Compound name
NR162
Protein family
Protein Kinase
Target name
CASK
Affinity biochemical (nM)
22
Affinity on-target cellular (nM)
80
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000723a
SMILES
O=C(NCCCN1CCOC1=O)C2=CN=C(NCC3=CC(Br)=CC=C3Br)N=C2NC4CCCC4
InChIKey
HOYFKJXFPMNFPM-UHFFFAOYSA-N
NCBI gene ID
8573
UniProt ID
O14936
Synonyms
LIN2, CAGH39, FGS4
Mode of action
Inhibitor
Negative control
NR187
Affinity biochemical definition
Kd
Affinity biochemical assay type
ITC
Affinity Biochemical Source Knowledge
https://www.thesgc.org/chemical-probes/NR162
https://doi.org/10.1021/acs.jmedchem.1c00845
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
KinomeScan (DiscoverX)
Selectivity platform number of targets
448
Selectivity remarks
Screened at 1 µM; 8 additional targets: AURKC, ABL1, RPS6KA6, PIKFYVE, ERBB3, RPS6KA5, LRRK2 and STK38L, initially identified, but confirmed as false positive by NanoBRET: closest targets: IC50(TYRO3) = 3.8 µM (47-fold selective), IC50(ERBB3) = 18.2 µM (227-fold selective), other targets >20 µM in NanoBRET assays.
Selectivity Source Knowledge
https://www.thesgc.org/chemical-probes/NR162
https://doi.org/10.1021/acs.jmedchem.1c00845
Selectivity Number of Off-targets
8