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Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting

PubChem AID
619747
Primary Citation
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs [PMID: 21907583]
Source
External ID
BioAssay Type
Confirmatory
Tested Substances
Tested Compounds
Version
Status
Live
Dates
  • Deposit:
    2012-04-30
  • Modify:
    2022-08-30
Description
This bioassay record (AID 619747) reports results from the above primary citation. Additional data from the same publication are reported in a total of 22 BioAssay records in PubChem.

1 Description

Title: CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.

Abstract: The marine invertebrate-derived meridianin A, the originally proposed structure for psammopemmin A, and several related 3-pyrimidylindole analogs were synthesized and subsequently investigated for central nervous system, antimalarial, and cytotoxic activity. A Suzuki coupling of an indoleborate ester to the pyrimidine electrophile was utilized to form the natural product and derivatives thereof. The 3-pyrimidineindoles were found to prevent radioligand binding to several CNS receptors and transporters, most notably, serotonin receptors (<0.2 μM K(i) for 5HT(2B)). Two compounds also inhibited the human malaria parasite Plasmodium falciparum (IC(50) <50 μM). Only the natural product was cytotoxic toward A549 cells (IC(50)=15 μM).

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

Year: 2011

Volume: 19

Issue: 19

First Page: 5756

Last Page: 5762

DOI: 10.1016/j.bmc.2011.08.033

Target ChEMBL ID: CHEMBL3426

ChEMBL Target Name: Serotonin 5a (5-HT5a) receptor

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

Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting

8.2 Source

8.3 External ID

8.4 Project Category

Literature, Extracted

8.5 BioAssay Type

Confirmatory

8.6 Deposit Date

2012-04-30

8.7 Modify Date

Version 1.1
Version 2.1
Version 3.1
Version 4.1
Version 4.2
Version 5.1
Version 5.2
Version 6.1
Version 6.2
Version 6.3
2022-08-30 (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
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