Assay Detail
Binding
CHEMBL2187699
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive inhibition of human recombinant PACE4 expressed in Drosophila S2 cells using pyroGlu-Arg-Val-Lys-Arg-methyl-coumaryl-7-amide as substrate at pH 6.5 after 60 mins by spectrofluorometric analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | S2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Proprotein convertase subtilisin/kexin type 6 (CHEMBL2951) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The Multi-Leu peptide inhibitor discriminates between PACE4 and furin and exhibits antiproliferative effects on prostate cancer cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.63 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2179430 | — | — | 1 | 9.47 |
| CHEMBL2179835 | — | — | 1 | 9.40 |
| CHEMBL2179836 | — | — | 1 | 8.96 |
| CHEMBL2179429 | — | — | 1 | 8.89 |
| CHEMBL2179431 | — | — | 1 | 8.70 |
| CHEMBL2179428 | — | — | 1 | 8.15 |
| CHEMBL2179434 | — | — | 1 | 7.75 |
| CHEMBL2179832 | — | — | 1 | 7.72 |
| CHEMBL2179435 | — | — | 1 | 7.66 |
| CHEMBL2179833 | — | — | 1 | 7.64 |
| CHEMBL2179436 | — | — | 1 | 7.16 |
| CHEMBL2049156 | — | — | 1 | 6.62 |
| CHEMBL2179437 | — | — | 1 | 6.52 |
| CHEMBL2179438 | — | — | 1 | 5.86 |
| CHEMBL2179432 | — | — | 1 | 5.80 |
| CHEMBL2179433 | — | — | 1 | 5.80 |
| CHEMBL2179427 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2179430 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL2179835 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2179836 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL2179429 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL2179431 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2179428 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2179434 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2179832 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL2179435 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2179833 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL2179436 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL2049156 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL2179437 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL2179438 | — | Ki | = | 1380.0 | nM | 5.86 |
| CHEMBL2179432 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL2179433 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL2179427 | — | Ki | > | 1000.0 | nM | - |