Compound name
FM-381
Protein family
Protein Kinase
Target name
JAK3@kinase 1
Affinity biochemical (nM)
0.154
Affinity on-target cellular (nM)
100
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000006b
SMILES
CN(C)C(=O)/C(C#N)=C/c1ccc(-c2nc3cnc4[nH]ccc4c3n2C2CCCCC2)o1
InChIKey
GJMZWYLOARVASY-NTCAYCPXSA-N
NCBI gene ID
3718
UniProt ID
P52333
Synonyms
L-JAK, JAKL, LJAK, JAK3_HUMAN, JAK-3
Mode of action
Inhibitor
Negative control
FM-479
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radiometric inhibition assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1016/j.chembiol.2016.10.008
https://www.thesgc.org/chemical-probes/FM-381
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (HEK293T cells)
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (ProQinase)
Selectivity platform number of targets
410
Selectivity remarks
No targets with >70% inhibition at 100 nM and 500 nM
Selectivity Source Knowledge
https://doi.org/10.1016/j.chembiol.2016.10.008
https://www.thesgc.org/chemical-probes/FM-381
Selectivity Number of Off-targets
0