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BioAssay: AID 50449

Selectivity ratio between Cathepsin B and Cathepsin K

A novel series of 3,4-disubstituted azetidinones based inhibitors of the cysteine protease cathepsin K (Cat K) has been identified. Although not optimized, some of these compounds show at least 100-fold selectivity against other cathepsins. The use of cyclic moieties as P2 elements has proven to be crucial to achieve a high degree of selectivity. ..more
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 Tested Compounds
 Tested Compounds
All(9)
 
 
Unspecified(9)
 
 
 Tested Substances
 Tested Substances
All(9)
 
 
Unspecified(9)
 
 
 Related BioAssays
 Related BioAssays
AID: 50449
Data Source: ChEMBL (47593)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-20
Modify Date: 2014-08-24

Data Table ( Complete ):           View All Data
Tested Compounds:
Description:
Title: 3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity.

Abstract: A novel series of 3,4-disubstituted azetidinones based inhibitors of the cysteine protease cathepsin K (Cat K) has been identified. Although not optimized, some of these compounds show at least 100-fold selectivity against other cathepsins. The use of cyclic moieties as P2 elements has proven to be crucial to achieve a high degree of selectivity.
(PMID: 12781193)
Comment
Putative Target:
ChEMBL Target ID: 10378
Target Type: SINGLE PROTEIN
Pref Name: Cathepsin B
Synonyms: APP secretase;APPS;Cathepsin B;Cathepsin B heavy chain;Cathepsin B light chain;Cathepsin B1;
Gene Name: CPSB;CTSB;
Protein Accession: P07858;
Protein GI: 68067549;
Organism: Homo sapiens
Tax ID: 9606
Target Classification: enzyme protease cysteine ca c1a
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Assay Data Source: Scientific Literature
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ratio activity commentRatio activity commentString
2Ratio standard flagRatio standard flagInteger
3Ratio qualifierRatio qualifierString
4Ratio published valueRatio published valueFloat
5Ratio standard valueRatio standard valueFloat

Data Table (Concise)
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