Compound name
MU1210
Protein family
Protein Kinase
Target name
DYRK1B
Affinity biochemical (nM)
956
Affinity on-target cellular (nM)
10000
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000008b
SMILES
CN1C=C(C2=NC3=C(OC=C3C4=CC(C5=CC=NC=C5)=CC=C4)C=C2)C=N1
InChIKey
HEAGNKNMQVIVMM-UHFFFAOYSA-N
NCBI gene ID
8445
UniProt ID
Q92630
Mode of action
Inhibitor
Negative control
MU140
Affinity biochemical definition
IC50
Affinity biochemical assay type
Eurofins radiometric assay
Affinity Biochemical Source Knowledge
https://onlinelibrary.wiley.com/doi/10.1002/anie.201810312
Affinity biochemical relation
=
Affinity on-target cellular definition
Ki
Affinity on-target cellular assay type
NanoBRET assay (in HEK293T cells)
Affinity on-target cellular source knowledge
https://www.thesgc.org/chemical-probes/MU1210
Affinity on-target cellular relation
=
Selectivity platform
Eurofins kinase panel
Selectivity platform number of targets
210
Selectivity remarks
Screened at 1 µM, closest targets as % of activity: HIPK2 (99%), HIPK3 (94%), GSK3A (90%); Eurofins binding assay: IC50(HIPK1) = 187 nM, IC50(HIPK2) = 23 nM, IC50(CLK3) >3 µM; In-cellular potency (NanoBRET assay in HEK293T cells): Ki(HIPK2) >10 µM, Ki(HIPK4) = 5.41 µM
Selectivity Source Knowledge
https://onlinelibrary.wiley.com/doi/10.1002/anie.201810312