Compound name
Lorecivivint
Protein family
Protein Kinase
Target name
HIPK2
Affinity biochemical (nM)
16.8
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001024a
SMILES
CC(C)CC(=O)Nc1cncc(-c2ccc3[nH]nc(-c4nc5cncc(-c6cccc(F)c6)c5[nH]4)c3c2)c1
InChIKey
AQDWDWAYVBQMAM-UHFFFAOYSA-N
NCBI gene ID
28996
UniProt ID
Q9H2X6
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic inhibition assay (Thermo Fisher)
Affinity Biochemical Source Knowledge
https://www.sciencedirect.com/science/article/pii/S106345841930994X?via%3Dihub
Affinity biochemical relation
=
Selectivity platform
Thermo Fisher Invitrogen Z-lyte and Lantha based platform
Selectivity platform number of targets
318
Selectivity remarks
Screened at 500 nM, >90% inhibiton; in-vitro potency (Enzymatic inhibition assay, Thermo Fisher) of closest target: IC50(CLK1) = 239 nM, IC50(HIPK3) = 126 nM, https://www.sciencedirect.com/science/article/pii/S106345841930994X?via%3Dihub;
Selectivity Source Knowledge
https://www.sciencedirect.com/science/article/pii/S106345841930994X?via%3Dihub
Selectivity Number of Off-targets
2