Assay Detail
Binding
CHEMBL2175124
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant cathepsin-k using Z-Phe-Arg-AMC as substrate preincubated for 15 mins measured after 1 hr by QFRET assay
28
Total Activities
28
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
Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.86 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2172003 | — | — | 1 | 8.52 |
| CHEMBL2172005 | — | — | 1 | 8.40 |
| CHEMBL2172002 | — | — | 1 | 8.30 |
| CHEMBL2171986 | — | — | 1 | 8.22 |
| CHEMBL2171988 | — | — | 1 | 8.22 |
| CHEMBL2172006 | — | — | 1 | 8.22 |
| CHEMBL2164676 | — | — | 1 | 8.15 |
| CHEMBL2172000 | — | — | 1 | 8.10 |
| CHEMBL2171987 | — | — | 1 | 8.10 |
| CHEMBL2171999 | — | — | 1 | 8.05 |
| CHEMBL2172004 | — | — | 1 | 8.05 |
| CHEMBL2171993 | — | — | 1 | 8.05 |
| CHEMBL2172007 | — | — | 1 | 7.96 |
| CHEMBL2171990 | — | — | 1 | 7.96 |
| CHEMBL2171985 | — | — | 1 | 7.96 |
| CHEMBL2171995 | — | — | 1 | 7.92 |
| CHEMBL2171992 | — | — | 1 | 7.85 |
| CHEMBL2070936 | — | — | 1 | 7.82 |
| CHEMBL2171991 | — | — | 1 | 7.82 |
| CHEMBL2169908 | — | — | 1 | 7.80 |
| CHEMBL2172001 | — | — | 1 | 7.77 |
| CHEMBL2171994 | — | — | 1 | 7.75 |
| CHEMBL2171984 | — | — | 1 | 7.64 |
| CHEMBL2171989 | — | — | 1 | 7.60 |
| CHEMBL2172126 | — | — | 1 | 7.35 |
| CHEMBL2171996 | — | — | 1 | 7.23 |
| CHEMBL2171997 | — | — | 1 | 6.68 |
| CHEMBL2171998 | — | — | 1 | 6.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2172003 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2172005 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2172002 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2171986 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2171988 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2172006 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2164676 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2172000 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2171987 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2171999 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2172004 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2171993 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2172007 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2171990 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2171985 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2171995 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2171992 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2070936 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2171991 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2169908 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2172001 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2171994 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2171984 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2171989 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2172126 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL2171996 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL2171997 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL2171998 | — | IC50 | = | 312.0 | nM | 6.51 |