Compounds > 2'-hydroxy-4-methoxychalcone
Page last updated: 2024-08-01 16:49:46

2'-hydroxy-4-methoxychalcone

Description

Cross-References

ID SourceID
PubMed CID5331295
CHEMBL ID241862
SCHEMBL ID2807599
MeSH IDM0099531

Synonyms (33)

Synonym
MLS000438984 ,
smr000113000
2'-hydroxy-4-methoxychalcone
NCGC00090578-01
CHEMBL241862
AKOS001075364
(e)-1-(2-hydroxyphenyl)-3-(4-methoxyphenyl)prop-2-en-1-one
(2e)-1-(2-hydroxyphenyl)-3-(4-methoxyphenyl)prop-2-en-1-one
STK863551
1-(2-hydroxyphenyl)-3-(4-methoxyphenyl)prop-2-en-1-one
34000-29-8
2-propen-1-one, 1-(2-hydroxyphenyl)-3-(4-methoxyphenyl)-, (2e)-
HMS2206A21
nsc 19030
4-methoxy-2'-hydroxychalcone
nsc 91850
AB-0721
1-(2-hydroxyphenyl)-3-(4-methoxyphenyl)-2-propen-1-one
AB00075790-01
F0013-0895
bdbm76395
cid_5331295
(e)-1-(2-hydroxyphenyl)-3-(4-methoxyphenyl)-2-propen-1-one
J-501813
SCHEMBL2807599
NXBNYUSXDBHELA-DHZHZOJOSA-N
mfcd00016447
VU0008664-4
Q63398187
T72315
DTXSID701345759
trans-2'-hydroxy-4-methoxychalcone
Z57101040

Protein Targets (32)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency63.0957AID504339
Chain A, Ferritin light chainEquus caballus (horse)Potency35.4813AID485281
LuciferasePhotinus pyralis (common eastern firefly)Potency0.2685AID588342
phosphopantetheinyl transferaseBacillus subtilisPotency70.7946AID1490
ATAD5 protein, partialHomo sapiens (human)Potency16.3601AID504466; AID504467
TDP1 proteinHomo sapiens (human)Potency15.4706AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency8.4719AID1460
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency10.0000AID2326
67.9K proteinVaccinia virusPotency22.3872AID720579
luciferasePhoturis pensylvanica (Pennsylania firefly)Potency11.2202AID1379
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency12.5893AID504333
P53Homo sapiens (human)Potency79.4328AID504706
pyruvate kinaseLeishmania mexicana mexicanaPotency25.1189AID1721; AID1722
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency44.6684AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency3.1623AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency1.2589AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency3.9811AID883
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency56.2341AID504847
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency29.0929AID504444
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency39.8107AID2551
gemininHomo sapiens (human)Potency0.1032AID624297
Endothelin receptor type BRattus norvegicus (Norway rat)Potency25.1189AID1721
Endothelin-1 receptorRattus norvegicus (Norway rat)Potency25.1189AID1721
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency3.9811AID883
TAR DNA-binding protein 43Homo sapiens (human)Potency19.9526AID652104

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
SUMO-1-specific proteaseHomo sapiens (human)IC506.0000AID488921
SUMO1/sentrin specific peptidase 7Homo sapiens (human)IC503.9300AID488904
caspase-3 isoform a preproproteinHomo sapiens (human)IC5023.1000AID488901
sentrin-specific protease 8Homo sapiens (human)IC5010.6000AID488903
AcetylcholinesteraseTetronarce californica (Pacific electric ray)IC5092.9000AID1799680
ATP-diphosphohydrolase 1Schistosoma mansoniIC5030.6200AID1752772
Shiga toxin subunit AShigella dysenteriaeKi9.9300AID1324538

Bioassays (60)

Assay IDTitleYearJournalArticle
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
ISSN: 1552-454X		A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID513962Induction of quinone reductase activity in rat liver at 22.5 mg/kg, po qd2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
ISSN: 1464-3391		Identification of chalcones as in vivo liver monofunctional phase II enzymes inducers.
AID1324538Inhibition of Shigella dysenteriae type 1 Shiga toxin A subunit assessed as change in transition temperature by SYPRO orange dye based fluorescence-based thermal shift assay2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
ISSN: 1520-4804		In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
AID1167300Antioxidant activity assessed as DPPH radical scavenging activity incubated at room temperature for 20 mins by UV-visible spectrophotometry2014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
ISSN: 1464-3405		Design, synthesis and exploring the quantitative structure-activity relationship of some antioxidant flavonoid analogues.
AID452853Antioxidant activity assessed as hydrogen peroxide scavenging activity by peroxyoxalate chemiluminescent method2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
ISSN: 1464-3391		Natural and synthetic 2'-hydroxy-chalcones and aurones: synthesis, characterization and evaluation of the antioxidant and soybean lipoxygenase inhibitory activity.
AID452850Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM after 60 mins2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
ISSN: 1464-3391		Natural and synthetic 2'-hydroxy-chalcones and aurones: synthesis, characterization and evaluation of the antioxidant and soybean lipoxygenase inhibitory activity.
AID295381Cytotoxicity against human MCF7 cells ATCC HTB38 in aerobic condition assessed as survival at 100 uM by sulforhodamine assay2007Bioorganic & medicinal chemistry, May-15, Volume: 15, Issue:10
ISSN: 0968-0896		Synthetic chalcones, flavanones, and flavones as antitumoral agents: biological evaluation and structure-activity relationships.
AID452848Antioxidant activity assessed as DPPH radical scavenging activity at 50 uM after 60 mins2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
ISSN: 1464-3391		Natural and synthetic 2'-hydroxy-chalcones and aurones: synthesis, characterization and evaluation of the antioxidant and soybean lipoxygenase inhibitory activity.
AID1186725Cytotoxicity against human HL60 cells by MTT assay2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
ISSN: 1464-3405		Cytotoxic activity of substituted chalcones in terms of molecular electronic properties.
AID638551Inhibition of MRP1 overexpressed in human 2008 MRP1 cells assessed as calcein AM accumulation at 10 uM by fluorimetry2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
ISSN: 1464-3391		Investigation of chalcones and benzochalcones as inhibitors of breast cancer resistance protein.
AID1324539Cytotoxicity against African green monkey Vero cells incubated for 24 hrs by neutral red uptake assay2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
ISSN: 1520-4804		In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
AID513976Toxicity in Sprague-Dawley rat assessed as glutamic-pyruvate level at 250 mg/kg, po (RVb = 22.8 +/-13.2 U/L)2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
ISSN: 1464-3391		Identification of chalcones as in vivo liver monofunctional phase II enzymes inducers.
AID513974Toxicity in Sprague-Dawley rat assessed as leucocyte level at 250 mg/kg, po (RVb = 200 +/- 1500 /uL)2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
ISSN: 1464-3391		Identification of chalcones as in vivo liver monofunctional phase II enzymes inducers.
AID513957Cytotoxicity against human MCF7 cells2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
ISSN: 1464-3391		Identification of chalcones as in vivo liver monofunctional phase II enzymes inducers.
AID1752772Inhibition of Schistosoma mansoni ATPDase1 incubated for 30 mins2020RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4
ISSN: 2632-8682		Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here?
AID513963Induction glutathione-S-transferase activity in rat liver at 22.5 mg/kg, po qd2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
ISSN: 1464-3391		Identification of chalcones as in vivo liver monofunctional phase II enzymes inducers.
AID1186727Cytotoxicity against human WM115 cells by MTT assay2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
ISSN: 1464-3405		Cytotoxic activity of substituted chalcones in terms of molecular electronic properties.
AID513977Toxicity in Sprague-Dawley rat assessed as glutamic-oxalate transaminase level at 250 mg/kg, po (RVb = 71.4 +/- 7.8 U/L)2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
ISSN: 1464-3391		Identification of chalcones as in vivo liver monofunctional phase II enzymes inducers.
AID638478Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation preincubated for 30 mins by fluorimetry2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
ISSN: 1464-3391		Investigation of chalcones and benzochalcones as inhibitors of breast cancer resistance protein.
AID759072Cytotoxicity against human HCT116 cells assessed as cell viability at 15 uM after 48 hrs by MTT assay relative to control2013European journal of medicinal chemistry, Jul, Volume: 65ISSN: 1768-3254Superior anticancer activity of halogenated chalcones and flavonols over the natural flavonol quercetin.
AID295385Growth inhibition of HT29 cells by sulforhodamine assay2007Bioorganic & medicinal chemistry, May-15, Volume: 15, Issue:10
ISSN: 0968-0896		Synthetic chalcones, flavanones, and flavones as antitumoral agents: biological evaluation and structure-activity relationships.
AID1698235Effect on cell viability in human neutrophils assessed as decrease in cell viability at 25 uM after 1 hr by Propidium staining based flow cytometric analysis2020Journal of natural products, 10-23, Volume: 83, Issue:10
ISSN: 1520-6025		Chalcones as Modulators of Neutrophil Oxidative Burst under Physiological and High Glucose Conditions.
AID513975Toxicity in Sprague-Dawley rat assessed as haemoglobin level at 250 mg/kg, po (RVb = 15.1 +/- 4.1 g/L)2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
ISSN: 1464-3391		Identification of chalcones as in vivo liver monofunctional phase II enzymes inducers.
AID670957Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 at 256 ug/ml after 24 hrs by disc diffusion method2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
ISSN: 1464-3405		Synthesis and anti Methicillin resistant Staphylococcus aureus activity of substituted chalcones alone and in combination with non-beta-lactam antibiotics.
AID1076733Growth inhibition of cisplatin-resistant human A2780cis cells after 7 days by crystal violet staining based clonogenic assay2014Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6
ISSN: 1464-3391		Polyphenols bearing cinnamaldehyde scaffold showing cell growth inhibitory effects on the cisplatin-resistant A2780/Cis ovarian cancer cells.
AID452849Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM after 20 mins2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
ISSN: 1464-3391		Natural and synthetic 2'-hydroxy-chalcones and aurones: synthesis, characterization and evaluation of the antioxidant and soybean lipoxygenase inhibitory activity.
AID295383Growth inhibition of TK10 cells by sulforhodamine assay2007Bioorganic & medicinal chemistry, May-15, Volume: 15, Issue:10
ISSN: 0968-0896		Synthetic chalcones, flavanones, and flavones as antitumoral agents: biological evaluation and structure-activity relationships.
AID513964Induction glutathione-CYP1A1 in rat liver at 22.5 mg/kg, po qd by EROD assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
ISSN: 1464-3391		Identification of chalcones as in vivo liver monofunctional phase II enzymes inducers.
AID295384Growth inhibition of MCF7 cells by sulforhodamine assay2007Bioorganic & medicinal chemistry, May-15, Volume: 15, Issue:10
ISSN: 0968-0896		Synthetic chalcones, flavanones, and flavones as antitumoral agents: biological evaluation and structure-activity relationships.
AID452847Antioxidant activity assessed as DPPH radical scavenging activity at 50 uM after 20 mins2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
ISSN: 1464-3391		Natural and synthetic 2'-hydroxy-chalcones and aurones: synthesis, characterization and evaluation of the antioxidant and soybean lipoxygenase inhibitory activity.
AID661075Antidiabetic activity in mouse 3T3L1 cells assessed as decrease in glucose consumption from cell culture medium using 450 mg/dL D-glucose at 30 ug/mL after 24 hrs (Rvb = 310 +/- 4 mg/dl)2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
ISSN: 1464-3405		Synthesis of chalcone derivatives as potential anti-diabetic agents.
AID452851Antioxidant activity assessed as superoxide anion radical scavenging activity at 10 uM2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
ISSN: 1464-3391		Natural and synthetic 2'-hydroxy-chalcones and aurones: synthesis, characterization and evaluation of the antioxidant and soybean lipoxygenase inhibitory activity.
AID295382Cytotoxicity against human HT29 cells ATCC HTB38 in aerobic condition assessed as survival at 100 uM by sulforhodamine assay2007Bioorganic & medicinal chemistry, May-15, Volume: 15, Issue:10
ISSN: 0968-0896		Synthetic chalcones, flavanones, and flavones as antitumoral agents: biological evaluation and structure-activity relationships.
AID418269Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 10 uM by MTT assay2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
ISSN: 1464-3405		Inhibitory activity of prostaglandin E2 production by the synthetic 2'-hydroxychalcone analogues: Synthesis and SAR study.
AID452854Antioxidant activity assessed as inhibition of AAPH-induced lipid peroxidation at 10 uM by uV spectrophotometry2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
ISSN: 1464-3391		Natural and synthetic 2'-hydroxy-chalcones and aurones: synthesis, characterization and evaluation of the antioxidant and soybean lipoxygenase inhibitory activity.
AID1737236Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells at 10 uM measured after 24 hrs by Griess reagent based assay relative to control2020European journal of medicinal chemistry, May-01, Volume: 193ISSN: 1768-3254Development of a novel nitric oxide (NO) production inhibitor with potential therapeutic effect on chronic inflammation.
AID418267Inhibition of COX2-mediated PGE2 production in LPS-stimulated mouse RAW264.7 cells at 10 uM by enzyme immunoassay2009Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6
ISSN: 1464-3405		Inhibitory activity of prostaglandin E2 production by the synthetic 2'-hydroxychalcone analogues: Synthesis and SAR study.
AID452852Antioxidant activity assessed as hydroxyl radical scavenging activity at 100 uM2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
ISSN: 1464-3391		Natural and synthetic 2'-hydroxy-chalcones and aurones: synthesis, characterization and evaluation of the antioxidant and soybean lipoxygenase inhibitory activity.
AID295386Growth inhibition of HK2 cells by sulforhodamine assay2007Bioorganic & medicinal chemistry, May-15, Volume: 15, Issue:10
ISSN: 0968-0896		Synthetic chalcones, flavanones, and flavones as antitumoral agents: biological evaluation and structure-activity relationships.
AID513959Cytotoxicity against human HT-29 cells2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
ISSN: 1464-3391		Identification of chalcones as in vivo liver monofunctional phase II enzymes inducers.
AID1698241Inhibition of PMA-induce ROS/RNS generation in human neutrophils at 25 uM measured up to 30 mins in presence of 5.5 mM glucose by luminol-amplified chemiluminescence method relative to control2020Journal of natural products, 10-23, Volume: 83, Issue:10
ISSN: 1520-6025		Chalcones as Modulators of Neutrophil Oxidative Burst under Physiological and High Glucose Conditions.
AID670950Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 at 256 ug/ml after 24 hrs by disc diffusion method2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
ISSN: 1464-3405		Synthesis and anti Methicillin resistant Staphylococcus aureus activity of substituted chalcones alone and in combination with non-beta-lactam antibiotics.
AID1324537Inhibition of Shigella dysenteriae type 1 Shiga toxin A subunit2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
ISSN: 1520-4804		In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin.
AID1186726Cytotoxicity against human NALM6 cells by MTT assay2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
ISSN: 1464-3405		Cytotoxic activity of substituted chalcones in terms of molecular electronic properties.
AID513978Toxicity in Sprague-Dawley rat assessed as change in body weight at 250 mg/kg, po2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
ISSN: 1464-3391		Identification of chalcones as in vivo liver monofunctional phase II enzymes inducers.
AID513958Cytotoxicity against human TK10 cells2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
ISSN: 1464-3391		Identification of chalcones as in vivo liver monofunctional phase II enzymes inducers.
AID295380Cytotoxicity against human TK10 cells in aerobic condition assessed as survival at 100 uM by sulforhodamine assay2007Bioorganic & medicinal chemistry, May-15, Volume: 15, Issue:10
ISSN: 0968-0896		Synthetic chalcones, flavanones, and flavones as antitumoral agents: biological evaluation and structure-activity relationships.
AID638550Inhibition of MDR1 in human A2780adr cells assessed as calcein AM accumulation at 10 uM by fluorimetry2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
ISSN: 1464-3391		Investigation of chalcones and benzochalcones as inhibitors of breast cancer resistance protein.
AID1752771Antischistosomal activity against Schistosoma mansoni BH infected in Balb/c mouse assessed as reduction in worm burden at 400 mg/kg, po measurement after 2 weeks2020RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4
ISSN: 2632-8682		Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here?
AID1698246Inhibition of PMA-induce ROS/RNS generation in human neutrophils at 25 uM measured up to 30 mins in presence of 30 mM glucose by luminol-amplified chemiluminescence method relative to control2020Journal of natural products, 10-23, Volume: 83, Issue:10
ISSN: 1520-6025		Chalcones as Modulators of Neutrophil Oxidative Burst under Physiological and High Glucose Conditions.
AID452856Inhibition of soybean 5-lipoxygenase at 100 uM by UV-absorbance based enzyme assay2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
ISSN: 1464-3391		Natural and synthetic 2'-hydroxy-chalcones and aurones: synthesis, characterization and evaluation of the antioxidant and soybean lipoxygenase inhibitory activity.
AID638477Inhibition of BCRP in human MCF7/MX cells assessed as Hoechst 33342 accumulation preincubated for 30 mins by Fluorometry2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
ISSN: 1464-3391		Investigation of chalcones and benzochalcones as inhibitors of breast cancer resistance protein.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13ISSN: 1934-9300Microsphere-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
ISSN: 1552-4922		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
ISSN: 1557-8127		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 13ISSN: 1934-9300Microsphere-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
ISSN: 1552-4922		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
ISSN: 1557-8127		High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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 13ISSN: 1934-9300Microsphere-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
ISSN: 1552-4922		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
ISSN: 1557-8127		High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression2022The Journal of biological chemistry, 08, Volume: 298, Issue:8
ISSN: 1083-351X
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
ISSN: 1945-7170		A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression2022The Journal of biological chemistry, 08, Volume: 298, Issue:8
ISSN: 1083-351X
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
ISSN: 1945-7170		A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1799680Enzyme Inhibition Assay from Article 10.1080/14756360400015231: \\Synthesis and inhibitory potential towards acetylcholinesterase, butyrylcholinesterase and lipoxygenase of some variably substituted chalcones.\\2005Journal of enzyme inhibition and medicinal chemistry, Feb, Volume: 20, Issue:1
ISSN: 1475-6366		Synthesis and inhibitory potential towards acetylcholinesterase, butyrylcholinesterase and lipoxygenase of some variably substituted chalcones.

Research

Studies (27)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (3.70)18.7374
1990's0 (0.00)18.2507
2000's6 (22.22)29.6817
2010's14 (51.85)24.3611
2020's6 (22.22)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (3.70%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other26 (96.30%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
salicylic acid
1
monohydroxybenzoic acidalgal metabolite;
antifungal agent;
antiinfective agent;
EC 1.11.1.11 (L-ascorbate peroxidase) inhibitor;
keratolytic drug;
plant hormone;
plant metabolite		2014201410.0low000010
gallic acid
1
trihydroxybenzoic acidantineoplastic agent;
antioxidant;
apoptosis inducer;
astringent;
cyclooxygenase 2 inhibitor;
EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor;
geroprotector;
human xenobiotic metabolite;
plant metabolite		2014201410.0low000010
4'-bromoflavone
2
2007201015.5low000200
4-phenyl-3-furoxancarbonitrile
1
1,2,5-oxadiazole;
benzenes;
N-oxide;
nitrile		geroprotector;
nitric oxide donor;
platelet aggregation inhibitor;
soluble guanylate cyclase activator;
vasodilator agent		202020204.0low000010
berberine
1
alkaloid antibiotic;
berberine alkaloid;
botanical anti-fungal agent;
organic heteropentacyclic compound		antilipemic drug;
antineoplastic agent;
antioxidant;
EC 1.1.1.141 [15-hydroxyprostaglandin dehydrogenase (NAD(+))] inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.13.11.52 (indoleamine 2,3-dioxygenase) inhibitor;
EC 1.21.3.3 (reticuline oxidase) inhibitor;
EC 2.1.1.116 [3'-hydroxy-N-methyl-(S)-coclaurine 4'-O-methyltransferase] inhibitor;
EC 2.1.1.122 [(S)-tetrahydroprotoberberine N-methyltransferase] inhibitor;
EC 2.7.11.10 (IkappaB kinase) inhibitor;
EC 3.1.1.4 (phospholipase A2) inhibitor;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor;
EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
geroprotector;
hypoglycemic agent;
metabolite;
potassium channel blocker		2012201212.0low000010
cgs 15943
1
aromatic amine;
biaryl;
furans;
organochlorine compound;
primary amino compound;
quinazolines;
triazoloquinazoline		adenosine A1 receptor antagonist;
adenosine A2A receptor antagonist;
antineoplastic agent;
central nervous system stimulant		202020204.0low000010
ciprofloxacin
1
aminoquinoline;
cyclopropanes;
fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone;
zwitterion		antibacterial drug;
antiinfective agent;
antimicrobial agent;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
environmental contaminant;
topoisomerase IV inhibitor;
xenobiotic		2012201212.0low000010
cl 387785
1
bromobenzenes;
quinazolines;
secondary carboxamide;
ynamide		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist		202020204.0low000010
masoprocol
1
catechols;
lignan;
tetrol		antioxidant;
ferroptosis inhibitor;
geroprotector;
plant metabolite		2009200915.0low000100
n-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide
1
aromatic ether;
C-nitro compound;
sulfonamide		antineoplastic agent;
cyclooxygenase 2 inhibitor		2009200915.0low000100
oxamniquine
1
aromatic primary alcohol;
C-nitro compound;
quinolines;
secondary amino compound		202020204.0low000010
pioglitazone
1
aromatic ether;
pyridines;
thiazolidinediones		antidepressant;
cardioprotective agent;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
geroprotector;
hypoglycemic agent;
insulin-sensitizing drug;
PPARgamma agonist;
xenobiotic		2012201212.0low000010
praziquantel
1
isoquinolines202020204.0low000010
chloramphenicol
1
C-nitro compound;
carboxamide;
diol;
organochlorine compound		antibacterial drug;
antimicrobial agent;
Escherichia coli metabolite;
geroprotector;
Mycoplasma genitalium metabolite;
protein synthesis inhibitor		2012201212.0low000010
adenosine monophosphate
1
adenosine 5'-phosphate;
purine ribonucleoside 5'-monophosphate		adenosine A1 receptor agonist;
cofactor;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
EC 3.1.3.11 (fructose-bisphosphatase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical		201620168.0low000010
salicylaldehyde
1
hydroxybenzaldehydenematicide;
plant metabolite		2014201410.0low000010
furaldehyde
1
aldehyde;
furans		Maillard reaction product;
metabolite		2014201410.0low000010
2'-hydroxyacetophenone
1
monohydroxyacetophenone;
phenols		flavouring agent2014201410.0low000010
piperonal
1
arenecarbaldehyde;
benzodioxoles		fragrance;
insect repellent;
plant metabolite		2014201410.0low000010
3-tert-butyl-4-hydroxyanisole
1
aromatic ether;
phenols		antioxidant;
human xenobiotic metabolite		2014201410.0low000010
2-aminopurine
1
2-aminopurines;
nucleobase analogue		antimetabolite201620168.0low000010
flavanone
2
flavanones2007201413.5low000110
flavone
3
flavonesmetabolite;
nematicide		2007201413.7low000210
3-hydroxyflavone
2
flavonols;
monohydroxyflavone		2013201410.5low000020
erythromycin
1
cyclic ketone;
erythromycin		2012201212.0low000010
vancomycin
1
glycopeptideantibacterial drug;
antimicrobial agent;
bacterial metabolite		2012201212.0low000010
2,6-diaminopurine
1
2,6-diaminopurines;
primary amino compound		antineoplastic agent201620168.0low000010
6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid
2
chromanol;
monocarboxylic acid;
phenols		antioxidant;
ferroptosis inhibitor;
neuroprotective agent;
radical scavenger;
Wnt signalling inhibitor		2009201412.5low000110
adenosine
1
adenosines;
purines D-ribonucleoside		analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent		201620168.0low000010
pinocembrin
1
(2S)-flavan-4-one;
dihydroxyflavanone		antineoplastic agent;
antioxidant;
metabolite;
neuroprotective agent;
vasodilator agent		2014201410.0low000010
4-chromanone
1
chromones2014201410.0low000010
4-aminopyrimidine
1
aminopyrimidine201620168.0low000010
8-azaadenine
1
aromatic amine;
nucleobase analogue;
triazolopyrimidines		EC 1.17.3.2 (xanthine oxidase) inhibitor;
Mycoplasma genitalium metabolite		201620168.0low000010
n-(hydroxymethyl)carbazole
1
2014201410.0medium000010
4'-methoxyflavone
2
ether;
flavonoids		2007201413.5low000110
rosiglitazone
1
aminopyridine;
thiazolidinediones		EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
insulin-sensitizing drug		2012201212.0low000010
mmv665852
1
202020204.0low000010
karanjin
1
extended flavonoid2014201410.0low000010
4'-methoxyflavanone
2
4'-methoxyflavanones2007201015.5medium000200
gr 127935
1
1,2,4-oxadiazole;
benzamides;
N-alkylpiperazine;
N-arylpiperazine		202020204.0low000010
parthenolide
1
germacranolide202020204.0low000010
4'-chloroflavone
2
2007201413.5high000110
e-z cinnamic acid
1
cinnamic acidplant metabolite2014201410.0low000010
clindamycin
1
2012201212.0low000010
gw 3965
1
diarylmethane202020204.0low000010
cinnamaldehyde
1
3-phenylprop-2-enal;
cinnamaldehydes		antifungal agent;
EC 4.3.1.24 (phenylalanine ammonia-lyase) inhibitor;
flavouring agent;
hypoglycemic agent;
plant metabolite;
sensitiser;
vasodilator agent		2014201410.0low000010
trans-4-coumaric acid
1
4-coumaric acidfood component;
mouse metabolite;
plant metabolite		2014201410.0low000010
benzylideneacetone
1
benzylideneacetonebacterial metabolite;
EC 3.1.1.4 (phospholipase A2) inhibitor;
flavouring agent;
fragrance		2014201410.0low000010
chalcone
7
chalconeEC 3.2.1.1 (alpha-amylase) inhibitor2005202012.0low000250
2'-hydroxychalcone
11
chalcones;
phenols		anti-inflammatory agent2005201412.9high000470
2,2'-dihydroxychalcone
2
201220208.0medium000020
cardamonin
1
chalcones202020204.0low000010
3',4',5'-trimethoxyflavonol
1
2013201311.0medium000010
caffeic acid
1
caffeic acidgeroprotector;
mouse metabolite		2009200915.0low000100
stattic
1
1-benzothiophenes;
C-nitro compound;
sulfone		antineoplastic agent;
radiosensitizing agent;
STAT3 inhibitor		202020204.0low000010
enpiroline
1
202020204.0low000010
rs 17053
1
indoles202020204.0low000010
quercetin
3
7-hydroxyflavonol;
pentahydroxyflavone		antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger		2009201412.0low000120
luteolin
1
3'-hydroxyflavonoid;
tetrahydroxyflavone		angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
c-Jun N-terminal kinase inhibitor;
EC 2.3.1.85 (fatty acid synthase) inhibitor;
immunomodulator;
nephroprotective agent;
plant metabolite;
radical scavenger;
vascular endothelial growth factor receptor antagonist		202020204.0low000010
beta carotene
1
carotenoid beta-end derivative;
cyclic carotene		antioxidant;
biological pigment;
cofactor;
ferroptosis inhibitor;
human metabolite;
mouse metabolite;
plant metabolite;
provitamin A		2009200915.0low000100
aureusidin
1
hydroxyauroneplant metabolite2009200915.0low000100
isobavachalcone
1
chalcones;
polyphenol		antibacterial agent;
metabolite;
platelet aggregation inhibitor		202020204.0low000010
galangin
1
7-hydroxyflavonol;
trihydroxyflavone		antimicrobial agent;
EC 3.1.1.3 (triacylglycerol lipase) inhibitor;
plant metabolite		2014201410.0low000010
wogonin
1
dihydroxyflavone;
monomethoxyflavone		angiogenesis inhibitor;
antineoplastic agent;
cyclooxygenase 2 inhibitor;
plant metabolite		2009200915.0low000100
4-hydroxychalcone
4
chalcones;
phenols		antihypertensive agent;
plant metabolite		2005202011.8medium000130
6-methylpurine
1
purinesEC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor201620168.0low000010
licochalcone a
1
chalcones202020204.0low000010
flavokawain a
5
chalcones2007202010.4medium000230
flavokawain b
1
chalcones;
dimethoxybenzene;
phenols		anti-inflammatory agent;
antileishmanial agent;
antineoplastic agent;
apoptosis inducer;
metabolite		202020204.0low000010
Isoliquiritigenin 4,4'-dimethyl ether
3
chalcones201220209.3high000030
2',4'-dihydroxychalcone
3
2012201411.3low000030
4-chlorochalcone
3
chalcones;
monochlorobenzenes		2007202011.7high000210
aldosterone
1
202020204.0low000010
4'-chloroaurone
1
2009200915.0medium000100
Crotaoprostrin
5
chalcones2009202010.4high000140
2',5'-dihydroxychalcone
1
chalcones2014201410.0medium000010
4-hydroxylonchocarpin
1
202020204.0low000010
2-chloro-4',6'-dimethoxy-2'-hydroxychalcone
1
2012201212.0high000010
metochalcone
1
2012201212.0low000010
flavokawain C
1
chalcones202020204.0low000010
broussochalcone a
1
202020204.0low000010
ekb 569
1
aminoquinoline;
monocarboxylic acid amide;
monochlorobenzenes;
nitrile		protein kinase inhibitor202020204.0low000010
ispinesib
1
benzamides202020204.0low000010
gentamicin sulfate
1
2012201212.0low000010
1,2,6,7-tetraoxaspiro(7.11)nonadecane
1
202020204.0low000010
2,4,2',4'-Tetrahydroxychalcone
1
chalcones202020204.0medium000010
sd-208
1
202020204.0low000010
ko 143
1
beta-carbolines;
tert-butyl ester		2012201212.0low000010
Kanzonol B
1
chalcones202020204.0medium000010
bi 2536
1
202020204.0low000010
ascorbic acid
1
ascorbic acid;
vitamin C		coenzyme;
cofactor;
flour treatment agent;
food antioxidant;
food colour retention agent;
geroprotector;
plant metabolite;
skin lightening agent		2014201410.0low000010
bms-833923
1
202020204.0low000010
guanine
1
2-aminopurines;
oxopurine;
purine nucleobase		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite		201620168.0low000010
allopurinol
1
nucleobase analogue;
organic heterobicyclic compound		antimetabolite;
EC 1.17.3.2 (xanthine oxidase) inhibitor;
gout suppressant;
radical scavenger		201620168.0low000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
theophylline
1
dimethylxanthineadenosine receptor antagonist;
anti-asthmatic drug;
anti-inflammatory agent;
bronchodilator agent;
drug metabolite;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
fungal metabolite;
human blood serum metabolite;
immunomodulator;
muscle relaxant;
vasodilator agent		1981198143.0low010000
dyphylline
1
oxopurine;
propane-1,2-diols		bronchodilator agent;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
muscle relaxant;
vasodilator agent		1981198143.0low010000
pioglitazone
1
aromatic ether;
pyridines;
thiazolidinediones		antidepressant;
cardioprotective agent;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
geroprotector;
hypoglycemic agent;
insulin-sensitizing drug;
PPARgamma agonist;
xenobiotic		2012201212.0low000010
ethane
1
alkane;
gas molecular entity		plant metabolite;
refrigerant		202220222.0low000001
dihydrochalcone
1
dihydrochalconesplant metabolite202220222.0low000001
rosiglitazone
1
aminopyridine;
thiazolidinediones		EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
insulin-sensitizing drug		2012201212.0low000010
chalcone
2
chalconeEC 3.2.1.1 (alpha-amylase) inhibitor1981202222.5low010001
2',4'-dihydroxychalcone
1
2007200717.0low000100
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Abnormalities, Autosome0
1
2007200717.0low000100
Anemia, Fanconi0
1
201620168.0low000010
Arteriosclerosis0
1
1981198143.0low010000
Arthritis0
1
202020204.0low000010
Atherogenesis0
1
2012201212.0low000010
Atherosclerosis0
1
2012201212.0low000010
Atrophy, Muscle0
1
202220222.0low000001
Breast Cancer0
1
2012201212.0low000010
Breast Neoplasms0
1
2012201212.0low000010
Cancer of Liver0
1
2010201014.0low000100
Cancer of Ovary0
1
2014201410.0low000010
Chronic Disease0
1
202020204.0low000010
Chronic Illness0
1
202020204.0low000010
Diabetes Mellitus0
1
2012201212.0low000010
Fanconi Anemia0
1
201620168.0low000010
Inflammation0
5
200920229.4medium000221
Innate Inflammatory Response0
5
200920229.4medium000221
Liver Neoplasms0
1
2010201014.0low000100
Muscular Atrophy0
1
202220222.0low000001
Ovarian Neoplasms0
1
2014201410.0low000010
Polyarthritis0
1
202020204.0low000010

Interactions (1)

ArticleYear
Synthesis and anti Methicillin resistant Staphylococcus aureus activity of substituted chalcones alone and in combination with non-beta-lactam antibiotics.
Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 22, Issue:14		2012