Page last updated: 2024-11-12

rpr260243

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Description

RPR260243: small molecule activator of the human ether-a-go-go-related gene (HERG) cardiac K+ channel; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11466357
CHEMBL ID406931
SCHEMBL ID5185288
MeSH IDM0483120

Synonyms (21)

Synonym
cid 11466357
rpr-260243
CHEMBL406931 ,
rpr260243
bdbm50376592
668463-35-2
(3r,4r)-4-[3-(6-methoxyquinolin-4-yl)-3-oxo-propyl]-1-[3-(2,3,5-trifluoro-phenyl)-prop-2-ynyl]-piperidine-3-carboxylic acid
(3r,4r)-4-[3-(6-methoxyquinolin-4-yl)-3-oxopropyl]-1-[3-(2,3,5-trifluorophenyl)prop-2-ynyl]piperidine-3-carboxylic acid
rpr 260243
gtpl7657
SCHEMBL5185288
(3r,4r)-4-[3-oxo-3-(6-methoxyquinolin-4-yl)propyl]-1-[3-(2,3,5-trifluorophenyl)prop-2-ynyl]piperidine-3-carboxylic acid
VWNMWKSURFWKAL-HXOBKFHXSA-N
HY-16915
AKOS025404891
DTXSID90466757
NCGC00402366-02
A914095
Q27088622
F85183
AC-37085

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]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency9.52210.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency7.56370.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency0.30110.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency7.56370.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency7.56370.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency7.56370.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency7.56370.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)EC50 (µMol)11.50000.00192.67568.0000AID329463; AID329464
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Activity9.40000.01104.70559.4000AID329465
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (67)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (29)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (47)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347157Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS2020Proceedings 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.
AID1347161Confirmatory screen NINDS Rhodamine 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.
AID1347160Primary screen NINDS Rhodamine 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.
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.
AID1347169Tertiary RLuc qRT-PCR qHTS assay 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.
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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID329457Activation of ERG1 in guinea pig myocytes assessed as Increase in rapid delayed rectifier potassium tail currents at 10 uM at -50 mV by voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329478Activation of human ERG1 L550A mutant expressed in Xenopus laevis oocytes assessed as shifting of voltage dependence of inactivation towards positive potentials at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329472Activation of human ERG1 N658A mutant expressed in Xenopus laevis oocytes assessed as slowing of tail current deactivation at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329491Activation of human ERG1 Y652A mutant expressed in Xenopus laevis oocytes assessed as shifting of voltage dependence of inactivation towards positive potentials at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329469Activation of human ERG1 V659A mutant expressed in Xenopus laevis oocytes assessed as slowing of tail current deactivation at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329468Activation of human ERG1 N658A mutant expressed in Xenopus laevis oocytes assessed as slowing of tail current deactivation at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329492Effect on human ERG1 S620T/L666A mutant expressed in Xenopus laevis oocytes at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329455Activation of human ERG1 isoform 1 expressed in Xenopus laevis oocytes assessed as enhancement of current magnitude by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329488Activation of human ERG1 isoform 1 expressed in Xenopus laevis oocytes assessed as slowing of tail current deactivation by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329481Inhibition of human ERG1 L666A mutant expressed in Xenopus laevis oocytes assessed as decrease in current amplitude by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329487Effect on human ERG1 G628C/N588K mutant expressed in Xenopus laevis oocytes assessed as current magnitude at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329476Activation of human ERG1 Y667A mutant expressed in Xenopus laevis oocytes assessed as shifting of voltage dependence of inactivation towards positive potentials at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329474Activation of human ERG1 I662A mutant expressed in Xenopus laevis oocytes assessed as shifting of voltage dependence of inactivation towards positive potentials at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329479Activation of human ERG1 F557L mutant expressed in Xenopus laevis oocytes assessed as shifting of voltage dependence of inactivation towards positive potentials at 30 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329486Effect on human ERG1 G628C/S631C mutant expressed in Xenopus laevis oocytes at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329459Activation of human ERG1 isoform 1 expressed in Xenopus laevis oocytes assessed as shifting of voltage dependence of inactivation towards positive potentials at 1 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329489Activation of human ERG1 isoform 1 expressed in Xenopus laevis oocytes assessed as increase in peak tail current at 30 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329460Activation of human ERG1 isoform 1 expressed in Xenopus laevis oocytes assessed as shifting of voltage dependence of inactivation towards positive potentials at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329475Activation of human ERG1 L666A mutant expressed in Xenopus laevis oocytes assessed as shifting of voltage dependence of inactivation towards positive potentials at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329485Effect on human ERG1 S631A/L666A mutant expressed in Xenopus laevis oocytes at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329471Activation of human ERG1 F557L mutant expressed in Xenopus laevis oocytes assessed as slowing of tail current deactivation at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329467Activation of human ERG1 F557L mutant expressed in Xenopus laevis oocytes assessed as slowing of tail current deactivation at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329456Activation of human ERG1 expressed in CHO cells assessed as enhancement of current magnitude at 10 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329461Activation of human ERG1 isoform 1 expressed in Xenopus laevis oocytes assessed as shifting of voltage dependence of inactivation towards positive potentials at 10 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329482Activation of human ERG1 S631A mutant expressed in Xenopus laevis oocytes assessed as slowing of tail current deactivation at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329465Binding affinity to human ERG1 expressed in Xenopus laevis oocytes assessed as half-saturation concentration2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329464Activation of human ERG1 isoform 1 expressed in Xenopus laevis oocytes assessed as increase in peak tail current magnitude by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329477Activation of human ERG1 V549A mutant expressed in Xenopus laevis oocytes assessed as shifting of voltage dependence of inactivation towards positive potentials at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329480Activation of human ERG1 L666A mutant expressed in Xenopus laevis oocytes assessed as shifting of voltage dependence of inactivation towards positive potentials at 30 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329484Activation of human ERG1 L666A mutant expressed in Xenopus laevis oocytes assessed as slowing of tail current deactivation at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329466Activation of human ERG1 L553A mutant expressed in Xenopus laevis oocytes assessed as slowing of tail current deactivation at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329458Activation of ERG1 in guinea pig myocytes assessed as increase in rapid delayed rectifier potassium tail currents at 30 uM at -50 mV by voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329463Activation of human ERG1 isoform 1 expressed in Xenopus laevis oocytes assessed as shifting of voltage dependence of inactivation towards positive potentials by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329483Activation of human ERG1 S631A mutant expressed in Xenopus laevis oocytes assessed as enhancement of current magnitude at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329462Activation of human ERG1 isoform 1 expressed in Xenopus laevis oocytes assessed as shifting of voltage dependence of inactivation towards positive potentials at 30 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329490Activation of human ERG1 Y652A mutant expressed in Xenopus laevis oocytes assessed as slowing of tail current deactivation at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329473Activation of human ERG1 V659A mutant expressed in Xenopus laevis oocytes assessed as slowing of tail current deactivation at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID329470Activation of human ERG1 L553A mutant expressed in Xenopus laevis oocytes assessed as slowing of tail current deactivation at 3 uM by two electrode voltage clamp technique2007Proceedings of the National Academy of Sciences of the United States of America, Aug-21, Volume: 104, Issue:34
Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.
AID1346751Human Kv11.1 (Voltage-gated potassium channels)2005Molecular pharmacology, Mar, Volume: 67, Issue:3
Discovery of a small molecule activator of the human ether-a-go-go-related gene (HERG) cardiac K+ channel.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (26.67)29.6817
2010's6 (40.00)24.3611
2020's5 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.87

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.87 (24.57)
Research Supply Index2.77 (2.92)
Research Growth Index4.64 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.87)

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%
Other15 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]