An official website of the United States government

Inhibition of FAP

PubChem AID
579753
Primary Citation
Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors [PMID: 21320777]
Source
External ID
BioAssay Type
Confirmatory
Tested Substances
Tested Compounds
Version
Status
Live
Dates
  • Deposit:
    2011-09-18
  • Modify:
    2018-09-17
Description
This bioassay record (AID 579753) reports results from the above primary citation. Additional data from the same publication are reported in a total of 10 BioAssay records in PubChem.

1 Description

Title: Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors.

Abstract: A series of 4-amino cyclohexanes and 4-substituted piperidines were prepared and evaluated for inhibition of DPP-4. Analog 20q displayed both good DPP-4 potency and selectivity against other proteases, while derivative 20k displayed long half life and modest oral bioavailability in rat. The most potent analog, 3-(5-aminocarbonylpyridyl piperidine 53j, displayed excellent DPP-4 activity with good selectivity versus other proline enzymes.

2 Comment

Journal: Bioorg Med Chem Lett

Year: 2011

Volume: 21

Issue: 6

First Page: 1880

Last Page: 1886

DOI: 10.1016/j.bmcl.2010.12.060

Target ChEMBL ID: CHEMBL4683

ChEMBL Target Name: Fibroblast activation protein alpha

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

Relationship Type: H - Homologous protein target assigned

Confidence: Homologous single protein target assigned

3 Result Definitions

4 Data Table

5 Target

8 Identity

8.1 BioAssay Name

Inhibition of FAP

8.2 Source

8.3 External ID

8.4 Project Category

Literature, Extracted

8.5 BioAssay Type

Confirmatory

8.6 Deposit Date

2011-09-18

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 4.3
Version 4.4
Version 4.5
Version 5.1
2018-09-17 (currently shown)

8.8 Status

Live

9 Same-Publication BioAssays

10 BioAssay Annotations

Assay Type
Binding

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
CONTENTS