| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Cathepsin S |
|---|
| Ligand | BDBM19858 |
|---|
| Substrate/Competitor | BDBM19490 |
|---|
| Meas. Tech. | Enzyme Inhibition Assay and Whole Cell Enzyme Occupancy Assay |
|---|
| pH | 6.5±n/a |
|---|
| Temperature | 295.15±n/a K |
|---|
| IC50 | 52000±6000 nM |
|---|
| EC50 | 4800±2600 nM |
|---|
| Citation |  Falgueyret, JP; Desmarais, S; Oballa, R; Black, WC; Cromlish, W; Khougaz, K; Lamontagne, S; Massé, F; Riendeau, D; Toulmond, S; Percival, MD Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. J Med Chem48:7535-43 (2005) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Solution Info, Assay Method |
|---|
| |
| Cathepsin S |
|---|
| Name: | Cathepsin S |
|---|
| Synonyms: | CATS_HUMAN | CTSS | Cathepsin S (Cat S) | cathepsin S preproprotein |
|---|
| Type: | Protein |
|---|
| Mol. Mass.: | 37507.38 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | P25774 |
|---|
| Residue: | 331 |
|---|
| Sequence: | MKRLVCVLLVCSSAVAQLHKDPTLDHHWHLWKKTYGKQYKEKNEEAVRRLIWEKNLKFVM
LHNLEHSMGMHSYDLGMNHLGDMTSEEVMSLMSSLRVPSQWQRNITYKSNPNRILPDSVD
WREKGCVTEVKYQGSCGACWAFSAVGALEAQLKLKTGKLVSLSAQNLVDCSTEKYGNKGC
NGGFMTTAFQYIIDNKGIDSDASYPYKAMDQKCQYDSKYRAATCSKYTELPYGREDVLKE
AVANKGPVSVGVDARHPSFFLYRSGVYYEPSCTQNVNHGVLVVGYGDLNGKEYWLVKNSW
GHNFGEEGYIRMARNKGNHCGIASFPSYPEI
|
|
|
|---|
| BDBM19858 |
|---|
| BDBM19490 |
|---|
| Name | BDBM19858 |
|---|
| Synonyms: | N-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-(morpholin-4-yl)benzamide | aryl-morpholino-containing analogue, 13 |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C20H26N4O3 |
|---|
| Mol. Mass. | 370.4454 |
|---|
| SMILES | O=C(NC1(CCCCC1)C(=O)NCC#N)c1ccc(cc1)N1CCOCC1 |
|---|
| Structure | 
|
|---|
Search and Browse
