Page last updated: 2024-12-10

ro 63-0563

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

4-amino-N-(2,6 bis-methylamino-pyridin-4-yl)-benzene sulfonamide: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5312144
CHEMBL ID46071
SCHEMBL ID679027
MeSH IDM0294538

Synonyms (19)

Synonym
ro-630563
gtpl275
ro630563
ro 63-0563
n-(2,6-bis(methylamino)pyridin-4-yl)-4-aminobenzenesulfonamide
bdbm50090524
4-amino-n-(2,6-diamino-pyridin-4-yl)-benzenesulfonamide
4-amino-n-(2,6-bis-methylamino-pyridin-4-yl)-benzenesulfonamide
CHEMBL46071 ,
ro-63-0563
L000518
4-amino-n-[2,6-bis(methylamino)pyridin-4-yl]benzenesulfonamide
[3h]ro 63-0563
gtpl3246
SCHEMBL679027
4-amino-n-(2,6 bis-methylamino-pyridin-4-yl)-benzene sulfonamide
Q27088598
202466-77-1
AKOS040749344
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki0.01260.00030.37088.1600AID6547
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.05850.00020.522910.0000AID1154620; AID1178357; AID239164; AID239920; AID313655; AID550979; AID599941; AID6512; AID6522; AID6547
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.01260.00000.437510.0000AID6522
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (6)

Processvia Protein(s)Taxonomy
cerebral cortex cell migration5-hydroxytryptamine receptor 6Homo sapiens (human)
positive regulation of TOR signaling5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 6Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
histamine receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 6Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
cilium5-hydroxytryptamine receptor 6Homo sapiens (human)
synapse5-hydroxytryptamine receptor 6Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (15)

Assay IDTitleYearJournalArticle
AID1345170Human 5-HT6 receptor (5-Hydroxytryptamine receptors)1998Molecular pharmacology, Sep, Volume: 54, Issue:3
The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
AID1345154Rat 5-HT6 receptor (5-Hydroxytryptamine receptors)1998Molecular pharmacology, Sep, Volume: 54, Issue:3
The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.
AID1345170Human 5-HT6 receptor (5-Hydroxytryptamine receptors)1998British journal of pharmacology, Jun, Volume: 124, Issue:3
Characterization of Ro 04-6790 and Ro 63-0563: potent and selective antagonists at human and rat 5-HT6 receptors.
AID1345154Rat 5-HT6 receptor (5-Hydroxytryptamine receptors)1998British journal of pharmacology, Jun, Volume: 124, Issue:3
Characterization of Ro 04-6790 and Ro 63-0563: potent and selective antagonists at human and rat 5-HT6 receptors.
AID239920Binding affinity for human 5-hydroxytryptamine 6 receptor2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
A three-dimensional pharmacophore model for 5-hydroxytryptamine6 (5-HT6) receptor antagonists.
AID1178357Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells2014Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
Serotonin 5-HT6 receptor antagonists for the treatment of cognitive deficiency in Alzheimer's disease.
AID313655Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists.
AID599941Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells2009Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
Identification of a novel series of 3-piperidinyl-5-sulfonylindazoles as potent 5-HT6 ligands.
AID6522Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
6-Bicyclopiperazinyl-1-arylsulfonylindoles and 6-bicyclopiperidinyl-1-arylsulfonylindoles derivatives as novel, potent, and selective 5-HT6 receptor antagonists.
AID550979Binding affinity to 5HT6 receptor2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
1-(Arylsulfonyl)-2,3-dihydro-1H-quinolin-4-one derivatives as 5-HT(6) serotonin receptor ligands.
AID1154620Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands.
AID239164Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands.
AID6547Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD1999Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2
5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist.
AID233486Antagonistic activity of compound in 5-HT induced cAMP accumulation2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID6512Binding affinity towards human 5-hydroxytryptamine 6 receptor2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (25.00)18.2507
2000's6 (50.00)29.6817
2010's3 (25.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.88

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.88 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.88)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (83.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]