327 | — | — | 1 | 7.47 |
| CHEMBL5075134 | — | — | 1 | 5.96 |
| CHEMBL5091873 | — | — | 1 | 5.10 |
| CHEMBL5081508 | — | — | 1 | 5.09 |
| CHEMBL5074750 | — | — | 1 | 5.05 |
| CHEMBL5091091 | — | — | 1 | 4.77 |
| CHEMBL5086585 | — | — | 1 | 4.73 |
| CHEMBL5083517 | — | — | 1 | - |
| CHEMBL5081575 | — | — | 1 | - |
| CHEMBL5081335 | — | — | 1 | - |
| CHEMBL5081090 | — | — | 1 | - |
| CHEMBL5077855 | — | — | 1 | - |
| CHEMBL5075263 | — | — | 1 | - |
| CHEMBL5078472 | — | — | 1 | - |
| CHEMBL5091578 | — | — | 1 | - |
| CHEMBL5088958 | — | — | 1 | - |
| CHEMBL5081851 | — | — | 1 | - |
| CHEMBL5084226 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5092327 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5075134 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL5091873 | — | IC50 | = | 7939.0 | nM | 5.10 |
| CHEMBL5081508 | — | IC50 | = | 8140.0 | nM | 5.09 |
| CHEMBL5074750 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL5091091 | — | IC50 | = | 17100.0 | nM | 4.77 |
| CHEMBL5086585 | — | IC50 | = | 18456.0 | nM | 4.73 |
| CHEMBL5083517 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5081575 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5081335 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5081090 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL5077855 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL5075263 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5078472 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL5091578 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL5088958 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL5081851 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL5084226 | — | IC50 | > | 200000.0 | nM | - |