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Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting

PubChem AID
448777
Primary Citation
Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs [PMID: 19660947]
Source
External ID
BioAssay Type
Confirmatory
Tested Substances
Version
Status
Live
Dates
  • Deposit:
    2010-07-08
  • Modify:
    2022-08-30
Description
This bioassay record (AID 448777) reports results from the above primary citation. Additional data from the same publication are reported in a total of 6 BioAssay records in PubChem.

1 Description

Title: Structural determinants for histamine H(1) affinity, hERG affinity and QTc prolongation in a series of terfenadine analogs.

Abstract: In the late 1980's reports linking the non-sedating antihistamines terfenadine and astemizole with torsades de pointes, a form of ventricular tachyarrhythmia that can degenerate into ventricular fibrillation and sudden death, appeared in the clinical literature. A substantial body of evidence demonstrates that the arrhythmogenic effect of these cardiotoxic antihistamines, as well as a number of structurally related compounds, results from prolongation of the QT interval due to suppression of specific delayed rectifier ventricular K+ currents via blockade of the hERG-IKr channel. In order to better understand the structural requirements for hERG and H(1) binding for terfenadine, a series of analogs of terfenadine has been prepared and studied in both in vitro and in vivo hERG and H(1) assays.

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: 2009

Volume: 19

Issue: 17

First Page: 5043

Last Page: 5047

DOI: 10.1016/j.bmcl.2009.07.047

Target ChEMBL ID: CHEMBL231

ChEMBL Target Name: Histamine H1 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

Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting

8.2 Source

8.3 External ID

8.4 Project Category

Literature, Extracted

8.5 BioAssay Type

Confirmatory

8.6 Deposit Date

2010-07-08

8.7 Modify Date

Version 1.1
Version 1.2
Version 1.3
Version 1.4
Version 2.1
Version 2.2
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 9.1
Version 10.1
Version 10.2
Version 11.1
Version 11.2
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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