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Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing human Prostaglandin D2 receptor

PubChem AID
239528
Primary Citation
Discovery of orally active prostaglandin D2 receptor antagonists [PMID: 15341946]
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 239528) reports results from the above primary citation. Additional data from the same publication are reported in a total of 11 BioAssay records in PubChem.

1 Description

Title: Discovery of orally active prostaglandin D2 receptor antagonists.

Abstract: A series of N-(p-alkoxy)benzoyl-2-methylindole-4-acetic acids were synthesized and evaluated for prostaglandin D(2) (DP) receptor affinity and antagonist activity. Some of them exhibited strong receptor binding and were potent in the cAMP formation assays. These antagonists also suppressed allergic inflammatory responses such as the PGD(2)-induced increase of microvascular permeability. Structure-activity relationship (SAR) data are presented.

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: 2004

Volume: 14

Issue: 19

First Page: 4891

Last Page: 4895

DOI: 10.1016/j.bmcl.2004.07.039

Target ChEMBL ID: CHEMBL4427

ChEMBL Target Name: Prostanoid DP 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

Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing human Prostaglandin D2 receptor

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 2.4
Version 3.1
Version 3.2
Version 4.1
Version 4.2
Version 5.1
Version 6.1
Version 7.1
Version 8.1
Version 8.2
Version 9.1
Version 9.2
Version 9.3
Version 9.4
Version 9.5
Version 10.1
Version 10.2
2022-08-30 (currently shown)

8.8 Status

Live

9 Same-Publication BioAssays

10 BioAssay Annotations

Assay Format
Cell-based
Assay Type
Binding
Assay Cell Type
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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