Page last updated: 2024-12-10

1-[3-[[4-(4-fluorophenyl)-1-piperazinyl]methyl]-4-methoxyphenyl]-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylic acid

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

You're asking about a complex molecule with the chemical name **1-[3-[[4-(4-fluorophenyl)-1-piperazinyl]methyl]-4-methoxyphenyl]-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylic acid**. This is a mouthful, so it's often referred to by its shorter **chemical name:** **SB-203580**.

**Here's what we know about SB-203580:**

* **It's a selective inhibitor of p38 MAPK.** p38 MAPK (mitogen-activated protein kinase) is a key enzyme involved in many cellular processes, including inflammation, stress responses, and cell death.
* **It's a research tool.** SB-203580 is not used clinically (in humans or animals) as a treatment for any disease. However, it's a valuable tool for researchers studying the role of p38 MAPK in various biological processes.

**Here's why SB-203580 is important for research:**

* **Understanding p38 MAPK's role:** By using SB-203580, researchers can block the activity of p38 MAPK and observe the resulting effects. This helps them understand what roles p38 MAPK plays in various processes.
* **Drug discovery:** SB-203580 and similar compounds are used as lead compounds in drug discovery programs. Researchers might use these compounds as a starting point to design new drugs that target p38 MAPK for specific therapeutic purposes.
* **Studying disease mechanisms:** SB-203580 can be used to study the role of p38 MAPK in various diseases, such as inflammatory diseases, cancer, and neurodegenerative disorders. This can lead to the development of new therapeutic strategies.

**Key points:**

* SB-203580 is a chemical compound that specifically blocks the activity of p38 MAPK.
* It's not a drug used for treatment but a valuable research tool for studying p38 MAPK's role in various processes.
* Its research applications include understanding p38 MAPK's function, drug discovery, and disease mechanism investigation.

**Note:** This information is provided for general knowledge and should not be taken as medical advice. If you have specific questions about SB-203580 or its potential applications, it's best to consult with a qualified medical professional or researcher.

Cross-References

ID SourceID
PubMed CID4559992
CHEMBL ID1500932
CHEBI ID116680

Synonyms (24)

Synonym
MLS000686795 ,
1-(3-{[4-(4-fluorophenyl)piperazin-1-yl]methyl}-4-methoxyphenyl)-2,3,4,9-tetrahydro-1h-beta-carboline-3-carboxylic acid
smr000339885
CHEMDIV1_017546 ,
1-(3-((4-(4-fluorophenyl)piperazin-1-yl)methyl)-4-methoxyphenyl)-2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indole-3-carboxylic acid
CHEBI:116680
AKOS000265950
HMS636N12
MLS002589508
1-[3-[[4-(4-fluorophenyl)piperazin-1-yl]methyl]-4-methoxyphenyl]-2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indole-3-carboxylic acid
HMS2745I17
1-(3-(4-(4-fluorophenyl)piperazinomethyl)-4-methoxyphenyl)-2,3,4,9-tetrahyd ro-1h-beta-carboline-3-carboxylic acid
AKOS021852291
CHEMBL1500932
1-[3-[[4-(4-fluorophenyl)-1-piperazinyl]methyl]-4-methoxyphenyl]-2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indole-3-carboxylic acid
cid_4559992
bdbm75026
1-[3-[[4-(4-fluorophenyl)piperazin-1-yl]methyl]-4-methoxy-phenyl]-2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indole-3-carboxylic acid
1-[3-[[4-(4-fluorophenyl)piperazino]methyl]-4-methoxy-phenyl]-2,3,4,9-tetrahydro-1h-beta-carboline-3-carboxylic acid
OPERA_ID_899
Q27200995
SR-01000597010-1
sr-01000597010
BRD-A15680534-001-18-6
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
harmala alkaloidAny member of a class of naturally occurring alkaloids based on a 1-methyl-9H-beta-carboline skeleton.
[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 (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency39.81070.044717.8581100.0000AID485341
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency3.97160.140911.194039.8107AID2451
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency56.23410.631035.7641100.0000AID504339
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency25.11890.177814.390939.8107AID2147
glp-1 receptor, partialHomo sapiens (human)Potency8.91250.01846.806014.1254AID624417
Microtubule-associated protein tauHomo sapiens (human)Potency31.62280.180013.557439.8107AID1460
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency19.95260.707912.194339.8107AID720542
glucocerebrosidaseHomo sapiens (human)Potency39.81070.01268.156944.6684AID2101
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency39.81070.707936.904389.1251AID504333
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.10000.035520.977089.1251AID504332
importin subunit beta-1 isoform 1Homo sapiens (human)Potency112.20205.804836.130665.1308AID540263
eyes absent homolog 2 isoform aHomo sapiens (human)Potency19.01481.199814.641950.1187AID720540
snurportin-1Homo sapiens (human)Potency112.20205.804836.130665.1308AID540263
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
alternatively spliced Trp4Mus musculus (house mouse)EC50 (µMol)0.53070.00033.337010.5907AID434942
karyopherin alpha 2 (RAG cohort 1, importin alpha 1), isoform CRA_bHomo sapiens (human)EC50 (µMol)8.57200.918141.9368121.5000AID435026
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (23)

Assay IDTitleYearJournalArticle
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain 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.
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.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (16.67)29.6817
2010's4 (66.67)24.3611
2020's1 (16.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.35

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 Index12.35 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.30 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.35)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]