BDBM50094465 CHEMBL3590106::US10525036, Example BVD-523::US10934304, Example BVD-523

SMILES CC(C)Nc1cc(-c2c[nH]c(c2)C(=O)N[C@H](CO)c2cccc(Cl)c2)c(Cl)cn1

InChI Key InChIKey=KSERXGMCDHOLSS-UHFFFAOYSA-N

Data  2 KI  15 IC50  2 Kd

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 19 hits for monomerid = 50094465   

TargetMitogen-activated protein kinase 1(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of MEK U911-activated ERK2 (unknown origin) using Erktide as substrate preincubated with enzyme for 20 mins prior to substrate addition by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/15/2016
Entry Details Article
PubMed
TargetMitogen-activated protein kinase 1(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
Affinity DataIC50: 11nMAssay Description:Inhibition of ERK2 (unknown origin) measured after 2 hr by ADP-glo assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetMitogen-activated protein kinase 1(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
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
Go to US Patent

TargetMitogen-activated protein kinase 1/3(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
Affinity DataIC50: 3.10E+3nMAssay 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
PubMed
TargetMitogen-activated protein kinase 1(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
Affinity DataKd:  10nMAssay 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
PubMed
TargetMitogen-activated protein kinase 1(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
Affinity DataKd:  0.316nMAssay 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
PubMed
TargetMitogen-activated protein kinase 1/3(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
Affinity DataIC50: 150nMAssay 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
PubMed
TargetMitogen-activated protein kinase 1(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
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
Go to US Patent

TargetMitogen-activated protein kinase 3(Human)
Recurium Ip Holdings

US Patent
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
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
Go to US Patent

TargetMitogen-activated protein kinase 1(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
Affinity DataIC50: 4.10E+3nMAssay 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
PubMed
TargetMitogen-activated protein kinase 1(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
Affinity DataIC50: 31nMAssay 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
PubMed
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of MEK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/13/2020
Entry Details Article
PubMed
TargetMitogen-activated protein kinase 1(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of ERK2 (unknown origin) in the presence of 1 mM ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/13/2020
Entry Details Article
PubMed
TargetMitogen-activated protein kinase 1(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
Affinity DataIC50: 0.0300nMAssay Description:Inhibition of ERK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2016
Entry Details Article
PubMed
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of MEK1 (unknown origin) autophosphorylation incubated with enzyme for 20 mins prior to ATP addition by ADP Glo kinase assay in presence o...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/15/2016
Entry Details Article
PubMed
TargetMitogen-activated protein kinase 1(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of MEK U911-activated ERK2 (unknown origin) using Erktide as substrate preincubated with enzyme for 20 mins prior to substrate addition by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/15/2016
Entry Details Article
PubMed
TargetMitogen-activated protein kinase 1(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
Affinity DataIC50: 4.10E+3nMAssay Description:Inhibition of ERK2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-ERK2 level after 2 hrs by Cellomics ArrayScanTM V...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/15/2016
Entry Details Article
PubMed
TargetMitogen-activated protein kinase 1(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
Affinity DataKi:  0.0400nMAssay Description:Binding affinity to ERK2 (unknown origin) measured after 20 mins in presence of [gamma33P]ATP by scintillation counter analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
TargetMitogen-activated protein kinase 3(Human)
Recurium Ip Holdings

US Patent
LigandPNGBDBM50094465(CHEMBL3590106 | US10525036, Example BVD-523 | US10...)
Affinity DataKi: <0.300nMAssay Description:Binding affinity to ERK1 (unknown origin) measured after 20 mins in presence of [gamma33P]ATP by scintillation counter analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed