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Found 1940 Enz. Inhib. hit(s) with Target = 'Dual specificity mitogen-activated protein kinase kinase 1'
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50341519((S)-3-(4-(2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl...)
Affinity DataKi: >1.00E+3nMAssay Description:Inhibition of MEK1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50463479(CHEMBL4249925)
Affinity DataKi: >1.00E+3nMAssay Description:Inhibition of MEK1 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50463484(CHEMBL4248525)
Affinity DataKi: >1.00E+4nMAssay Description:Inhibition of MEK1 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50180838(CHEMBL3818606)
Affinity DataIC50:  0.00715nMAssay Description:Inhibition of purified MEK1 (unknown origin) assessed as reduction in phosphorylation of inactive Erk2 incubated for 30 mins by Kinase-Glo luminescen...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50180834(CHEMBL3819302)
Affinity DataIC50:  0.0150nMAssay Description:Inhibition of purified MEK1 (unknown origin) assessed as reduction in phosphorylation of inactive Erk2 incubated for 30 mins by Kinase-Glo luminescen...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50180836(CHEMBL3818677)
Affinity DataIC50:  0.0190nMAssay Description:Inhibition of purified MEK1 (unknown origin) assessed as reduction in phosphorylation of inactive Erk2 incubated for 30 mins by Kinase-Glo luminescen...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Mus musculus)
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM104963(CHEMBL507361 | US11147816, PD0325901 | US11701360,...)
Affinity DataIC50:  0.330nMAssay Description:Inhibition of MEK1 in mouse colon 26 cells assessed as reduction in ERK1/2 phosphorylation after 1 hr by Western blot analysisMore data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50180837(CHEMBL3819622)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of purified MEK1 (unknown origin) assessed as reduction in phosphorylation of inactive Erk2 incubated for 30 mins by Kinase-Glo luminescen...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM104963(CHEMBL507361 | US11147816, PD0325901 | US11701360,...)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of MEK1-mediated ERK2 T202/Y204 phosphorylation using biotinylated MBP as substrate preincubated for 30 mins measured after 100 mins by cR...More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50531540(CHEBI:75998 | GSK-1120212 | GSK1120212 | JTP 74057...)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of MEK1 (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50391802((3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl...)
Affinity DataIC50:  0.900nMAssay Description:Inhibition of MEK1-mediated ERK2 T202/Y204 phosphorylation using biotinylated MBP as substrate preincubated for 30 mins measured after 100 mins by cR...More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50531540(CHEBI:75998 | GSK-1120212 | GSK1120212 | JTP 74057...)
Affinity DataIC50:  0.920nMAssay Description:Non competitive inhibition of MEK1 (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50531540(CHEBI:75998 | GSK-1120212 | GSK1120212 | JTP 74057...)
Affinity DataIC50:  0.920nMAssay Description:Inhibition of MEK1 (unknown origin)More data for this Ligand-Target Pair
LigandPNGBDBM200424(US10011599, Example 51 | US9227969, 51 | US9629836...)
Affinity DataIC50:  1nMpH: 7.5Assay Description:A BRAF-MEK-ERK cascade assay is used to evaluate the effects of these compounds as inhibitors of the MAP kinase pathway. An enzymatic cascade assay i...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM50531540(CHEBI:75998 | GSK-1120212 | GSK1120212 | JTP 74057...)
Affinity DataIC50: <1nMAssay Description:Inhibition of MEK in human KYSE-520 cells assessed as reduction in p-ERK levelsMore data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM350231(US20230270730, Compound A-13)
Affinity DataIC50:  1nMAssay Description:The test compound, CRAF (Thermo Fisher Scientific Inc.), MEK1 (Thermo Fisher Scientific Inc.) and ERK2 (Carna Biosciences, Inc.) were mixed in ATP-co...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetDual specificity mitogen-activated protein kinase kinase 1 [K97R](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM200424(US10011599, Example 51 | US9227969, 51 | US9629836...)
Affinity DataIC50:  1nMAssay Description:The radioactive filter binding assay is standardized using recombinant human activated BRAF (V599E) kinase (Cat No. 14-557) and kinase dead MEK1 (K97...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM200424(US10011599, Example 51 | US9227969, 51 | US9629836...)
Affinity DataIC50:  1nMAssay Description:[MEK1 1mM ATP IC50 uM] A BRAF-MEK-ERK cascade assay is used to evaluate the effects of these compounds as inhibitors of the MAP kinase pathway. An en...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM614413(US20230270730, Compound N-2)
Affinity DataIC50:  1nMAssay Description:The test compound, CRAF (Thermo Fisher Scientific Inc.), MEK1 (Thermo Fisher Scientific Inc.) and ERK2 (Carna Biosciences, Inc.) were mixed in ATP-co...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM614412(US20230270730, Compound N-1)
Affinity DataIC50:  1nMAssay Description:The test compound, CRAF (Thermo Fisher Scientific Inc.), MEK1 (Thermo Fisher Scientific Inc.) and ERK2 (Carna Biosciences, Inc.) were mixed in ATP-co...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50375656(ARCTIGENIN)
Affinity DataIC50:  1nMAssay Description:Inhibition of MKK1Checked by AuthorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM4552(4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human MEK1 after 40 mins in presence of MgATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50132262(4-[3-Chloro-4-(1,5-dimethyl-1H-imidazol-2-ylsulfan...)
Affinity DataIC50:  1nMAssay Description:Inhibitory concentration of the compound against Mitogen activated protein kinase kinase kinase 1 was determined using Raf/MEK1 coupled assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM28124(3-cyanoquinoline, 9 | 6-methoxy-7-[3-(morpholin-4-...)
Affinity DataIC50:  1.10nMAssay Description:Inhibitory activity against Dual specificity mitogen-activated protein kinase kinase using coupled MEK assay (which uses activated Raf to activate an...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50222709(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-N-(2-h...)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of MEK assessed as inhibition of ERK phosphorylation by Raf-MEK-ERK cascade assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM520651(US11147816, PD318088 | US11701360, PD318088)
Affinity DataIC50:  1.40nMAssay Description:TBDMore data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM520651(US11147816, PD318088 | US11701360, PD318088)
Affinity DataIC50:  1.40nMAssay Description:The IC50 for MEK1 and 2 can be measured by methods in references such as [Yamaguchi et al. (2011) International Journal of Oncology 39:23-31].More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1 [K97R](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM200427(US10011599, Example 54 | US9227969, 54 | US9629836...)
Affinity DataIC50:  1.5nMAssay Description:The radioactive filter binding assay is standardized using recombinant human activated BRAF (V599E) kinase (Cat No. 14-557) and kinase dead MEK1 (K97...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM200427(US10011599, Example 54 | US9227969, 54 | US9629836...)
Affinity DataIC50:  1.5nMAssay Description:[MEK1 1mM ATP IC50 uM] A BRAF-MEK-ERK cascade assay is used to evaluate the effects of these compounds as inhibitors of the MAP kinase pathway. An en...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM200427(US10011599, Example 54 | US9227969, 54 | US9629836...)
Affinity DataIC50:  1.5nMpH: 7.5Assay Description:A BRAF-MEK-ERK cascade assay is used to evaluate the effects of these compounds as inhibitors of the MAP kinase pathway. An enzymatic cascade assay i...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50014413(CHEMBL3261161)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of MEK1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM200420(US10011599, Example 47 | US9227969, 47 | US9629836...)
Affinity DataIC50:  1.70nMpH: 7.5Assay Description:A BRAF-MEK-ERK cascade assay is used to evaluate the effects of these compounds as inhibitors of the MAP kinase pathway. An enzymatic cascade assay i...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM200420(US10011599, Example 47 | US9227969, 47 | US9629836...)
Affinity DataIC50:  1.70nMAssay Description:[MEK1 1mM ATP IC50 uM] A BRAF-MEK-ERK cascade assay is used to evaluate the effects of these compounds as inhibitors of the MAP kinase pathway. An en...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetDual specificity mitogen-activated protein kinase kinase 1 [K97R](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM200420(US10011599, Example 47 | US9227969, 47 | US9629836...)
Affinity DataIC50:  1.70nMAssay Description:The radioactive filter binding assay is standardized using recombinant human activated BRAF (V599E) kinase (Cat No. 14-557) and kinase dead MEK1 (K97...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50134989(CHEMBL3746640)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of MEK1 in human HeLa-MaTu matched pair cells assessed as reduction in ERK phosphorylationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50014412(Pimasertib | US11147816, Pimasertib (AS703026) | U...)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of MEK1 in human COLO205 cellsMore data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50391804(CHEMBL2146893)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of MEK1-mediated ERK2 T202/Y204 phosphorylation using biotinylated MBP as substrate preincubated for 30 mins measured after 100 mins by cR...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50337926((R)-3-(2,3-dihydroxypropyl)-6-fluoro-5-(2-fluoro-4...)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of MEK1 (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM614292(US20230270730, Compound A-44)
Affinity DataIC50:  2nMAssay Description:The test compound, CRAF (Thermo Fisher Scientific Inc.), MEK1 (Thermo Fisher Scientific Inc.) and ERK2 (Carna Biosciences, Inc.) were mixed in ATP-co...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM614293(US20230270730, Compound A-45)
Affinity DataIC50:  2nMAssay Description:The test compound, CRAF (Thermo Fisher Scientific Inc.), MEK1 (Thermo Fisher Scientific Inc.) and ERK2 (Carna Biosciences, Inc.) were mixed in ATP-co...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM50531540(CHEBI:75998 | GSK-1120212 | GSK1120212 | JTP 74057...)
Affinity DataIC50:  2nMAssay Description:Inhibition of MEK 1/2 (unknown origin)More data for this Ligand-Target Pair
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM350232(US20230270730, Compound A-14)
Affinity DataIC50:  2nMAssay Description:The test compound, CRAF (Thermo Fisher Scientific Inc.), MEK1 (Thermo Fisher Scientific Inc.) and ERK2 (Carna Biosciences, Inc.) were mixed in ATP-co...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetDual specificity mitogen-activated protein kinase kinase 1 [K97R](Homo sapiens (Human))
Novartis

US Patent
LigandPNGBDBM200417(US9227969, 44 | US9629836, 44)
Affinity DataIC50:  2nMAssay Description:The radioactive filter binding assay is standardized using recombinant human activated BRAF (V599E) kinase (Cat No. 14-557) and kinase dead MEK1 (K97...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50132264(4-[3-Chloro-4-(1,4,5-trimethyl-1H-imidazol-2-ylsul...)
Affinity DataIC50:  2nMAssay Description:Inhibitory concentration of the compound against Mitogen activated protein kinase kinase kinase 1 was determined using Raf/MEK1 coupled assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50132266(4-[3-Bromo-4-(1-methyl-1H-imidazol-2-ylsulfanyl)-p...)
Affinity DataIC50:  2nMAssay Description:Inhibitory concentration of the compound against Mitogen activated protein kinase kinase kinase 1 was determined using Raf/MEK1 coupled assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM28123(3-cyanoquinoline, 8 | 4-({3-chloro-4-[(1-methyl-1H...)
Affinity DataIC50:  2nMAssay Description:Inhibitory concentration of the compound against Mitogen activated protein kinase kinase kinase 1 was determined using Raf/MEK1 coupled assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50132261(4-[3-Chloro-4-(1-methyl-1H-imidazol-2-ylsulfanyl)-...)
Affinity DataIC50:  2nMAssay Description:Inhibitory concentration of the compound against Mitogen activated protein kinase kinase kinase 1 was determined using Raf/MEK1 coupled assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50014413(CHEMBL3261161)
Affinity DataIC50:  2nMAssay Description:Inhibition of MEK1 in human COLO205 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50132260(2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmetho...)
Affinity DataIC50:  2nMAssay Description:Inhibitory concentration of the compound against Mitogen activated protein kinase kinase kinase 1 was determined using Raf/MEK1 coupled assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Homo sapiens (Human))
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM402212(1-(4-(8-(2-chloro-4-((6-(hydroxymethyl)pyridin-2- ...)
Affinity DataIC50:  2nMAssay Description:[MEK1 1mM ATP IC50 uM] A BRAF-MEK-ERK cascade assay is used to evaluate the effects of these compounds as inhibitors of the MAP kinase pathway. An en...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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