Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

Discovery of a Novel Class of Negative Allosteric Modulator of the Dopamine D2 Receptor Through Fragmentation of a Bitopic Ligand.

Journal of medicinal chemistry - 10 Sept 2015

Mistry Shailesh N, Shonberg Jeremy, Draper-Joyce Christopher J, Klein Herenbrink Carmen, Michino Mayako, Shi Lei, Christopoulos Arthur, Capuano Ben, Scammells Peter J, Lane J Robert

Abstract excerpt

Recently, we have demonstrated that N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652) (1) adopts a bitopic pose at one protomer of a dopamine D2 receptor (D2R) dimer to negatively modulate the binding of dopamine at the other protomer. The 1H-indole-2-carboxamide moiety of 1 extends into a secondary pocket between the extracellular ends of TM2 and TM7...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Amides
Share to Arrestins

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to beta-Arrestins

Share to Dopamine Agents

Share to Isoquinolines

Share to Mitogen-Activated Protein Kinase 1

Share to Mitogen-Activated Protein Kinase 3

Share to Radioligand Assay

Source

Open in PubMed Open full text

Identifiers

PMID: 26258690
DOI: 10.1021/acs.jmedchem.5b00585
PMCID: PMC10823399

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 2 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Discovery of a Novel Class of Negative Allosteric Modulator of the Dopamine D2 Receptor Through Fragmentation of a Bitopic Ligand.PMID 26258690Read ↗

The structural determinants of the bitopic binding mode of a negative allosteric modulator of the dopamine D2 receptor.Semantic proximity Read ↗

Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT2C Receptor Agonists.Semantic proximity Read ↗

Structural insight into the mechanism of 4-aminoquinolines selectivity for the alpha2A-adrenoceptorSemantic proximity Read ↗

The E2.65A mutation disrupts dynamic binding poses of SB269652 at the dopamine D2 and D3 receptors.Semantic proximity Read ↗

Engineering a GPCR-ligand pair that simulates the activation of D(2L) by Dopamine.Semantic proximity Read ↗

Designing drugs and chemical probes with the dualsteric approach.Semantic proximity Read ↗

Three amino acids in the D2 dopamine receptor regulate selective ligand function and affinity.Semantic proximity Read ↗

Design, Synthesis, and Evaluation of Functionalized 5-(4-arylpiperazin-1-yl)-N-Quinolinyl-pentanamides as Selective Dopamine D3 Receptor LigandsSemantic proximity Read ↗

Defining the putative inhibitory site for a selective negative allosteric modulator of human α4β2 neuronal nicotinic receptors.Semantic proximity Read ↗

Allosteric "beta-blocker" isolated from a DNA-encoded small molecule library.Semantic proximity Read ↗

A diversity oriented synthesis of natural product inspired molecular libraries.Semantic proximity Read ↗

Structural and functional studies of the modulator NS9283 reveal agonist-like mechanism of action at α4β2 nicotinic acetylcholine receptors.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.