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Inhibitory concentration against recombinant human Cathepsin L at 37 degree C at pH 5.5

PubChem AID
254422
Protein Target
Primary Citation
Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 1 [PMID: 16183279]
Source
External ID
BioAssay Type
Confirmatory
Tested Substances
Tested Compounds
Version
Status
Live
Dates
  • Deposit:
    2010-05-24
  • Modify:
    2022-08-30
Description
This bioassay record (AID 254422) reports results from the above primary citation. Additional data from the same publication are reported in a total of 2 BioAssay records in PubChem.

1 Description

Title: Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 1.

Abstract: A series of Nalpha-acyl-alpha-amino acid-(arylaminoethyl)amides were found to be potent and noncovalent cathepsin S inhibitors. Compound 20 possessed high cathepsin S affinity (Ki=3.3 nM) and showed excellent selectivity over cathepsin K, L, F, and V. Molecular modeling, design, synthesis, and in vitro activity are described.

2 Comment

Compounds with activity <= 10uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Journal: Bioorg Med Chem Lett

Year: 2005

Volume: 15

Issue: 22

First Page: 4979

Last Page: 4984

DOI: 10.1016/j.bmcl.2005.08.017

Target ChEMBL ID: CHEMBL3837

ChEMBL Target Name: Cathepsin L

ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain

Relationship Type: D - Direct protein target assigned

Confidence: Direct single protein target assigned

3 Result Definitions

4 Data Table

5 Target

8 Identity

8.1 BioAssay Name

Inhibitory concentration against recombinant human Cathepsin L at 37 degree C at pH 5.5

8.2 Source

8.3 External ID

8.4 Project Category

Literature, Extracted

8.5 BioAssay Type

Confirmatory

8.6 Deposit Date

2010-05-24

8.7 Modify Date

Version 1.1
Version 2.1
Version 2.2
Version 3.1
Version 3.2
Version 4.1
Version 4.2
Version 5.1
Version 6.1
Version 7.1
Version 7.2
Version 8.1
Version 8.2
Version 8.3
Version 8.4
Version 8.5
Version 9.1
Version 9.2
2022-08-30 (currently shown)

8.8 Status

Live

9 Same-Publication BioAssays

10 BioAssay Annotations

Assay Type
Binding
Assay Organism

11 Information Sources

  1. PubChem
  2. ChEMBL
    LICENSE
    Access to the web interface of ChEMBL is made under the EBI's Terms of Use (http://www.ebi.ac.uk/Information/termsofuse.html). The ChEMBL data is made available on a Creative Commons Attribution-Share Alike 3.0 Unported License (http://creativecommons.org/licenses/by-sa/3.0/).
    http://www.ebi.ac.uk/Information/termsofuse.html
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