Compound name
GSK8612
Protein family
Protein Kinase
Target name
TBK1
Affinity biochemical (nM)
10
Affinity on-target cellular (nM)
1000
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002248a
SMILES
Cc1nn(CC(F)(F)F)cc1Nc1ncc(Br)c(NCc2ccc(S(N)(=O)=O)cc2)n1
InChIKey
FFPHMUIGESPOTK-UHFFFAOYSA-N
NCBI gene ID
29110
UniProt ID
Q9UHD2
Synonyms
NAK
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radiometric assay (HotSpot assay, Reaction Biology)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/31097999/
Affinity biochemical relation
=
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Western Blot assay (phosphorylation of IRF3 using Ramos cells stimulated with TLR3 ligand poly(I:C))
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/31097999/
Affinity on-target cellular relation
<
Selectivity platform
Chemoproteomics (kinobeads in mixed HEK293, K-562, HepG2, and placenta cell extracts and lipid kinobeads in mixed HeLa, Jurkat, and K-562 cell extracts)
Selectivity platform number of targets
285
Selectivity remarks
In-vitro potency of closest targets in the screen: IC50(TBK1) = 12.6 nM, IC50(STK17B) = 631 nM, IC50(IKBKE) = 631 nM, IC50(LRRK2) = 1259 nM, IC50(FLT4) = 1585 nM, IC50(CSNK2A1) = 2512 nM, full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/31097999/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/31097999/
Selectivity Number of Off-targets
2