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Binding affinity to PAF

PubChem AID
265808
Primary Citation
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist [PMID: 16722655]
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 265808) reports results from the above primary citation. Additional data from the same publication are reported in a total of 61 BioAssay records in PubChem.

1 Description

Title: Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.

Abstract: Gonadotropin releasing hormone (GnRH) plays an important role in the biology of reproduction. The use of GnRH receptor antagonists has been reported in the literature for the treatment of breast, ovarian, and prostate cancers. In this article, we report the synthesis, in vitro characterization, pharmacokinetics, and pharmacodynamics of an orally bioavailable, potent, small molecule GnRH receptor antagonist N-{4,6-dimethoxy-2-[(3-morpholin-4-ylpropyl)amino]pyrimidin-5-yl}-5-[3,3,6-trimthyl-2,3-dihydro-1H-inden-5-yl)oxy]-2-furamide (compound 1).

2 Comment

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

Journal: J Med Chem

Year: 2006

Volume: 49

Issue: 11

First Page: 3362

Last Page: 3367

DOI: 10.1021/jm060012g

Target ChEMBL ID: CHEMBL250

ChEMBL Target Name: Platelet activating factor receptor

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

Binding affinity to PAF

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 2.3
Version 3.1
Version 3.2
Version 4.1
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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