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 %