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Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor

PubChem AID
66709
Primary Citation
Endothelin antagonists: evaluation of 2,1,3-benzothiadiazole as a methylendioxyphenyl bioisoster [PMID: 9871621]
Source
External ID
BioAssay Type
Confirmatory
Tested Substances
Tested Compounds
Version
Status
Live
Dates
  • Deposit:
    2010-05-20
  • Modify:
    2022-08-30
Description
This bioassay record (AID 66709) 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: Endothelin antagonists: evaluation of 2,1,3-benzothiadiazole as a methylendioxyphenyl bioisoster.

Abstract: The methylendioxyphenyl group is present in a number of endothelin receptor antagonists thus far reported. By means of a Kohonen neural network we discovered with a benzothiadiazole a bioisosteric replacement instead. This group should be devoid of the negative metabolic interactions with cytochrome P450 ascribed to methylendioxyphenyl in vivo. The synthesis of a potent benzothiadiazole analogue EMD 122801 together with in vitro studies of different methylendioxyphenyl, benzothiadiazole and benzofurazan derivatives is 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: 1998

Volume: 8

Issue: 1

First Page: 17

Last Page: 22

DOI: 10.1016/s0960-894x(97)10151-2

Target ChEMBL ID: CHEMBL1785

ChEMBL Target Name: Endothelin receptor ET-B

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

Encoding Gene
NCBI GeneID

8 Identity

8.1 BioAssay Name

Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor

8.2 Source

8.3 External ID

8.4 Project Category

Literature, Extracted

8.5 BioAssay Type

Confirmatory

8.6 Deposit Date

2010-05-20

8.7 Modify Date

Version 1.1
Version 2.1
Version 2.2
Version 2.3
Version 2.4
Version 2.5
Version 3.1
Version 3.2
Version 4.1
Version 5.1
Version 5.2
Version 6.1
Version 6.2
Version 6.3
Version 7.1
Version 7.2
Version 8.1
Version 8.2
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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