Reaction Details |
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Target | Cathepsin B |
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Ligand | BDBM19856 |
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Substrate/Competitor | BDBM19517 |
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Meas. Tech. | Enzyme Inhibition Assay and Whole Cell Enzyme Occupancy Assay |
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pH | 6±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 86000±14000 nM |
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EC50 | 4400±2000 nM |
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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 |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Cathepsin B |
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Name: | Cathepsin B |
Synonyms: | APP secretase | APPS | CATB_HUMAN | CPSB | CTSB | Cathepsin B heavy chain | Cathepsin B light chain | Cathepsin B1 |
Type: | Enzyme |
Mol. Mass.: | 37819.69 |
Organism: | Homo sapiens (Human) |
Description: | gi_63102437 |
Residue: | 339 |
Sequence: | MWQLWASLCCLLVLANARSRPSFHPLSDELVNYVNKRNTTWQAGHNFYNVDMSYLKRLCG
TFLGGPKPPQRVMFTEDLKLPASFDAREQWPQCPTIKEIRDQGSCGSCWAFGAVEAISDR
ICIHTNAHVSVEVSAEDLLTCCGSMCGDGCNGGYPAEAWNFWTRKGLVSGGLYESHVGCR
PYSIPPCEHHVNGSRPPCTGEGDTPKCSKICEPGYSPTYKQDKHYGYNSYSVSNSEKDIM
AEIYKNGPVEGAFSVYSDFLLYKSGVYQHVTGEMMGGHAIRILGWGVENGTPYWLVANSW
NTDWGDNGFFKILRGQDHCGIESEVVAGIPRTDQYWEKI
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BDBM19856 |
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BDBM19517 |
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Name | BDBM19856 |
Synonyms: | (2R)-N-(cyanomethyl)-4-methyl-2-{3-[4-(piperazin-1-yl)phenyl]phenyl}pentanamide | CHEMBL184514 | JMC463709 (R)-2 | piperazine-containing compound, 11 |
Type | Small organic molecule |
Emp. Form. | C24H30N4O |
Mol. Mass. | 390.5212 |
SMILES | CC(C)C[C@@H](C(=O)NCC#N)c1cccc(c1)-c1ccc(cc1)N1CCNCC1 |r| |
Structure |
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