Page last updated: 2024-11-13

LimKi 3

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

Description

LIMKi3: LIMK inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

LimKi 3 : A member of the class of pyrazoles that is 1-(2,6-dichlorophenyl)-1H-pyrazole which is substituted by a difluoromethyl group at position 3 and by a 2-(isobutyrylamino)-1,3-thiazol-5-yl group at position 5. It is a a potent cell-permeable inhibitor of LIM kinase 1 and 2. [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]

Cross-References

ID SourceID
PubMed CID56965901
CHEMBL ID2141887
CHEBI ID138670
SCHEMBL ID15543888

Synonyms (44)

Synonym
n-(5-(1-(2,6-dichlorophenyl)-3-(difluoromethyl)-1h-pyrazol-5-yl)thiazol-2-yl)isobutyramide
lim kinase inhibitor i
CHEBI:138670
n-{5-[1-(2,6-dichlorophenyl)-3-(difluoromethyl)-1h-pyrazol-5-yl]-1,3-thiazol-2-yl}-2-methylpropanamide
1338247-35-0
limki 3
HMS3244J07
HMS3244I07
HMS3244I08
NCGC00263197-01
CHEMBL2141887 ,
c17h14cl2f2n4os
bms-5
SCHEMBL15543888
bms 5 ,
n-[5-[1-(2,6-dichlorophenyl)-3-(difluoromethyl)-1h-pyrazol-5-yl]-2-thiazolyl]-2-methylpropanamide
AC-35331
AKOS024458322
J-523083
n-[5-[2-(2,6-dichlorophenyl)-5-(difluoromethyl)pyrazol-3-yl]-1,3-thiazol-2-yl]-2-methylpropanamide
HY-18305
EX-A934
CS-5617
mfcd17019327
NCGC00263197-03
gtpl9839
limki3
FT-0700442
BCP17223
AS-16195
limki-3 (bms-5)
limki-3
HMS3743I19
bms5
A888014
n-{5-[1-(2,6-dichlorophenyl)-3-(difluoromethyl)-1h-pyrazol-5-yl]- 1,3-thiazol-2-yl}-2-methylpropanamide
DTXSID201113664
propanamide, n-[5-[1-(2,6-dichlorophenyl)-3-(difluoromethyl)-1h-pyrazol-5-yl]-2-thiazolyl]-2-methyl-
S0185
LH0 ,
bdbm50591090
ivugbsglhrjssp-uhfffaoysa-n
EN300-115361
Z1460124046

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]

Roles (1)

RoleDescription
LIM kinase inhibitorAn that interferes with the activity of any of the actin-binding kinases that phosphorylate members of the ADF/cofilin family of actin binding and filament severing proteins.
[role 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]

Drug Classes (5)

ClassDescription
pyrazoles
1,3-thiazoles
dichlorobenzeneAny member of the class of chlorobenzenes carrying two chloro groups at unspecified positions.
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
secondary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a primary amine; formula RC(=O)NHR(1).
[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 (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency13.20660.00308.794948.0869AID1347053
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency6.00810.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency35.19730.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
GVesicular stomatitis virusPotency5.35470.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency10.68400.00108.379861.1304AID1645840
polyproteinZika virusPotency13.20660.00308.794948.0869AID1347053
tyrosine-protein kinase YesHomo sapiens (human)Potency27.40380.00005.018279.2586AID686947
Interferon betaHomo sapiens (human)Potency5.35470.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency5.35470.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency5.35470.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency5.35470.01238.964839.8107AID1645842
[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)
LIM domain kinase 1Homo sapiens (human)IC50 (µMol)0.05770.00240.32451.7783AID1856745; AID1856747; AID1856749; AID1856820; AID1857470; AID1857472; AID1857474; AID1857476
LIM domain kinase 2Homo sapiens (human)IC50 (µMol)0.08750.00801.25137.9433AID1856746; AID1856748; AID1856750; AID1856821; AID1857471; AID1857473; AID1857475; AID1857476
[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)
LIM domain kinase 1Homo sapiens (human)Kd0.05900.02601.784021.0890AID1856751
LIM domain kinase 2Homo sapiens (human)Kd0.05700.05704.971752.0560AID1856752
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (66)

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)
protein phosphorylationLIM domain kinase 1Homo sapiens (human)
signal transductionLIM domain kinase 1Homo sapiens (human)
Rho protein signal transductionLIM domain kinase 1Homo sapiens (human)
nervous system developmentLIM domain kinase 1Homo sapiens (human)
positive regulation of actin filament bundle assemblyLIM domain kinase 1Homo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisLIM domain kinase 1Homo sapiens (human)
stress fiber assemblyLIM domain kinase 1Homo sapiens (human)
positive regulation of axon extensionLIM domain kinase 1Homo sapiens (human)
axon extensionLIM domain kinase 1Homo sapiens (human)
negative regulation of ubiquitin-protein transferase activityLIM domain kinase 1Homo sapiens (human)
positive regulation of stress fiber assemblyLIM domain kinase 1Homo sapiens (human)
actin cytoskeleton organizationLIM domain kinase 1Homo sapiens (human)
positive regulation of protein phosphorylationLIM domain kinase 2Homo sapiens (human)
protein phosphorylationLIM domain kinase 2Homo sapiens (human)
spermatogenesisLIM domain kinase 2Homo sapiens (human)
phosphorylationLIM domain kinase 2Homo sapiens (human)
astral microtubule organizationLIM domain kinase 2Homo sapiens (human)
establishment of vesicle localizationLIM domain kinase 2Homo sapiens (human)
head developmentLIM domain kinase 2Homo sapiens (human)
cornea development in camera-type eyeLIM domain kinase 2Homo sapiens (human)
positive regulation of protein localization to nucleusLIM domain kinase 2Homo sapiens (human)
negative regulation of cilium assemblyLIM domain kinase 2Homo sapiens (human)
actin cytoskeleton organizationLIM domain kinase 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 (23)

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)
protein kinase activityLIM domain kinase 1Homo sapiens (human)
protein serine/threonine kinase activityLIM domain kinase 1Homo sapiens (human)
protein bindingLIM domain kinase 1Homo sapiens (human)
ATP bindingLIM domain kinase 1Homo sapiens (human)
heat shock protein bindingLIM domain kinase 1Homo sapiens (human)
metal ion bindingLIM domain kinase 1Homo sapiens (human)
protein serine kinase activityLIM domain kinase 1Homo sapiens (human)
protein serine/threonine kinase activityLIM domain kinase 2Homo sapiens (human)
protein bindingLIM domain kinase 2Homo sapiens (human)
ATP bindingLIM domain kinase 2Homo sapiens (human)
metal ion bindingLIM domain kinase 2Homo sapiens (human)
protein serine kinase activityLIM domain kinase 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 (34)

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)
postsynapseLIM domain kinase 1Homo sapiens (human)
glutamatergic synapseLIM domain kinase 1Homo sapiens (human)
male germ cell nucleusLIM domain kinase 1Homo sapiens (human)
cytoplasmLIM domain kinase 1Homo sapiens (human)
cytosolLIM domain kinase 1Homo sapiens (human)
cytoskeletonLIM domain kinase 1Homo sapiens (human)
focal adhesionLIM domain kinase 1Homo sapiens (human)
membraneLIM domain kinase 1Homo sapiens (human)
nuclear speckLIM domain kinase 1Homo sapiens (human)
lamellipodiumLIM domain kinase 1Homo sapiens (human)
neuron projectionLIM domain kinase 1Homo sapiens (human)
nucleusLIM domain kinase 1Homo sapiens (human)
neuron projectionLIM domain kinase 1Homo sapiens (human)
cytoplasmLIM domain kinase 1Homo sapiens (human)
nucleusLIM domain kinase 2Homo sapiens (human)
cytoplasmLIM domain kinase 2Homo sapiens (human)
cis-Golgi networkLIM domain kinase 2Homo sapiens (human)
centrosomeLIM domain kinase 2Homo sapiens (human)
perinuclear region of cytoplasmLIM domain kinase 2Homo sapiens (human)
mitotic spindleLIM domain kinase 2Homo sapiens (human)
nucleusLIM domain kinase 2Homo sapiens (human)
cytoplasmLIM domain kinase 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 (127)

Assay IDTitleYearJournalArticle
AID1856786Downregulation of SEPTS expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856808Downregulation of CEP170 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856796Upregulation of SPDL1 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856771Upregulation of ARHGAP17 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856743Binding affinity to recombinant LIMK2 (330 to 632 residues) (unknown origin) expressed in baculovirus infected insect cells assessed as change in melting temperature at 10 uM by differential scanning fluorimetry2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856752Binding affinity to LIMK2 in human HeLa cells assessed as apparent dissociation constant incubated for 45 mins by kinobead based pulldown assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1857477Aqueous solubility of the compound at pH 72022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
AID1889525Toxicity in human mature brain organoids differentiated from iPSCs assessed as decrease in organoid volume and surface area incubated for 10 days2022Bioorganic & medicinal chemistry letters, 04-01, Volume: 61A dual aurora and lim kinase inhibitor reduces glioblastoma proliferation and invasion.
AID1857484Volume of distribution at steady state in Sprague-Dawley rat at 0.2 mg/kg, iv by LCMS/MS analysis2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
AID1856794Upregulation of CLASP1 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856809Downregulation of RBBP6 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856760Upregulation of CAP2 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856748Inhibition of recombinant LIMK2 (330 to 632 residues) (unknown origin) expressed in baculovirus infected insect cells using CFL1 as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by RapidFir2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1857471Inhibition of recombinant LIMK2 (347 to 659 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 180 mins by RapidFire Mass Spectrometry kinase assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
AID1856815Downregulation of MZT29;MZT2A expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856812Downregulation of MAP18 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856787Downregulation of PARVA expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856747Inhibition of recombinant LIMK1 (330 to 637 residues) (unknown origin) expressed in baculovirus infected insect cells using CFL1 as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by RapidFir2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1857470Inhibition of recombinant LIMK1 (330 to 637 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 105 mins by RapidFire Mass Spectrometry kinase assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
AID1856805Downregulation of NUSAP1 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856746Inhibition of recombinant full length LIMK2 (330 to 632 residues) (unknown origin) expressed in HEK293T cells incubated for 2 hrs in presence of tracer K10 by NanoBRET assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856749Inhibition of LIMK1 in human HeLa cells lysate incubated for 45 mins by kinobead based pulldown assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856770Upregulation of CTTNBP2NL expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1857476Inhibition of LIMK1/LIMK2 in human SH-SY5Y cells assessed as effect on phospho cofilin serine 3 phosphorylation incubated for 2 hr by AlphaLISA SureFire assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
AID1856751Binding affinity to LIMK1 in human HeLa cells assessed as apparent dissociation constant incubated for 45 mins by kinobead based pulldown assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856802Downregulation of LMNA expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856767Upregulation of CACNB2 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856774Downregulation of EPB41L1 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856778Downregulation of BIN1 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856763Upregulation of CAP1 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856758Upregulation of EPB41L1 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856801Downregulation of KLC1 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856807Downregulation of KIF11 expression expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1857473Inhibition of PAK mediated recombinant LIMK2 phosphorylation (347 to 659 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 180 mins by RapidFire Mass Spectrometry kinase assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
AID1856798Upregulation of CLIP2 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856810Downregulation of KIF20A expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856797Upregulation of MPLKIP expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856765Upregulation of CALD1 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856768Upregulation of HNRNPC expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1857487Half life in Sprague-Dawley rat at 0.2 mg/kg, iv by LCMS/MS analysis2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
AID1856766Upregulation of ABLIMI expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856789Upregulation of NPM1 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856773Downregulation of EPB41L2 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856755Inhibition of neurite outgrowth in BMP7 stimulated mouse N1E-115 cells transfected with siFMR1 preincubated for 12 hrs followed by BMP7 stimulation for 24 hrs2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1857479Microsomal stability in human liver microsomes assessed as intrinsic clearance at 4 uM incubated for 30 mins in presence of NADPH by LCMS/MS analysis2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
AID1856759Upregulation of AHNAK expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856820Inhibition of human glutathione S-transferase-tagged LIMK1 (321 to 647 residues) expressed in baculovirus-infected Sf9 cells incubated for 30 mins by radiometric scintillation counting analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856757Upregulation of ANLN expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856785Downregulation of MA18 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856821Inhibition of human glutathione S-transferase-tagged LIMK2 (312 to 638 residues) expressed in baculovirus-infected Sf9 cells incubated for 60 mins by radiometric scintillation counting analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1857472Inhibition of PAK mediated recombinant LIMK1 phosphorylation (330 to 637 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 105 mins by RapidFire Mass Spectrometry kinase assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
AID1856816Downregulation of DPYSL2 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856791Upregulation of CDC20 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856761Upregulation of FLNA expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856756Upregulation of NCOAS expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856762Upregulation of DPYSL3 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856783Downregulation of PPP1R12A expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1857481Clearance in Sprague-Dawley rat at 0.2 mg/kg, iv by LCMS/MS analysis2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
AID1889523Antiproliferative activity against fluorescently labelled human GBM cells are co-cultured with mature brain organoids differentiated from iPSCs assessed as reduction in total number of GBM cells incubated for 10 days by fluorescent confocal microscopy2022Bioorganic & medicinal chemistry letters, 04-01, Volume: 61A dual aurora and lim kinase inhibitor reduces glioblastoma proliferation and invasion.
AID1856782Downregulation of PLEC expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1857474Inhibition of recombinant LIMK1(unknown origin) expressed in HEK293 cells using NanoGlo substrate incubated for 2 hrs followed by substrate addition by NanoBRET assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
AID1856788Downregulation of ANLN expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856742Binding affinity to recombinant LIMK1 (330 to 637 residues) (unknown origin) expressed in baculovirus infected insect cells assessed as change in melting temperature at 10 uM by differential scanning fluorimetry2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856792Upregulation of GTF2F2 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856750Inhibition of LIMK2 in human HeLa cells lysate incubated for 45 mins by kinobead based pulldown assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856793Upregulation of APC expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856779Downregulation of AB12 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1857478Microsomal stability in rat liver microsomes assessed as intrinsic clearance at 4 uM incubated for 30 mins in presence of NADPH by LCMS/MS analysis2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
AID1856800Upregulation of NEFH expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856811Downregulation of CLTC expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856745Inhibition of recombinant full length LIMK1 (330 to 637 residues) (unknown origin) expressed in HEK293T cells incubated for 2 hrs in presence of tracer K10 by NanoBRET assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1857475Inhibition of recombinant LIMK2(unknown origin) expressed in HEK293 cells using NanoGlo substrate incubated for 2 hrs followed by substrate addition by NanoBRET assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
AID1856799Upregulation of PCM1 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856806Downregulation of PCM1 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1857490Brain to plasma ratio in Sprague-Dawley rat at 3 mg/kg, ip by LCMS/MS analysis2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
AID1856804Downregulation of MCM2 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856814Downregulation of DYNC1L12 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856813Downregulation of KRT18 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856781Downregulation of CTTN expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856784Downregulation of CALD expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856777Downregulation of HNRNPU expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856776Downregulation of FMNL1 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856769Upregulation of INF2 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1889524Anti-invasion activity against fluorescently labelled human GBM cells are co-cultured with mature brain organoids differentiated from iPSCs assessed as reduction in number of invading GBM cells incubated for 10 days by fluorescent confocal microscopy2022Bioorganic & medicinal chemistry letters, 04-01, Volume: 61A dual aurora and lim kinase inhibitor reduces glioblastoma proliferation and invasion.
AID1856764Upregulation of ARHGAP21 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1856790Upregulation of BAG3 expression in human HeLa cells assessed as fold increase at 100 uM incubated for 30 mins by phosphoproteomic analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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.
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.
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.
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.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID686947qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Identification of potent Yes1 kinase inhibitors using a library screening approach.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1345768Human LIM domain kinase 1 (LIMK subfamily)2012The Journal of neuroscience : the official journal of the Society for Neuroscience, Apr-11, Volume: 32, Issue:15
The actin-severing protein cofilin is downstream of neuregulin signaling and is essential for Schwann cell myelination.
AID1345768Human LIM domain kinase 1 (LIMK subfamily)2010The Journal of cell biology, Oct-04, Volume: 191, Issue:1
LIM kinases are required for invasive path generation by tumor and tumor-associated stromal cells.
AID1345706Human LIM domain kinase 2 (LIMK subfamily)2008Molecular cancer therapeutics, Nov, Volume: 7, Issue:11
Identification of a nonkinase target mediating cytotoxicity of novel kinase inhibitors.
AID1345706Human LIM domain kinase 2 (LIMK subfamily)2012The Journal of neuroscience : the official journal of the Society for Neuroscience, Apr-11, Volume: 32, Issue:15
The actin-severing protein cofilin is downstream of neuregulin signaling and is essential for Schwann cell myelination.
AID1345768Human LIM domain kinase 1 (LIMK subfamily)2008Molecular cancer therapeutics, Nov, Volume: 7, Issue:11
Identification of a nonkinase target mediating cytotoxicity of novel kinase inhibitors.
AID1345768Human LIM domain kinase 1 (LIMK subfamily)2018British journal of pharmacology, 06, Volume: 175, Issue:11
Inhibition of human prostate smooth muscle contraction by the LIM kinase inhibitors, SR7826 and LIMKi3.
AID1345706Human LIM domain kinase 2 (LIMK subfamily)2018British journal of pharmacology, 06, Volume: 175, Issue:11
Inhibition of human prostate smooth muscle contraction by the LIM kinase inhibitors, SR7826 and LIMKi3.
AID1345706Human LIM domain kinase 2 (LIMK subfamily)2010The Journal of cell biology, Oct-04, Volume: 191, Issue:1
LIM kinases are required for invasive path generation by tumor and tumor-associated stromal cells.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (5.26)29.6817
2010's6 (31.58)24.3611
2020's12 (63.16)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other19 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]