Compound name
AZ191
Protein family
Protein Kinase
Target name
DYRK1A
Affinity biochemical (nM)
88
Affinity on-target cellular (nM)
81
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
1859
UniProt ID
Q13627
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