Assay Detail
Binding
CHEMBL3772516
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Inhibition of human recombinant KLK4 expressed in Escherichia coli using Bachem I-1120 as substrate preincubated for 15 mins followed by substrate addition by microplate reader analysis
11
Total Activities
11
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
The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.53 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1184949 | — | — | 1 | 8.47 |
| CHEMBL239535 | — | — | 1 | 7.92 |
| CHEMBL238913 | — | — | 1 | 7.82 |
| CHEMBL239331 | — | — | 1 | 7.40 |
| CHEMBL238707 | — | — | 1 | 7.39 |
| CHEMBL3770794 | — | — | 1 | 7.10 |
| CHEMBL3771081 | — | — | 1 | 6.60 |
| CHEMBL3769636 | — | — | 1 | - |
| CHEMBL3771195 | — | — | 1 | - |
| CHEMBL3770879 | — | — | 1 | - |
| CHEMBL1179439 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1184949 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL239535 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL238913 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL239331 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL238707 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3770794 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3771081 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3769636 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3771195 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3770879 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1179439 | — | IC50 | > | 2500.0 | nM | - |