Page last updated: 2024-12-10

ro 4-6790

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

Description

Ro 4-6790: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5312145
CHEMBL ID433461
CHEBI ID92762
SCHEMBL ID678897
MeSH IDM0294534

Synonyms (50)

Synonym
BRD-K43290182-001-01-9
gtpl274
ro-04-6790
BIOMOL-NT_000164
BPBIO1_000551
NCGC00015885-01 ,
lopac-r-140
PDSP2_001360
PDSP1_001376
LOPAC0_001045
ro 04-6790
NCGC00162326-02
ro 04-6790 dihydrochloride
NCGC00162326-01
NCGC00015885-04
n-(2,6-bis(methylamino)pyrimidin-4-yl)-4-aminobenzenesulfonamide
4-amino-n-(2,6-bis(methylamino)pyrimidin-4-yl)benzenesulfonamide
4-amino-n-(2,6-bis-methylamino-pyrimidin-4-yl)-benzenesulfonamide
4-amino-n-(2,6-bis-dimethylamino-pyrimidin-4-yl)-benzenesulfonamide
bdbm50090528
4-amino-n-(2-methylamino-pyrimidin-4-yl)-benzenesulfonamide
ro 4-6790
ro-046790
CHEMBL433461 ,
L000511
4-amino-n-[2,6-bis(methylamino)pyrimidin-4-yl]benzenesulfonamide
CCG-205122
NCGC00015885-02
NCGC00015885-03
202466-68-0
SCHEMBL678897
JELFWSXQTXRMAJ-UHFFFAOYSA-N ,
4-amino-n-[2,6-bis(methylamino)-4-pyrimidinyl]-benzenesulfonamide
AKOS024457330
CHEBI:92762
HY-14335
CS-0003291
FT-0748141
(4-amino-n-[2,6-bis(methylamino)-4-pyrimidinyl]-benzenesulfonamide)
ro04-6790
BCP02244
Q855636
DTXSID701017998
SDCCGSBI-0051015.P002
NCGC00015885-09
benzenesulfonamide, 4-amino-n-[2,6-bis(methylamino)-4-pyrimidinyl]-
4-azanyl-n-(2,6-bis(methylamino)pyrimidin-4-yl)benzenesulfonamide
cu78rar5zh ,
CIA46668
4-amino-n-[2,6-bis(methylamino)-4-pyrimidinyl]benzenesulfonamide
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
sulfonamideAn amide of a sulfonic acid RS(=O)2NR'2.
benzenesAny benzenoid aromatic compound consisting of the benzene skeleton and its substituted derivatives.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (36)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency17.78280.100020.879379.4328AID588453
ATAD5 protein, partialHomo sapiens (human)Potency2.59180.004110.890331.5287AID493107
Microtubule-associated protein tauHomo sapiens (human)Potency15.84890.180013.557439.8107AID1460
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency28.18380.011212.4002100.0000AID1030
hypothetical protein, conservedTrypanosoma bruceiPotency23.93410.223911.245135.4813AID624147
regulator of G-protein signaling 4Homo sapiens (human)Potency9.46620.531815.435837.6858AID504845
arylsulfatase AHomo sapiens (human)Potency9.52831.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency26.67950.035520.977089.1251AID504332
cytochrome P450 2C19 precursorHomo sapiens (human)Potency39.81070.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency1.99530.00636.904339.8107AID883
chromobox protein homolog 1Homo sapiens (human)Potency50.11870.006026.168889.1251AID488953
ras-related protein Rab-9AHomo sapiens (human)Potency6.51310.00022.621531.4954AID485297
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency0.79430.031610.279239.8107AID884; AID885
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.81070.251215.843239.8107AID504327
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency25.11890.00106.000935.4813AID944
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency0.79431.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency0.79431.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency0.79431.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency0.79431.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency0.79431.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency0.79431.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency0.79431.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency0.79431.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency0.79431.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency0.79431.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency0.79431.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency1.99530.00638.235039.8107AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency0.79431.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency0.79431.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency0.79431.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency0.79431.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency0.79431.000012.224831.6228AID885
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency37.93300.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki0.05010.00030.37088.1600AID6547
5-hydroxytryptamine receptor 6Homo sapiens (human)IC50 (µMol)0.02630.00170.83815.4200AID6507
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.05150.00020.522910.0000AID1178357; AID1452785; AID239164; AID239920; AID313655; AID369091; AID550979; AID599941; AID6512; AID6522; AID6547
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.05000.00000.437510.0000AID6522
[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 membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
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)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (37)

Assay IDTitleYearJournalArticle
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.
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.
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).
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).
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.
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.
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.
AID369091Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
Indene-based scaffolds. 2. An indole-indene switch: discovery of novel indenylsulfonamides as 5-HT6 serotonin receptor agonists.
AID1452785Binding affinity to human 5HT6R
AID6507Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Identification of a potent and selective 5-HT(6) antagonist: one-step synthesis of (E)-3-(benzenesulfonyl)-2- (methylsulfanyl)pyrido[1,2-a]pyrimidin-4-ylidenamine from 2-(benzenesulfonyl)-3,3-bis(methylsulfanyl)acrylonitrile.
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.
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.
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.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
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)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)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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (38)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (13.16)18.2507
2000's18 (47.37)29.6817
2010's10 (26.32)24.3611
2020's5 (13.16)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.09

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 Index11.09 (24.57)
Research Supply Index3.66 (2.92)
Research Growth Index4.76 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (5.26%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other36 (94.74%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]