Compile Data Set for Download or QSAR
Report error Found 17 Enz. Inhib. hit(s) for PDB: 5K4I
TargetMitogen-activated protein kinase 1(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataKd:  1.60nMAssay Description:Binding affinity to MEK-activated phosphorylated biotinylated ERK2 (unknown origin) by SPR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase 1(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataKd:  1.60nMAssay Description:Binding affinity to non-phosphorylated biotinylated ERK2 (unknown origin) by SPR analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase 1(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of ERK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/2/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase 3(Human)
Ontario Institute For Cancer Research

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of ERK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/2/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase 1(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataIC50: 3.10nMAssay Description:Inhibition of ERK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase 1(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataIC50: 3.10nMAssay Description:Inhibition of ERK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase 1(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataIC50: 3.30nMpH: 7.3Assay Description:Compounds were tested in an enzymatic assay using human ERK-2 (Mitogen Activated Kinase 1), recombinantly expressed as an n-terminal 6-His fusion pro...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/28/2016
Entry Details
US Patent
PDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase 1(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataIC50: 3.30nMpH: 7.3Assay Description:Compounds were tested in an enzymatic assay using human ERK-2 (Mitogen Activated Kinase 1), recombinantly expressed as an n-terminal 6-His fusion pro...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/6/2014
Entry Details
US Patent
PDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase 3(Human)
Ontario Institute For Cancer Research

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataIC50: 6.10nMAssay Description:Inhibition of ERK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase 3(Human)
Ontario Institute For Cancer Research

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataIC50: 6.10nMAssay Description:Inhibition of ERK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase 1/3(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataIC50: 31nMAssay Description:Inhibition of ERK1/2 in human A375 cells assessed as inhibition of ERK phosphorylation after 2 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase 1(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataIC50: 50nMAssay Description:Activated ERK1 and ERK2 activity was determined in a Mobility Shift Assay (MSA) format as follows: Compound and kinase solution were prepared with as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/12/2021
Entry Details
US Patent
PDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase 1(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataIC50: 50nMAssay Description:Activated ERK1 and ERK2 activity was determined in a Mobility Shift Assay (MSA) format as follows: Compound and kinase solution were prepared with as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2020
Entry Details
US Patent
PDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase 3(Human)
Ontario Institute For Cancer Research

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataIC50: 50nMAssay Description:Activated ERK1 and ERK2 activity was determined in a Mobility Shift Assay (MSA) format as follows: Compound and kinase solution were prepared with as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/25/2020
Entry Details
US Patent
PDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase 1/3(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataIC50: 86nMAssay Description:Inhibition of ERK1/2 in human A375 cells assessed as inhibition of RSK phosphorylation after 2 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase 1(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataIC50: 86nMAssay Description:Inhibition of ERK2 in human A375 cells harboring BRAF V600E mutant assessed as decrease in phosphorylated ERK2 levelsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/13/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetMitogen-activated protein kinase 1(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM120095(US8697715, 39 | US9259470, 39 | US10525036, Exampl...)
Affinity DataIC50: 140nMAssay Description:Inhibition of ERK2 in human A375 cells harboring BRAF V600E mutant assessed as decrease in phosphorylated RSK levelsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/13/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)