Compounds > sc 514
Page last updated: 2024-12-10

sc 514

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

Description

SC 514: inhibits IkappaB kinase-2; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2807869
CHEMBL ID193093
CHEBI ID92464
SCHEMBL ID4082097
MeSH IDM0454172

Synonyms (55)

Synonym
bdbm26098
chembl193093 ,
3-amino-5-(thiophen-3-yl)thiophene-2-carboxamide
CURATOR_000007
BRD-K26373640-001-02-8
BIOMOLKI_000076
OPREA1_591652
NCGC00163392-01
sc-514
sc 514
BIOMOLKI2_000080
4-amino-2,3'-bithiophene-5-carboximide
3-amino-5-(3-thienyl)thiophene-2-carboxamide
3-amino-5-thiophen-3-ylthiophene-2-carboxamide
4-amino-[2,3'-bithiophene]-5-carboxamide
5-(thien-3-yl)-3-aminothiophene-2-carboxamide
CCG-100680
HY-13802
CS-1388
FT-0674534
354812-17-2
S4907
3-amino-5-(3-thienyl)-2-thiophenecarboxamide
BMUACLADCKCNKZ-UHFFFAOYSA-N
SCHEMBL4082097
4-amino-[2',3'-bithiophene]-5-carboxamide
sc514
AKOS024457548
gk 01140
CHEBI:92464
HMS3652N12
SW219322-1
sc-514 (gk 01140)
BCP21098
Q27164200
3-amino-5-(3-thiophenyl)-2-thiophenecarboxamide
3-azanyl-5-thiophen-3-yl-thiophene-2-carboxamide
EU3S753TY9
4-amino[2,3'-bithiophene]-5-carboxamide
EX-A2157
HMS3677J04
AS-16630
(2,3'-bithiophene)-5-carboxamide, 4-amino-
HMS3413J04
SB19543
NCGC00163392-13
ikk-2-inhibitor
H12046
NCGC00163392-12
ikk-2 inhibitor
A899632
[2,3'-bithiophene]-5-carboxamide, 4-amino-
DTXSID001257563
4-amino-2,3'-bithiophene-5-carboxamide
AC-35954

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
ring assemblyTwo or more cyclic systems (single rings or fused systems) which are directly joined to each other by double or single bonds are named ring assemblies when the number of such direct ring junctions is one less than the number of cyclic systems involved.
thiophenesCompounds containing at least one thiophene ring.
[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 (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Microtubule-associated protein tauHomo sapiens (human)Potency25.11890.180013.557439.8107AID1460
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency23.75580.011212.4002100.0000AID1030
regulator of G-protein signaling 4Homo sapiens (human)Potency0.18890.531815.435837.6858AID504845
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency14.12540.035520.977089.1251AID504332
[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)
Inhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)IC50 (µMol)7.38000.00090.97819.8200AID1798631; AID241864; AID264519; AID435574
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (30)

Processvia Protein(s)Taxonomy
positive regulation of NF-kappaB transcription factor activityInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
stimulatory C-type lectin receptor signaling pathwayInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class I, TAP-dependentInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
MyD88-dependent toll-like receptor signaling pathwayInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
protein phosphorylationInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
inflammatory responseInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
canonical NF-kappaB signal transductionInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
response to virusInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
regulation of tumor necrosis factor-mediated signaling pathwayInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
peptidyl-serine phosphorylationInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
cortical actin cytoskeleton organizationInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
tumor necrosis factor-mediated signaling pathwayInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
toll-like receptor 3 signaling pathwayInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
negative regulation of myosin-light-chain-phosphatase activityInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
TRIF-dependent toll-like receptor signaling pathwayInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
Fc-epsilon receptor signaling pathwayInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
regulation of phosphorylationInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
innate immune responseInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
positive regulation of DNA-templated transcriptionInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
T cell receptor signaling pathwayInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
stress-activated MAPK cascadeInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
protein maturationInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
interleukin-1-mediated signaling pathwayInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
cellular response to tumor necrosis factorInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
protein localization to plasma membraneInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
regulation of establishment of endothelial barrierInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
negative regulation of bicellular tight junction assemblyInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
regulation of toll-like receptor signaling pathwayInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
protein kinase activityInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
protein serine/threonine kinase activityInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
protein bindingInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
ATP bindingInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
IkappaB kinase activityInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
protein kinase bindingInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
identical protein bindingInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
protein homodimerization activityInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
protein heterodimerization activityInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
scaffold protein bindingInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
protein serine kinase activityInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
transferrin receptor bindingInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
cytoplasmInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
nucleusInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
cytosolInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
IkappaB kinase complexInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
cytoplasmic side of plasma membraneInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
membrane raftInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
CD40 receptor complexInhibitor of nuclear factor kappa-B kinase subunit betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (85)

Assay IDTitleYearJournalArticle
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.
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.
AID435971Percentage MAPKAPK3 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID241864Inhibitory concentration against human recombinant I-kappa-B-kinase 2 from 3 experiments2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides.
AID435356Percentage IKK-beta activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID436080Percentage ERK1 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID1323223Inhibition of TNFalpha-induced NFkappaB activation in mouse NIH-3T3 cells expressing NFkappaB (unknown origin) preincubated for 15 mins followed by TNFalpha addition measured after 6 hrs by luciferase reporter gene assay2016Journal of natural products, 07-22, Volume: 79, Issue:7
Neuroactive and Anti-inflammatory Frankincense Cembranes: A Structure-Activity Study.
AID435234Percentage IKKalpha activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435966Percentage EF2K activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435726Percentage JNK2 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID436078Percentage DYRK2 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435994Percentage SRPK1 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435308Percentage PKCalpha activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435119Percentage MKK1 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435963Percentage CK2 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435745Percentage PLK1 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435341Percentage CHK2 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435859Percentage JNK1 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435968Percentage GSK3-beta activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID436028Percentage PHK activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435494Percentage PRK2 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435993Percentage Src activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435580Percentage Aurora B activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435455Percentage CDK2-cyclinA activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID436038Percentage PIM2 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID364905Inhibition of purified recombinant histidine-HA-tagged IKK-beta expressed in SF9 cells at 10 uM2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
Inhibition of IkappaB kinase-beta and anticancer activities of novel chalcone adamantyl arotinoids.
AID435977Percentage MNK2 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435172Percentage PAK6 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID264519Inhibition of IKK beta2006Journal of medicinal chemistry, May-18, Volume: 49, Issue:10
Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies.
AID435113Percentage MAPKAPK2 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435725Percentage IKKepsilon activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID436064Percentage Aurora C activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435850Percentage DYRK3 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435876Percentage PRAK activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435316Percentage MELK activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435869Percentage p38alpha activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435480Percentage MSK1 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435126Percentage p38-gamma activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435542Percentage PKBbeta activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435622Percentage p38delta activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435241Percentage Lck activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435705Percentage BRSK2 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435840Percentage AMPK activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435459Percentage CK1delta activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435812Percentage PIM1 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435967Percentage ERK8 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435991Percentage SGK1 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435416Percentage PAK4 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID436067Percentage CaMKKbeta activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435628Percentage ROCK2 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435483Percentage NEK2a activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435376Percentage RSK2 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435488Percentage p38beta activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435603Percentage HIPK3 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID436073Percentage CSK activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435631Percentage RSK1 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID590193Antiinflammatory activity in Swiss mouse assessed as inhibition of arachidonic acid-induced ear edema at 10 umol/kg, ip administered 60 mins before arachidonic acid challenge measured after 1 to 6 hrs by electronic digital caliper2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Structure-based design and biological profile of (E)-N-(4-Nitrobenzylidene)-2-naphthohydrazide, a novel small molecule inhibitor of IκB kinase-β.
AID435884Percentage SmMLCK activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435367Percentage NEK6 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435574Inhibition of IKK-beta in the presence of 5uM ATP2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435383Percentage TBK1 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435173Percentage PDK1 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435476Percentage MNK1 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435753Percentage S6K1 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435368Percentage NEK7 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435121Percentage MST2 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435129Percentage PKD1 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435668Percentage PAK5 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435824Percentage PKA activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435682Percentage PIM3 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435597Percentage DYRK1A activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435240Percentage JNK3 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435313Percentage CHK1 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435426Percentage PKBalpha activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435741Percentage PKCzeta activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435844Percentage CaMK1 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435218Percentage CaMKKalpha activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435720Percentage ERK2 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID435973Percentage MARK3 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID436085Percentage HIPK2 activity remaining in the presence of 10uM inhibitor2007The Biochemical journal, Dec-15, Volume: 408, Issue:3
The selectivity of protein kinase inhibitors: a further update.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1798631IKK Inhibition Assay from Article 10.1016/j.bmcl.2005.03.090: \\Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides.\\2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (50)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's11 (22.00)29.6817
2010's34 (68.00)24.3611
2020's5 (10.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.57

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index28.57 (24.57)
Research Supply Index3.93 (2.92)
Research Growth Index4.83 (4.65)
Search Engine Demand Index27.81 (26.88)
Search Engine Supply Index1.75 (0.95)

This Compound (28.57)

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%
Other50 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
benzo(a)pyrene
Benzo(a)pyrene: A potent mutagen and carcinogen. It is a public health concern because of its possible effects on industrial workers, as an environmental pollutant, an as a component of tobacco smoke.. benzo[a]pyrene : An ortho- and peri-fused polycyclic arene consisting of five fused benzene rings.		2.0410ortho- and peri-fused polycyclic arenecarcinogenic agent;
mouse metabolite
go 6976
[no description available]		2.0310indolocarbazole;
organic heterohexacyclic compound		EC 2.7.11.13 (protein kinase C) inhibitor
n-(2-(methylamino)ethyl)-5-isoquinolinesulfonamide
[no description available]		2.0310isoquinolines;
sulfonamide
fasudil
fasudil: intracellular calcium antagonist; structure in first source. fasudil : An isoquinoline substituted by a (1,4-diazepan-1-yl)sulfonyl group at position 5. It is a Rho-kinase inhibitor and its hydrochloride hydrate form is approved for the treatment of cerebral vasospasm and cerebral ischemia.		2.0310isoquinolines;
N-sulfonyldiazepane		antihypertensive agent;
calcium channel blocker;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
geroprotector;
neuroprotective agent;
nootropic agent;
vasodilator agent
harmaline
Harmaline: A beta-carboline alkaloid isolated from seeds of PEGANUM.. harmaline : A harmala alkaloid in which the harman skeleton is methoxy-substituted at C-7 and has been reduced across the 3,4 bond.		2.0310harmala alkaloidoneirogen
harmalol
harmalol: inhibitor of rat liver microsomal UDP-glucuronyltransferase; RN given refers to parent cpd; structure. harmalol : A harmala alkaloid in which the harman skeleton is hydroxy-substituted at C-7 and has been reduced across the 3,4 bond.		2.0310harmala alkaloidalgal metabolite;
EC 1.4.3.4 (monoamine oxidase) inhibitor
ic 261
[no description available]		2.0310indoles
nsc 664704
kenpaullone: inhibits CDK1/cyclin B; structure in first source. kenpaullone : An indolobenzazepine that is paullone in which the hydrogen at position 9 is replaced by a bromo substituent. It is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs) and glycogen synthase kinase 3beta (GSK3beta).		2.0310indolobenzazepine;
lactam;
organobromine compound		cardioprotective agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
geroprotector
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first source		2.9640chromones;
morpholines;
organochlorine compound		autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector
pd 98059
2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one: inhibits MAP kinase kinase (MEK) activity, p42 MAPK and p44 MAPK; structure in first source. 2-(2-amino-3-methoxyphenyl)chromen-4-one : A member of the class of monomethoxyflavones that is 3'-methoxyflavone bearing an additional amino substituent at position 2'.		2.0710aromatic amine;
monomethoxyflavone		EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector
1-NA-PP1
[no description available]		2.0310pyrazolopyrimidinetyrosine kinase inhibitor
ag 1879
3-(4-chlorophenyl)-1-(1,1-dimethylethyl)-1H-pyrazolo(3,4-d)pyrimidin-4-amine: Fyn kinase inhibitor		2.0310aromatic amine;
monochlorobenzenes;
pyrazolopyrimidine		beta-adrenergic antagonist;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector
ro 31-8220
Ro 31-8220: a protein kinase C inhibitor		2.0310imidothiocarbamic ester;
indoles;
maleimides		EC 2.7.11.13 (protein kinase C) inhibitor
sb 202190
4-(4-fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)imidazole: structure given in first source; inhibits p38 MAP kinase		2.7430imidazoles;
organofluorine compound;
phenols;
pyridines		apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
sevoflurane
Sevoflurane: A non-explosive inhalation anesthetic used in the induction and maintenance of general anesthesia. It does not cause respiratory irritation and may also prevent PLATELET AGGREGATION.. sevoflurane : An ether compound having fluoromethyl and 1,1,1,3,3,3-hexafluoroisopropyl as the two alkyl groups.		2.0510ether;
organofluorine compound		central nervous system depressant;
inhalation anaesthetic;
platelet aggregation inhibitor
zm 336372
N-(5-(3-dimethylaminobenzamido)-2-methylphenyl)-4-hydroxybenzamide: an inhibitor of c-Raf; activates Raf-1; structure in first source		2.0310benzamides
serine
Serine: A non-essential amino acid occurring in natural form as the L-isomer. It is synthesized from GLYCINE or THREONINE. It is involved in the biosynthesis of PURINES; PYRIMIDINES; and other amino acids.. serine : An alpha-amino acid that is alanine substituted at position 3 by a hydroxy group.		2.0210L-alpha-amino acid;
proteinogenic amino acid;
serine family amino acid;
serine zwitterion;
serine		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
gliotoxin
Gliotoxin: A fungal toxin produced by various species of Trichoderma, Gladiocladium fimbriatum, Aspergillus fumigatus, and Penicillium. It is used as an immunosuppressive agent.. gliotoxin : A pyrazinoindole with a disulfide bridge spanning a dioxo-substituted pyrazine ring; mycotoxin produced by several species of fungi.		2.0410dipeptide;
organic disulfide;
organic heterotetracyclic compound;
pyrazinoindole		antifungal agent;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
immunosuppressive agent;
mycotoxin;
proteasome inhibitor
thymol
Thymol: A phenol obtained from thyme oil or other volatile oils used as a stabilizer in pharmaceutical preparations, and as an antiseptic (antibacterial or antifungal) agent.. thymol : A phenol that is a natural monoterpene derivative of cymene.		2.1310monoterpenoid;
phenols		volatile oil component
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		5.07390mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
pyrazolanthrone
pyrazolanthrone: JNK (c-Jun N-terminal kinase) inhibitor; structure in first source. anthra[1,9-cd]pyrazol-6(2H)-one : A member of the class of anthrapyrazoles that is anthra[1,9-cd]pyrazole substituted at position 6 by an oxo group. An inhibitor of c-Jun N-terminal kinase.		2.4520anthrapyrazole;
aromatic ketone;
cyclic ketone		antineoplastic agent;
c-Jun N-terminal kinase inhibitor;
geroprotector
pyrazines
Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.		2.0810diazine;
pyrazines		Daphnia magna metabolite
methamphetamine
Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.. methamphetamine : A member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent.		2.0710amphetamines;
secondary amine		central nervous system stimulant;
environmental contaminant;
neurotoxin;
psychotropic drug;
xenobiotic
malondialdehyde
Malondialdehyde: The dialdehyde of malonic acid.. malonaldehyde : A dialdehyde that is propane substituted by two oxo groups at the terminal carbon atoms respectively. A biomarker of oxidative damage to lipids caused by smoking, it exists in vivo mainly in the enol form.		2.1710dialdehydebiomarker
acetylcysteine
N-acetyl-L-cysteine : An N-acetyl-L-amino acid that is the N-acetylated derivative of the natural amino acid L-cysteine.		2.0710acetylcysteine;
L-cysteine derivative;
N-acetyl-L-amino acid		antidote to paracetamol poisoning;
antiinfective agent;
antioxidant;
antiviral drug;
ferroptosis inhibitor;
geroprotector;
human metabolite;
mucolytic;
radical scavenger;
vulnerary
tetradecanoylphorbol acetate
Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.. phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.. phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types.		2.0710acetate ester;
diester;
phorbol ester;
tertiary alpha-hydroxy ketone;
tetradecanoate ester		antineoplastic agent;
apoptosis inducer;
carcinogenic agent;
mitogen;
plant metabolite;
protein kinase C agonist;
reactive oxygen species generator
staurosporine
[no description available]		2.0610indolocarbazole alkaloid;
organic heterooctacyclic compound		apoptosis inducer;
bacterial metabolite;
EC 2.7.11.13 (protein kinase C) inhibitor;
geroprotector
phorbolol myristate acetate
[no description available]		2.0710
cki 7
N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide: casein kinase I inhibitor; structure given in first source. N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide : A member of the class of isoquinolines that is isoquinoline-8-sulfonamide which is substituted by chlorine at position 5 and in which the sulfonamide nitrogen is substituted by a 2-aminoethyl group. It is an inhibitor of casein kinase I.		2.0310isoquinolines;
organochlorine compound;
primary amino compound;
sulfonamide		EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
ruboxistaurin
ruboxistaurin: inhibits protein kinase C beta; structure in first source		2.0310
birb 796
[no description available]		2.0310aromatic ether;
morpholines;
naphthalenes;
pyrazoles;
ureas		EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
immunomodulator
cyc 202
seliciclib : 2,6-Diaminopurine carrying benzylamino, (2R)-1-hydroxybutan-2-yl and isopropyl substituents at C-6, C-2-N and N-9 respectively. It is an experimental drug candidate in the family of pharmacological cyclin-dependent kinase (CDK) inhibitors.		2.03102,6-diaminopurinesantiviral drug;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
sb 203580
[no description available]		2.9940imidazoles;
monofluorobenzenes;
pyridines;
sulfoxide		EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent
sb 216763
[no description available]		2.0310indoles;
maleimides
sorafenib
[no description available]		2.0310(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide		angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor
wortmannin
[no description available]		2.0310acetate ester;
cyclic ketone;
delta-lactone;
organic heteropentacyclic compound		anticoronaviral agent;
antineoplastic agent;
autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector;
Penicillium metabolite;
radiosensitizing agent
bortezomib
[no description available]		2.0810amino acid amide;
L-phenylalanine derivative;
pyrazines		antineoplastic agent;
antiprotozoal drug;
protease inhibitor;
proteasome inhibitor
leupeptins
Leupeptins: A group of acylated oligopeptides produced by Actinomycetes that function as protease inhibitors. They have been known to inhibit to varying degrees trypsin, plasmin, KALLIKREINS, papain and the cathepsins.		2.0810
n-(4-methoxybenzyl)-n'-(5-nitro-1,3-thiazol-2-yl)urea
N-(4-methoxybenzyl)-N'-(5-nitro-1,3-thiazol-2-yl)urea: structure in first source		2.0310
y 27632
Y 27632: RN given for di-HCl salt; inhibits Rho-associated protein kinase; inhibits calcium sensitization to affect smooth muscle relaxation; structure in first source. Y-27632 : A monocarboxylic acid amide that is trans-[(1R)-1-aminoethyl]cyclohexanecarboxamide in which one of the nitrogens of the aminocarbony group is substituted by a pyridine nucleus. It has been shown to exhibit inhibitory activity against Rho-associated protein kinase (ROCK) enzyme.		2.0310aromatic amide
h 1152
(S)-2-methyl-1-(4-methylisoquinoline-5-sulfonyl)-1,4-diazepane : A member of the class of isoquinolines that is the sulfonamide formed by the formal condensation of the sulfo group of 4-methylisoquinoline-5-sulfonic acid with the 1-amino group of (S)-2-methyl-1,4-diazepane.		2.0310isoquinolines;
N-sulfonyldiazepane		EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
h 89
N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide: structure given in first source. N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A member of the class of isoquinolines that is the sulfonamide obtained by formal condensation of the sulfo group of isoquinoline-5-sulfonic acid with the primary amino group of N(1)-[3-(4-bromophenyl)prop-2-en-1-yl]ethane-1,2-diamine. It is a protein kinase A inhibitor.. (E)-N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide in which the double bond adopts a trans-configuration.		2.4520N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide
purvalanol a
6-((3-chloro)anilino)-2-(isopropyl-2-hydroxyethylamino)-9-isopropylpurine: purvalanol A is the (1R)-isomer;		2.0310purvalanol
benzyloxycarbonylleucyl-leucyl-leucine aldehyde
benzyloxycarbonylleucyl-leucyl-leucine aldehyde: proteasome inhibitor. N-benzyloxycarbonyl-L-leucyl-L-leucyl-L-leucinal : A tripeptide that is L-leucyl-L-leucyl-L-leucine in which the C-terminal carboxy group has been reduced to the corresponding aldehyde and the N-terminal amino group is protected as its benzyloxycarbonyl derivative.		2.0810amino aldehyde;
carbamate ester;
tripeptide		proteasome inhibitor
curcumin
Curcumin: A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes.. curcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by feruloyl groups. A natural dyestuff found in the root of Curcuma longa.		2.1710aromatic ether;
beta-diketone;
diarylheptanoid;
enone;
polyphenol		anti-inflammatory agent;
antifungal agent;
antineoplastic agent;
biological pigment;
contraceptive drug;
dye;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
flavouring agent;
food colouring;
geroprotector;
hepatoprotective agent;
immunomodulator;
iron chelator;
ligand;
lipoxygenase inhibitor;
metabolite;
neuroprotective agent;
nutraceutical;
radical scavenger
Src Inhibitor-1
Src Inhibitor-1 : A member of the class of quinazolines that is quinazoline which is substituted at position 4 by a p-phenoxyanilino group and at positions 6 and 7 by methoxy groups. It is a potent, competitive dual site (both the ATP- and peptide-binding) Src kinase inhibitor. Src Inhibitor-1 is one of the 'gold standards' for Src kinase inhibition that has been shown to use PP1 or PP2 in parallel with Src-I1 to inhbit Src family kinases.		2.0310aromatic ether;
polyether;
quinazolines;
secondary amino compound		EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
u 0126
U 0126: protein kinase kinase inhibitor; structure in first source		2.0310aryl sulfide;
dinitrile;
enamine;
substituted aniline		antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
osteogenesis regulator;
vasoconstrictor agent
7-epi-hydroxystaurosporine
[no description available]		2.0310
sb 415286
3-(3-chloro-4-hydroxyphenylamino)-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione: a glycogen synthase kinase-3 inhibitor; structure in first source		2.0310C-nitro compound;
maleimides;
monochlorobenzenes;
phenols;
secondary amino compound;
substituted aniline		antioxidant;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
neuroprotective agent
alsterpaullone
alsterpaullone: structure in first source. alsterpaullone : An organic heterotetracyclic compound that is 1,3-dihydro-2H-1-benzazepin-2-one which shares its 4-5 bond with the 3-2 bond of 5-nitro-1H-indole.		2.0310C-nitro compound;
caprolactams;
organic heterotetracyclic compound		anti-HIV-1 agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
EC 2.7.11.26 (tau-protein kinase) inhibitor
1-tert-butyl-3-naphthalen-1-ylmethyl-1h-pyrazolo(3,4-d)pyrimidin-4-ylemine
[no description available]		2.0310pyrazolopyrimidinetyrosine kinase inhibitor
dinoprostone
prostaglandin E2 : Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostaglandins.		2.0610prostaglandins Ehuman metabolite;
mouse metabolite;
oxytocic
dinoprost
Dinoprost: A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions.. prostaglandin F2alpha : A prostaglandins Falpha that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15. It is a naturally occurring prostaglandin used to induce labor.		2.2510monocarboxylic acid;
prostaglandins Falpha		human metabolite;
mouse metabolite
harmine
Harmine: Alkaloid isolated from seeds of PEGANUM HARMALA; ZYGOPHYLLACEAE. It is identical to banisterine, or telepathine, from Banisteria caapi and is one of the active ingredients of hallucinogenic drinks made in the western Amazon region from related plants. It has no therapeutic use, but (as banisterine) was hailed as a cure for postencephalitic PARKINSON DISEASE in the 1920's.. harmine : A harmala alkaloid in which the harman skeleton is methoxy-substituted at C-7.		2.0310harmala alkaloidanti-HIV agent;
EC 1.4.3.4 (monoamine oxidase) inhibitor;
metabolite
harman
harman: a beta-carboline; RN given refers to parent cpd; structure. harman : An indole alkaloid fundamental parent with a structure of 9H-beta-carboline carrying a methyl substituent at C-1. It has been isolated from the bark of Sickingia rubra, Symplocus racemosa, Passiflora incarnata, Peganum harmala, Banisteriopsis caapi and Tribulus terrestris, as well as from tobacco smoke. It is a specific, reversible inhibitor of monoamine oxidase A.		2.0310harmala alkaloid;
indole alkaloid fundamental parent;
indole alkaloid		anti-HIV agent;
EC 1.4.3.4 (monoamine oxidase) inhibitor;
plant metabolite
rottlerin
rottlerin: an angiogenesis inhibitor; an inhibitor of protein kinase Cdelta (PKCdelta) and calmodulin kinase III; RN refers to (E)-isomer; do not confuse this chalcone with an anthraquinone that is also called rottlerin (RN 481-72-1);. rottlerin : A chromenol that is 2,2-dimethyl-2H-chromene substituted by hydroxy groups at positions 5 and 7, a 3-acetyl-2,4,6-trihydroxy-5-methylbenzyl group at position 6 and a (1E)-3-oxo-1-phenylprop-1-en-3-yl group at position 8. A potassium channel opener, it is isolated from Mallotus philippensis.		2.0310aromatic ketone;
benzenetriol;
chromenol;
enone;
methyl ketone		anti-allergic agent;
antihypertensive agent;
antineoplastic agent;
apoptosis inducer;
K-ATP channel agonist;
metabolite
sirolimus
Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.		2.0310antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol		antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
fluprostenol
fluprostenol: synthetic prostaglandin F 2 alpha analog used as an abortifacient; RN given refers to ((1alpha(Z),2beta(1E,3R*),3alpha,5alpha)-(+-))-isomer. fluprostenol : An organofluorine compound that is racemic prostaglandin F2alpha in which the pentyl group is replaced by a 3-(trifluoromethyl)phenoxymethyl group. A synthetic analogue of prostaglandin F2alpha, ophthalmic solutions of its isopropyl ester prodrug, travoprost, are used as a topical medication for controlling the progression of open-angle glaucoma and ocular hypertension, by reducing intraocular pressure. The isopropyl ester group of travoprost is hydrolysed to the biologically active free acid by esterases in the cornea.		2.2510(trifluoromethyl)benzenes;
hydroxy monocarboxylic acid;
prostaglandins Falpha		abortifacient;
antiglaucoma drug;
antihypertensive agent;
female contraceptive drug;
prostaglandin receptor agonist
su 6656
SU 6656: a c-Src kinase inhibitor; used to probe growth signaling; structure in first source. SU6656 : A member of the class of oxindoles that is 3-methyleneoxindole in which the hydrogeh at position 5 has been replaced by a dimethylaminosulfonyl group and in which one of the hydrogens of the methylene group has been replaced by a 4,5,6,7-tetrahydro-indol-2-yl group. It is a specific inhibitor of Src family kinase.		2.0310
orantinib
orantinib: an antiangiogenic agent. orantinib : An oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is substituted by a 2-(2-carboxyethyl)-3,5-dimethylpyrrol-3-yl group. It is an ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth factor receptor 1.		2.0310
vx680
[no description available]		2.0310N-arylpiperazine
d 4476
[no description available]		2.0310imidazoles
mdl 201053
MDL 201053: Immunosuppressive Agent; RN given refers to compound with no isomeric designation		2.0810
pd 184352
2-(2-chloro-4-iodophenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamide: inhibits MAP kinase kinase; structure in first source		2.0310aminobenzoic acid
bms345541
4(2'-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline: structure in first source		2.0310quinoxaline derivative
pd 0325901
mirdametinib: has antineoplastic activity; appears to be a MEK inhibitor. PD 0325901 : A hydroxamic acid ester that is benzhydroxamic acid (N-hydroxybenzamide) in which the hydroxamic acid group has been converted to the corresponding 2,3-dihydroxypropyl ester and in which the benzene ring has been substituted at position 2 by a (2-fluoro-4-iodophenyl)amino group and at positions 3 and 4 by fluorines (the R enantiomer).		2.0310difluorobenzene;
hydroxamic acid ester;
monofluorobenzenes;
organoiodine compound;
propane-1,2-diols;
secondary amino compound		antineoplastic agent;
EC 2.7.12.2 (mitogen-activated protein kinase kinase) inhibitor
pi103
PI103: pyridofuropyrimidine antineoplastic; a potent inhibitor of class I phosphatidylinositide 3-kinases (PI3K); structure in first soruce		2.0310aromatic amine;
morpholines;
organic heterotricyclic compound;
phenols;
tertiary amino compound		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor
bms 204493
BMS-493 : A member of the class of dihydronaphthalenes that is 1,2-dihydronaphthalene which is substituted at positions 1, 1, 4, and 6 by methyl, methyl, phenylethynyl, and 2-(p-carboxyphenyl)vinyl groups, respectively (the E isomer).		2.0410acetylenic compound;
benzoic acids;
dihydronaphthalenes;
stilbenoid		retinoic acid receptor antagonist
bms345541
[no description available]		2.0410
ps1145
PS1145: IkappaB kinase inhibitor; structure in first source		2.0310beta-carbolines
chir 99021
Chir 99021: structure in first source. CHIR 99021 : A member of the class of aminopyrimidines that is 2-aminopyrimidine substituted at positions N2, 5 and 6 by (5-cyanopyridin-2-yl)ethyl, 4-methylimidazol-2-yl and 2,4-dichlorophenyl groups respectively.		2.0310aminopyridine;
aminopyrimidine;
cyanopyridine;
diamine;
dichlorobenzene;
imidazoles;
secondary amino compound		EC 2.7.11.26 (tau-protein kinase) inhibitor
bx795
BX795: structure in first source		2.0310ureas
a 443654
A 443654: an Akt kinase inhibitor; structure in first source		2.0310indoles
sl0101
SL0101: p90 Ribosomal S6 Kinase; structure in first source		2.0310
dorsomorphin
dorsomorphin: an AMPK inhibitor. dorsomorphin : A pyrazolopyrimidine that is pyrazolo[1,5-a]pyrimidine which is substituted at positions 3 and 6 by pyridin-4-yl and p-[2-(piperidin-1-yl)ethoxy]phenyl groups, respectively. It is a potent, selective, reversible, and ATP-competitive inhibitor of AMPK (AMP-activated protein kinase, EC 2.7.11.31) and a selective inhibitor of bone morphogenetic protein (BMP) signaling.		2.0310aromatic ether;
piperidines;
pyrazolopyrimidine;
pyridines		bone morphogenetic protein receptor antagonist;
EC 2.7.11.31 {[hydroxymethylglutaryl-CoA reductase (NADPH)] kinase} inhibitor
cgp 57380
CGP 57380: inhibits the mitogen-activated protein kinase-interacting kinase Mnk1		2.0310pyrazolopyrimidine
cytochrome c-t
Cytochromes c: Cytochromes of the c type that are found in eukaryotic MITOCHONDRIA. They serve as redox intermediates that accept electrons from MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX III and transfer them to MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX IV.		2.4520
oligonucleotides
[no description available]		2.0610
jsh 23
4-methyl-N1-(3-phenylpropyl)benzene-1,2-diamine: structure in first source. JSH-23 : A diamine that is 1,2-phenylenediamine carrying a methyl substituent at position 4 and a 3-phenylpropyl substituent at position N1.		2.0510diamine;
substituted aniline		NF-kappaB inhibitor
bi d1870
[no description available]		2.0310
interleukin-8
Interleukin-8: A member of the CXC chemokine family that plays a role in the regulation of the acute inflammatory response. It is secreted by variety of cell types and induces CHEMOTAXIS of NEUTROPHILS and other inflammatory cells.		2.4820
akt-i-1,2 compound
Akt-I-1,2 compound: an aminopeptidase P inhibitor; structure in first source		2.0310
ConditionIndicatedRelationship StrengthStudiesTrials
Anasarca
[description not available]		02.0610
Edema
Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.		02.0610
Plasmodium falciparum Malaria
[description not available]		02.110
Malaria, Falciparum
Malaria caused by PLASMODIUM FALCIPARUM. This is the severest form of malaria and is associated with the highest levels of parasites in the blood. This disease is characterized by irregularly recurring febrile paroxysms that in extreme cases occur with acute cerebral, renal, or gastrointestinal manifestations.		02.110
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.9130
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Diabetes Mellitus, Adult-Onset
[description not available]		02.2510
Innate Inflammatory Response
[description not available]		02.7830
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.		02.2510
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		02.7830
Diabetic Cardiomyopathies
Diabetes complications in which VENTRICULAR REMODELING in the absence of CORONARY ATHEROSCLEROSIS and hypertension results in cardiac dysfunctions, typically LEFT VENTRICULAR DYSFUNCTION. The changes also result in myocardial hypertrophy, myocardial necrosis and fibrosis, and collagen deposition due to impaired glucose tolerance.		02.2510
Benign Neoplasms
[description not available]		02.1710
Angiogenesis, Pathologic
[description not available]		02.1710
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		02.1710
Bronze Diabetes
[description not available]		02.1710
Hemochromatosis
A disorder of iron metabolism characterized by a triad of HEMOSIDEROSIS; LIVER CIRRHOSIS; and DIABETES MELLITUS. It is caused by massive iron deposits in parenchymal cells that may develop after a prolonged increase of iron absorption. (Jablonski's Dictionary of Syndromes & Eponymic Diseases, 2d ed)		02.1710
Cancer of Stomach
[description not available]		02.2110
Stomach Neoplasms
Tumors or cancer of the STOMACH.		02.2110
Preterm Birth
[description not available]		02.1710
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		02.1710
Premature Birth
CHILDBIRTH before 37 weeks of PREGNANCY (259 days from the first day of the mother's last menstrual period, or 245 days after FERTILIZATION).		02.1710
Dermatitis
Any inflammation of the skin.		02.0810
Alloxan Diabetes
[description not available]		02.1110
Asymmetric Diabetic Proximal Motor Neuropathy
[description not available]		02.1110
Peripheral Nerve Diseases
[description not available]		02.1110
Diabetic Neuropathies
Peripheral, autonomic, and cranial nerve disorders that are associated with DIABETES MELLITUS. These conditions usually result from diabetic microvascular injury involving small blood vessels that supply nerves (VASA NERVORUM). Relatively common conditions which may be associated with diabetic neuropathy include third nerve palsy (see OCULOMOTOR NERVE DISEASES); MONONEUROPATHY; mononeuropathy multiplex; diabetic amyotrophy; a painful POLYNEUROPATHY; autonomic neuropathy; and thoracoabdominal neuropathy. (From Adams et al., Principles of Neurology, 6th ed, p1325)		02.1110
Peripheral Nervous System Diseases
Diseases of the peripheral nerves external to the brain and spinal cord, which includes diseases of the nerve roots, ganglia, plexi, autonomic nerves, sensory nerves, and motor nerves.		02.1110
Cancer of Cervix
[description not available]		02.1310
Uterine Cervical Neoplasms
Tumors or cancer of the UTERINE CERVIX.		02.1310
Malignant Melanoma
[description not available]		02.1510
Metastase
[description not available]		02.1510
Melanoma
A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)		02.1510
Neoplasm Metastasis
The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.		02.1510
Injury, Myocardial Reperfusion
[description not available]		02.0510
Atrophy, Muscle
[description not available]		02.0510
Muscular Atrophy
Derangement in size and number of muscle fibers occurring with aging, reduction in blood supply, or following immobilization, prolonged weightlessness, malnutrition, and particularly in denervation.		02.0510
Depression, Endogenous
[description not available]		02.0510
Depressive Disorder
An affective disorder manifested by either a dysphoric mood or loss of interest or pleasure in usual activities. The mood disturbance is prominent and relatively persistent.		02.0510
Allodynia
[description not available]		02.0610
Cardiac Diseases
[description not available]		02.0710
Heart Diseases
Pathological conditions involving the HEART including its structural and functional abnormalities.		02.0710
Atherogenesis
[description not available]		02.0710
Atherosclerosis
A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.		02.0710
Polyarthritis
[description not available]		02.0710
Arthritis
Acute or chronic inflammation of JOINTS.		02.0710