Compound name
AZ191
Protein family
Protein Kinase
Target name
DYRK1B
Affinity biochemical (nM)
17
Affinity on-target cellular (nM)
153
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001032a
SMILES
CN2C=C(C3=CC=NC(NC4=C(OC)C=C(N5CCN(C)CC5)C=C4)=N3)C1=CC=NC=C12
InChIKey
ZYVXTMKTGDARKR-UHFFFAOYSA-N
NCBI gene ID
9149
UniProt ID
Q9Y463
Synonyms
MIRK
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radioactive kinase inhibiton assay (phosphorylation of synthetic peptide substrate Woodtid, [γ -32P]ATP)
Affinity Biochemical Source Knowledge
https://portlandpress.com/biochemj/article-abstract/457/1/43/46825/A-novel-DYRK1B-inhibitor-AZ191-demonstrates-that?redirectedFrom=fulltext
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (in HEK293T cells)
Affinity on-target cellular source knowledge
https://www.sciencedirect.com/science/article/abs/pii/S0960894X22002402?via%3Dihub
Affinity on-target cellular relation
=
Selectivity platform
KINOMEscan (DiscoverX)
Selectivity platform number of targets
402
Selectivity remarks
Screened at 1 µM, S(1) = 0.023, ~100-fold selective over DYRK2 (IC50 = 1890 nM); Screened at 1 µM against 124 kinases, Millipore kinase panel, closest targets as % of inhibition: AURAB (85%), DRAK1 (95%), DYRK2 (85%), FLT1(98%), FLT3(95%), KDR(88%), LOK(87%), MARK1(80%), MINK (87%), MLK1 (95%), MNK2 (90%), https://pubs.acs.org/doi/10.1021/acs.jmedchem.5b00098;
Selectivity Source Knowledge
https://portlandpress.com/biochemj/article-abstract/457/1/43/46825/A-novel-DYRK1B-inhibitor-AZ191-demonstrates-that?redirectedFrom=fulltext
Selectivity Number of Off-targets
7