BDBM50094464 CHEMBL3590107::US10525036, Example SCH772984::US10934304, Example SCH772984

SMILES O=C(CN1CC[C@H](C1)C(=O)Nc1ccc2[nH]nc(-c3ccncc3)c2c1)N1CCN(CC1)c1ccc(cc1)-c1ncccn1

InChI Key InChIKey=HDAJDNHIBCDLQF-UHFFFAOYSA-N

Data  25 IC50  3 Kd

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 28 hits for monomerid = 50094464   

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

US Patent
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
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)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 1nMAssay Description:Inhibition of ERK2 (unknown origin) incubated for 45 mins in presence of ATP by IMAP assayMore 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
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 4nMAssay Description:Inhibition of ERK1 (unknown origin) incubated for 45 mins in presence of ATP by IMAP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
TargetMitogen-activated protein kinase 6(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataKd:  1.43E+4nMAssay Description:Binding affinity to recombinant wild-type ERK3 (9 to 327 residues) (unknown origin) expressed in Escherichia coli by microscale thermophoresis assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetMitogen-activated protein kinase 1(Human)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
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

LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 9nMAssay Description:Inhibition of MEK in human A375 cells assessed as inhibition of ERK phosphorylationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetMitogen-activated protein kinase 1(Human)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human ERK2 preincubated for 15 mins followed by addition of IMAP peptide substrate and ATP measured after 60 mins by IMAP-FP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 9nMAssay Description:Inhibition of MEK in human A375 cells assessed as inhibition of ERK phosphorylationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetMitogen-activated protein kinase 1(Human)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human ERK2 preincubated for 15 mins followed by addition of IMAP peptide substrate and ATP measured after 60 mins by IMAP-FP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
TargetMitogen-activated protein kinase 1(Human)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataKd:  0.0501nMAssay 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 1/3(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 12nMAssay 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)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataKd:  0.100nMAssay 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
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 2.5nMAssay 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)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
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)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 4nMAssay 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)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 1nMAssay Description:Inhibition of ERK2 (unknown origin) preincubated for 45 mins followed by substrate addition measured after 0.5 hrs by IMAP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetMitogen-activated protein kinase 1(Human)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 1nMAssay Description:Inhibition of ERK2 (unknown origin) using peptide substrate measured after 45 mins by IMAP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 5.70E+6nMAssay Description:Inhibition of CYP3A4 (unknown origin) preincubated followed by substrate additionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetMitogen-activated protein kinase 3(Human)
Recurium Ip Holdings

US Patent
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 8nMAssay Description:Inhibition of ERK1 (unknown origin) using peptide substrate measured after 45 mins by IMAP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Merck

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 7.80E+6nMAssay Description:Inhibition of CYP3A4 (unknown origin) co-incubated with substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetMitogen-activated protein kinase 1(Human)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 20nMAssay 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
TargetMitogen-activated protein kinase 1(Human)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 4nMAssay 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
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
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 3(Human)
Recurium Ip Holdings

US Patent
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 4nMAssay Description:Inhibition of ERK1 (unknown origin) after 45 mins by IMAP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/2/2016
Entry Details Article
PubMed
TargetMitogen-activated protein kinase 1(Human)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
Affinity DataIC50: 1nMAssay Description:Inhibition of ERK2 (unknown origin) after 45 mins by IMAP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/2/2016
Entry Details Article
PubMed
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
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)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
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)
Southwest Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50094464(CHEMBL3590107 | US10525036, Example SCH772984 | US...)
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