Compound name
SR-302
Protein family
Protein Kinase
Target name
MAPK14
Affinity biochemical (nM)
6.2
Affinity on-target cellular (nM)
125
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000712a
SMILES
CS(N1CCCC(NC([C@@H](NC(C2=CC=C(C=C2)CNC(C3=CN=C4C=CC=CN34)=O)=O)CCC5CCCCC5)=O)C1)(=O)=O
InChIKey
WGMNFJAFXXXRLZ-GEVKEYJPSA-N
NCBI gene ID
1432
UniProt ID
Q16539
Synonyms
PRKM14, p38, Mxi2, PRKM15
Mode of action
Inhibitor
Negative control
SR301
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzyme kinetic assay (Reaction Biology)
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/acs.jmedchem.1c00868
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/SR-302
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (HEK293T cells)
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
468
Selectivity remarks
Screened at 1 µM, closest targets as % of contr.: ABL1-nonphosphorylated (14%), RIPK2 (30%), RPS6KA5RPS6KA5(Kin.Dom.2-C-terminal) (35%), CHEK2 (37%), PIK3CA (37%), STK38L (40%); Follow-up IC50s in cellular NanoBRET assays: all targets IC50 >25 µM (>125-fold selective);
Selectivity Source Knowledge
https://doi.org/10.1021/acs.jmedchem.1c00868
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/SR-302
Selectivity Number of Off-targets
0