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TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

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 Depth
Date in BDB:
9/22/2017
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

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 Depth
Date in BDB:
9/22/2017
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

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 Depth
Date in BDB:
9/22/2017
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50420692(CHEMBL2087076)
Affinity DataEC50:  0.200nMAssay Description:Inhibition of MEK1-mediated ERK1 phosphorylation in human HCT116 cells after 2 hrs by immunoblotting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50338038(US8575391, 334 | 3,4-difluoro-2-[(2-fluoro-4-iodop...)
Affinity DataKd:  0.240nMAssay Description:Binding affinity to MEK1 by surface plasmon resonance in presence of ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/24/2011
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50420692(CHEMBL2087076)
Affinity DataEC50:  0.400nMAssay Description:Inhibition of MEK1-mediated ERK1 phosphorylation in human A375 cells after 2 hrs by immunoblotting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50420696(CHEMBL2087080)
Affinity DataEC50:  0.400nMAssay Description:Inhibition of MEK1-mediated ERK1 phosphorylation in human HCT116 cells after 2 hrs by immunoblotting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM104963(CHEMBL507361 | US8575391, Q | US11147816, PD032590...)
Affinity DataKd:  0.400nMAssay Description:Binding affinity to MEK1 by surface plasmon resonance in presence of ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/24/2011
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

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 Depth
Date in BDB:
9/22/2017
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM104963(CHEMBL507361 | US8575391, Q | US11147816, PD032590...)
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
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50420701(CHEMBL2087461)
Affinity DataEC50:  0.600nMAssay Description:Inhibition of MEK1-mediated ERK1 phosphorylation in human HCT116 cells after 2 hrs by immunoblotting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50623718(CHEMBL5433950)
Affinity DataIC50: 0.700nMAssay Description:Inhibition of MEK1 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

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
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50391802(CHEMBL2146883 | cobimetinib | (3,4-difluoro-2-(2-f...)
Affinity DataIC50: 0.900nMAssay Description:Inhibition of MEK1 (unknown origin) by biochemical assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details PDB3D3D Structure (crystal)
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50391802(CHEMBL2146883 | cobimetinib | (3,4-difluoro-2-(2-f...)
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
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50420701(CHEMBL2087461)
Affinity DataEC50:  0.900nMAssay Description:Inhibition of MEK1-mediated ERK1 phosphorylation in human A375 cells after 2 hrs by immunoblotting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50420702(CHEMBL2087462)
Affinity DataEC50:  0.900nMAssay Description:Inhibition of MEK1-mediated ERK1 phosphorylation in human HCT116 cells after 2 hrs by immunoblotting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

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
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

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
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 0.930nMAssay Description:Inhibition of MEK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM200424(US9227969, 51 | US9629836, 51 | US10011599, Exampl...)
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
In Depth
Date in BDB:
5/20/2019
Entry Details
US Patent

TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM4552(CHEMBL288441 | SKI-606 | 4-[(2,4-Dichloro-5-methox...)
Affinity DataIC50: 1nMAssay Description:Inhibition of human MEK1 after 40 mins in presence of MgATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/4/2017
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM614412(US20230270730, Compound N-1 | US11964950, Compound...)
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
In Depth
Date in BDB:
10/15/2023
Entry Details
US Patent

TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM200424(US9227969, 51 | US9629836, 51 | US10011599, Exampl...)
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
In Depth
Date in BDB:
5/26/2020
Entry Details
US Patent

TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50375656(ARCTIGENIN)
Affinity DataIC50: 1nMAssay Description:Inhibition of MKK1More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMed
LigandPNGBDBM200424(US9227969, 51 | US9629836, 51 | US10011599, Exampl...)
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
In Depth
Date in BDB:
11/14/2016
Entry Details
US Patent

TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM614413(US20230270730, Compound N-2 | US11964950, Compound...)
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
In Depth
Date in BDB:
10/15/2023
Entry Details
US Patent

TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM104963(CHEMBL507361 | US8575391, Q | US11147816, PD032590...)
Affinity DataIC50: 1nMAssay Description:Inhibition of MEK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM350231(US20230270730, Compound A-13 | US11964950, Compoun...)
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
In Depth
Date in BDB:
10/15/2023
Entry Details
US Patent

TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50132262(4-[3-Chloro-4-(1,5-dimethyl-1H-imidazol-2-ylsulfan...)
Affinity DataIC50: 1nMAssay Description:Inhibitory concentration against Mitogen activated protein kinase kinase kinase 1 was determined using Raf/MEK1 coupled assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
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
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50420702(CHEMBL2087462)
Affinity DataEC50:  1.10nMAssay Description:Inhibition of MEK1-mediated ERK1 phosphorylation in human A375 cells after 2 hrs by immunoblotting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM28124(6-methoxy-7-[3-(morpholin-4-yl)propoxy]-4-{[4-(phe...)
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 Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandPNGBDBM50222709(CHEMBL244488 | 3,4-difluoro-2-(2-fluoro-4-iodophen...)
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 Depth
Date in BDB:
8/24/2020
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50420698(CHEMBL2087082)
Affinity DataEC50:  1.30nMAssay Description:Inhibition of MEK1-mediated ERK1 phosphorylation in human HCT116 cells after 2 hrs by immunoblotting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM130909(US8822500, Stauro- sporine | US9920060, Staurospor...)
Affinity DataIC50: 1.30nMAssay Description:Inhibition of human MEK1 using ERK2 (K52R) as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

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
In Depth
Date in BDB:
3/12/2022
Entry Details
US Patent
PDB3D3D Structure (crystal)
LigandPNGBDBM520651(US11147816, PD318088 | US11701360, PD318088)
Affinity DataIC50: 1.40nMAssay Description:TBDMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2023
Entry Details
US Patent
PDB3D3D Structure (crystal)
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM200427(US9227969, 54 | US9629836, 54 | US10011599, Exampl...)
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
In Depth
Date in BDB:
5/26/2020
Entry Details
US Patent

LigandPNGBDBM200427(US9227969, 54 | US9629836, 54 | US10011599, Exampl...)
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
In Depth
Date in BDB:
11/14/2016
Entry Details
US Patent

LigandPNGBDBM200427(US9227969, 54 | US9629836, 54 | US10011599, Exampl...)
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
In Depth
Date in BDB:
5/20/2019
Entry Details
US Patent

TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50420697(CHEMBL2087081)
Affinity DataEC50:  1.5nMAssay Description:Inhibition of MEK1-mediated ERK1 phosphorylation in human A375 cells after 2 hrs by immunoblotting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50420697(CHEMBL2087081)
Affinity DataEC50:  1.5nMAssay Description:Inhibition of MEK1-mediated ERK1 phosphorylation in human HCT116 cells after 2 hrs by immunoblotting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50014413(CHEMBL3261161)
Affinity DataIC50: 1.60nMAssay Description:Inhibition of MEK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM200420(US9227969, 47 | US9629836, 47 | US10011599, Exampl...)
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
In Depth
Date in BDB:
5/26/2020
Entry Details
US Patent

LigandPNGBDBM200420(US9227969, 47 | US9629836, 47 | US10011599, Exampl...)
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
In Depth
Date in BDB:
11/14/2016
Entry Details
US Patent

LigandPNGBDBM200420(US9227969, 47 | US9629836, 47 | US10011599, Exampl...)
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
In Depth
Date in BDB:
5/20/2019
Entry Details
US Patent

TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

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 Depth
Date in BDB:
5/26/2017
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

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 Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetDual specificity mitogen-activated protein kinase kinase 1(Human)
The University of Michigan Medical School

Curated by ChEMBL
LigandPNGBDBM50337926(3-[(2R)-2,3-dihydroxypropyl]-6-fluoro-5-[(2-fluoro...)
Affinity DataIC50: 1.80nMAssay Description:Inhibition of MEK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMed
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