Page last updated: 2024-12-09

1-[[4-[(3,4-dichlorophenyl)thio]-3-pyridinyl]sulfonyl]-3-propylurea

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

1-[[4-[(3,4-dichlorophenyl)thio]-3-pyridinyl]sulfonyl]-3-propylurea, also known as **L-735,524**, is a potent and selective **inhibitor of the enzyme carbonic anhydrase IX (CA IX)**.

**Carbonic anhydrase IX (CA IX)** is an enzyme that plays a crucial role in the growth and survival of tumor cells. It is overexpressed in various types of cancers, particularly those that are hypoxic (low oxygen levels). CA IX helps tumor cells adapt to these harsh conditions by regulating the pH of the tumor microenvironment.

**Why is L-735,524 important for research?**

* **Anti-cancer drug development:** L-735,524 has shown promising anti-cancer activity in preclinical studies. By inhibiting CA IX, it can slow down tumor growth and potentially improve the efficacy of other cancer therapies.
* **Understanding the role of CA IX in cancer:** L-735,524 acts as a valuable tool to investigate the role of CA IX in cancer progression and metastasis.
* **Development of new CA IX inhibitors:** Understanding the mechanism of action of L-735,524 can guide the development of more potent and selective CA IX inhibitors for future therapeutic applications.

**Key features of L-735,524:**

* **High potency:** It exhibits strong inhibition of CA IX with a Ki value in the nanomolar range.
* **Selectivity:** It is highly selective for CA IX over other isoforms of carbonic anhydrase.
* **Good pharmacokinetic properties:** It has favorable bioavailability and pharmacokinetic profile, making it suitable for in vivo studies.

**However, it is important to note that L-735,524 is not currently used clinically. Further research is needed to assess its safety and efficacy in human patients.**

Cross-References

ID SourceID
PubMed CID1825804
CHEMBL ID1472183
CHEBI ID112888

Synonyms (10)

Synonym
MLS000539686
smr000162110
AJ-333/25006003
4-[(3,4-dichlorophenyl)sulfanyl]-3-({[(propylamino)carbonyl]amino}sulfonyl)pyridine
CHEBI:112888
1-[4-(3,4-dichlorophenyl)sulfanylpyridin-3-yl]sulfonyl-3-propylurea
HMS2303H13
CHEMBL1472183
1-[[4-[(3,4-dichlorophenyl)thio]-3-pyridinyl]sulfonyl]-3-propylurea
Q27193351
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aryl sulfideAny organic sulfide in which the sulfur is attached to at least one aromatic group.
[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 (14)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency28.18380.044717.8581100.0000AID485294
ClpPBacillus subtilisPotency22.38721.995322.673039.8107AID651965
phosphopantetheinyl transferaseBacillus subtilisPotency63.09570.141337.9142100.0000AID1490
thioredoxin glutathione reductaseSchistosoma mansoniPotency56.23410.100022.9075100.0000AID485364
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency3.16230.011212.4002100.0000AID1030
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency0.70790.707936.904389.1251AID504333
pyruvate kinaseLeishmania mexicana mexicanaPotency25.11890.398113.744731.6228AID1721; AID1722
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency22.38720.035520.977089.1251AID504332
huntingtin isoform 2Homo sapiens (human)Potency35.48130.000618.41981,122.0200AID1688
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency11.91730.168316.404067.0158AID720504
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency100.00000.050127.073689.1251AID588590
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency0.08910.075215.225339.8107AID485360
Endothelin receptor type BRattus norvegicus (Norway rat)Potency25.11890.562315.160931.6228AID1721
Endothelin-1 receptorRattus norvegicus (Norway rat)Potency25.11890.562315.160931.6228AID1721
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (13)

Assay IDTitleYearJournalArticle
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (20.00)29.6817
2010's3 (60.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.56

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 Index12.56 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]