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In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.

PubChem AID
65935
Primary Citation
N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide: a potent and selective dopamine D4 ligand [PMID: 9822559]
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 65935) reports results from the above primary citation. Additional data from the same publication are reported in a total of 8 BioAssay records in PubChem.

1 Description

Title: N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide: a potent and selective dopamine D4 ligand.

Abstract: A series of new 1-aryl-4-alkylpiperazines containing a terminal benzamide fragment or a tetralin-1-yl nucleus on the alkyl chain were synthesized and tested for binding at cloned human dopamine D4 and D2 receptor subtypes. A SAFIR (structure-affinity relationship) study on this series is herein discussed. The most relevant D4 receptor affinities were displayed by N-[omega-[4-arylpiperazin-1-yl]alkyl]-methoxybenzamides (compounds 5, 16-20), their IC50 values ranging between 0.057 and 7.8 nM. Among these, N-[2-[4-(4-chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide (17) emerged since it exhibited very high affinity for dopamine D4 receptor (IC50 = 0.057 nM) with selectivity of >10 000 for the D4 versus the D2 receptor; compound 17 was also selective versus serotonin 5-HT1A and adrenergic alpha1 receptors.

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: 1998

Volume: 41

Issue: 24

First Page: 4903

Last Page: 4909

DOI: 10.1021/jm981041x

Target ChEMBL ID: CHEMBL219

ChEMBL Target Name: Dopamine D4 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

In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.

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 2.5
Version 3.1
Version 3.2
Version 3.3
Version 4.1
Version 5.1
Version 5.2
Version 5.3
Version 6.1
Version 6.2
Version 7.1
Version 7.2
Version 8.1
Version 8.2
Version 8.3
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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