243494
4
ChEMBL
CHEMBL830593
Percent inhibition against AMPK at 10 uM using 100 uM ATP
Title: (1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors.
Abstract: The novel imidazo[4,5-c]pyridine 1,2,5-oxadiazol-3-yl template affords an excellent start point for identification of inhibitors of a number of protein kinases. Here we report on its optimisation for mitogen and stress-activated protein kinase-1 (MSK-1) inhibitory activity, and selectivity over other kinases.
Journal: Bioorg Med Chem Lett
Year: 2005
Volume: 15
Issue: 14
First Page: 3407
Last Page: 3411
DOI: 10.1016/j.bmcl.2005.05.020
Target ChEMBL ID: CHEMBL4045
ChEMBL Target Name: AMP-activated protein kinase, alpha-1 subunit
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: D - Direct protein target assigned
Confidence: Direct single protein target assigned
9606
Homo sapiens
15955699
1
https://www.ebi.ac.uk/chembl/
https://www.ebi.ac.uk/chembl/assay_report_card/CHEMBL830593
1
Standard Type
Standardized activity type (e.g. IC50 rather than Ic-50/Ic50/ic50/ic-50)
4
2
Standard Relation
Qualifier (e.g. >, <, =) for 'Standard Value'
4
3
Standard Value
Standardized activity value transformed to common units: e.g. mM concentrations converted to nM
1
4
Standard Units
Selected units for 'Standard Type': e.g. concentrations are in nM
4
1
5'-AMP-activated protein kinase catalytic subunit alpha-1
Q13131
AMP-activated protein kinase, alpha-1 subunit
7
PMID: 15955699
103456750
4
1
Inhibition
2
=
3
59
4
%