Compound name
Ulixertinib
Protein family
Protein Kinase
Target name
MAPK1
Affinity biochemical (nM)
0.3
Affinity on-target cellular (nM)
4100
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002341a
SMILES
CC(C)Nc1cc(-c2c[nH]c(C(=O)N[C@H](CO)c3cccc(Cl)c3)c2)c(Cl)cn1
InChIKey
KSERXGMCDHOLSS-LJQANCHMSA-N
NCBI gene ID
5594
UniProt ID
P28482
Synonyms
ERK, ERK2, p41mapk, MAPK2
Mode of action
Reversible covalent inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Rapidfire Mass Spectrometry Inhibition of Catalysis Assay (Km ATP)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/25977981/
Affinity biochemical relation
<
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Immunoblot assay (phosphorylation of ERK using A375 cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/25977981/
Affinity on-target cellular relation
=
Selectivity platform
Proteomics (Kinobeads assay using lysate from K-562, COLO 205, SK-N-BE(2), and MV-4-11 cells)
Selectivity platform number of targets
300
Selectivity remarks
In-vitro potency (competition binding assay) of closest targets in the screen: Kd(MAPK3) = 160 nM, Kd(MAPK1) = 183 nM, Kd(TAO1) = 388 nM, Kd(PRKD2) = 6336 nM, full screening data available in paper https://www.science.org/doi/10.1126/science.aan4368, and Chembl;
Selectivity Source Knowledge
https://www.science.org/doi/10.1126/science.aan4368
Selectivity Number of Off-targets
2