ATP-competitive inhibitor of MAPK14
In Vitro Validations
Uniprot ID: Q16539
Target Class: Protein kinase
Target SubClass: CMGC
Potency Value: 2.8 nM
Potency Assay: KD was determined in a kinase binding assay. The IC50 (0.009 uM) was determined using a spectrophotometric coupled-enzyme assay.
PDB ID for probe-target interaction (3D structure): 3FC1
Mitogen-activated protein kinase 14, SAPK2A, MXI2, ...
In Cell Validations
In Vivo Data
Off-Target Selectivity Assesments
Potency end-point : KD MAPK11 74 nM
Potency assay (off target): VX-745 was 20-fold selective for MAPK14 (p38alpha) > MAPK11 (p38beta) in IC50 assays. VX-745 was tested for kinase binding activity in a panel of 317 kinases showing <10 uM activity against 11 kinases (ABL1, BLK,CSF1R, DDR1, FGR, FYN, LCK, LYN, PDGFRB, SRC, YES).
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