Assay Detail
Binding
CHEMBL2175120
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant cathepsin-B using Z-Arg-Arg-AMC as substrate preincubated for 15 mins measured after 1 hr by QFRET assay
26
Total Activities
26
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 | 26 | 5.85 | 6.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2171984 | — | — | 1 | 6.50 |
| CHEMBL2171986 | — | — | 1 | 6.40 |
| CHEMBL2164676 | — | — | 1 | 6.34 |
| CHEMBL2172006 | — | — | 1 | 6.33 |
| CHEMBL2171985 | — | — | 1 | 6.24 |
| CHEMBL2169908 | — | — | 1 | 6.22 |
| CHEMBL2172004 | — | — | 1 | 6.19 |
| CHEMBL2172007 | — | — | 1 | 6.19 |
| CHEMBL2172000 | — | — | 1 | 6.12 |
| CHEMBL2171999 | — | — | 1 | 6.01 |
| CHEMBL2171995 | — | — | 1 | 6.01 |
| CHEMBL2070936 | — | — | 1 | 5.96 |
| CHEMBL2172003 | — | — | 1 | 5.94 |
| CHEMBL2171990 | — | — | 1 | 5.93 |
| CHEMBL2171988 | — | — | 1 | 5.90 |
| CHEMBL2171992 | — | — | 1 | 5.84 |
| CHEMBL2171991 | — | — | 1 | 5.84 |
| CHEMBL2172002 | — | — | 1 | 5.77 |
| CHEMBL2172005 | — | — | 1 | 5.73 |
| CHEMBL2171994 | — | — | 1 | 5.62 |
| CHEMBL2172001 | — | — | 1 | 5.53 |
| CHEMBL2171993 | — | — | 1 | 5.51 |
| CHEMBL2171996 | — | — | 1 | 5.46 |
| CHEMBL2172126 | — | — | 1 | 5.46 |
| CHEMBL2171997 | — | — | 1 | 4.60 |
| CHEMBL2171998 | — | — | 1 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2171984 | — | IC50 | = | 315.0 | nM | 6.50 |
| CHEMBL2171986 | — | IC50 | = | 399.0 | nM | 6.40 |
| CHEMBL2164676 | — | IC50 | = | 455.0 | nM | 6.34 |
| CHEMBL2172006 | — | IC50 | = | 462.0 | nM | 6.33 |
| CHEMBL2171985 | — | IC50 | = | 572.0 | nM | 6.24 |
| CHEMBL2169908 | — | IC50 | = | 603.0 | nM | 6.22 |
| CHEMBL2172004 | — | IC50 | = | 645.0 | nM | 6.19 |
| CHEMBL2172007 | — | IC50 | = | 649.0 | nM | 6.19 |
| CHEMBL2172000 | — | IC50 | = | 766.0 | nM | 6.12 |
| CHEMBL2171999 | — | IC50 | = | 971.0 | nM | 6.01 |
| CHEMBL2171995 | — | IC50 | = | 977.0 | nM | 6.01 |
| CHEMBL2070936 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL2172003 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL2171990 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL2171988 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL2171992 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL2171991 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL2172002 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL2172005 | — | IC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL2171994 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2172001 | — | IC50 | = | 2940.0 | nM | 5.53 |
| CHEMBL2171993 | — | IC50 | = | 3060.0 | nM | 5.51 |
| CHEMBL2171996 | — | IC50 | = | 3430.0 | nM | 5.46 |
| CHEMBL2172126 | — | IC50 | = | 3510.0 | nM | 5.46 |
| CHEMBL2171997 | — | IC50 | = | 24900.0 | nM | 4.60 |
| CHEMBL2171998 | — | IC50 | = | 40000.0 | nM | 4.40 |