Compound name
AZD1208
Protein family
Protein Kinase
Target name
PIM1
Affinity biochemical (nM)
0.4
Affinity on-target cellular (nM)
10
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001547a
SMILES
N[C@@H]1CCCN(c2c(/C=C3\SC(=O)NC3=O)cccc2-c2ccccc2)C1
InChIKey
MCUJKPPARUPFJM-MRXNPFEDSA-N
NCBI gene ID
5292
UniProt ID
P11309
Mode of action
inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Mobility shift assay (Caliper Life Sciences, conc. ATP = Km)
Affinity Biochemical Source Knowledge
https://ashpublications.org/blood/article/123/6/905/32601/AZD1208-a-potent-and-selective-pan-Pim-kinase
https://ashpublications.org/blood/article/123/6/905/32601/AZD1208-a-potent-and-selective-pan-Pim-kinase
https://ashpublications.org/blood/article/123/6/905/32601/AZD1208-a-potent-and-selective-pan-Pim-kinase
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Enzyme-linked immunosorbent assay (phosphorylation of BAD in U2OS cells)
Affinity on-target cellular source knowledge
https://ashpublications.org/blood/article/123/6/905/32601/AZD1208-a-potent-and-selective-pan-Pim-kinase
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
442
Selectivity remarks
Screened at 1 µM, 16 kinases with >50% inhibition, in-vitro follow-up of closest targets: Kd(CDK7) = 38 nM, Kd(MAPK15) = 53 nM, others Kd(CAMK4) = 360 nM, Kd(DAPK1) = 420 nM, Kd(HIPK3) = 480 nM, Kd(STK17B) = 930 nM;
Selectivity Source Knowledge
https://ashpublications.org/blood/article/123/6/905/32601/AZD1208-a-potent-and-selective-pan-Pim-kinase