Assay Detail
Binding
CHEMBL833001
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory concentration against human cathepsin K using 10 uM Cbz-Phe-Arg-AMC
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Novel and potent cyclic cyanamide-based cathepsin K inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.43 | 10.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183812 | — | — | 1 | 10.32 |
| CHEMBL114462 | — | — | 1 | 9.89 |
| CHEMBL180839 | — | — | 1 | 8.74 |
| CHEMBL116402 | — | — | 1 | 8.57 |
| CHEMBL369080 | — | — | 1 | 8.05 |
| CHEMBL183660 | — | — | 1 | 7.92 |
| CHEMBL183658 | — | — | 1 | 7.72 |
| CHEMBL362589 | — | — | 1 | 7.29 |
| CHEMBL183670 | — | — | 1 | 7.22 |
| CHEMBL2096777 | — | — | 1 | 7.09 |
| CHEMBL2096698 | — | — | 1 | 6.70 |
| CHEMBL182578 | — | — | 1 | 6.70 |
| CHEMBL182832 | — | — | 1 | 6.52 |
| CHEMBL361185 | — | — | 1 | 6.42 |
| CHEMBL183446 | — | — | 1 | 6.37 |
| CHEMBL262697 | CYANO-PYRROLIDINE | — | 1 | 5.68 |
| CHEMBL182143 | — | — | 1 | 5.09 |
| CHEMBL434529 | — | — | 1 | - |
| CHEMBL369564 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183812 | — | IC50 | = | 0.048 | nM | 10.32 |
| CHEMBL114462 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL180839 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL116402 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL369080 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL183660 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL183658 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL362589 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL183670 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2096777 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL2096698 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL182578 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL182832 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL361185 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL183446 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL262697 | CYANO-PYRROLIDINE | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL182143 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL434529 | — | IC50 | > | 1300.0 | nM | - |
| CHEMBL369564 | — | IC50 | > | 1300.0 | nM | - |