Compound name
GSK2606414
Protein family
Protein Kinase
Target name
RIPK1
Affinity biochemical (nM)
18.2
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001324a
SMILES
Cn1cc(-c2ccc3c(c2)CCN3C(=O)Cc2cccc(C(F)(F)F)c2)c2c(N)ncnc21
InChIKey
SIXVRXARNAVBTC-UHFFFAOYSA-N
NCBI gene ID
8737
UniProt ID
Q13546
Synonyms
RIP
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
ADP-Glo assay
Affinity Biochemical Source Knowledge
https://www.nature.com/articles/cdd201758
Affinity biochemical relation
=
Selectivity platform
Kinase panel (Reaction Biology)
Selectivity platform number of targets
294
Selectivity remarks
Screened at 10 µM, using conc. ATP = Km, closest targets as % of control: DDR2 (0.08%), MAP3K9 (1.20%), MAP4K5 (3.22%), BRK (4.25%), MER(4.34%), MAP3K11 (4.40%), MYLK2 (4.41%), RET (4.80%), MAP3K10 (5.86%), NTRK1 (5.92%), NTRK3 (6.85%), IKBKE (8.81%), LCK (10.19%), full screening data available as supporting information, https://pubmed.ncbi.nlm.nih.gov/22827572/;
In-vitro follow-up of closest targets in the screen (enzymatic assay, ReactionBiology): IC50(KIT) = 154 nM, IC50(AURKB) = 407 nM, IC50(BRK) = 412 nM, IC50(MAP3K10) = 452 nM, IC50(MER) = 474 nM, IC50(DDR2) = 524 nM, IC50(MYLK2) = 701 nM, IC50(IKBKE) = 1064 nM, IC50(MAP3K11) = 1140 nM, IC500(RET) = 1215 nM, IC50(LCK) = 1250 nM, IC50(NEK4) = 1402 nM, IC50(MAP4K5) = 1569 nM, IC50(MAp3K9) = 1578 nM, IC50(NTRK1) = 1756 nM, IC50(AXL) = 2705 nM, IC50(YES1) = 3195 nM, IC50(WNK2) = 3892 nM, https://pubmed.ncbi.nlm.nih.gov/22827572/;
In-vitro potency (HTRF assay): IC50(EIF2AK1) = 420 nM, https://pubmed.ncbi.nlm.nih.gov/22827572/;
In-vitro potency (HTRF assay): IC50(EIF2AK2) = 696 nM, https://pubmed.ncbi.nlm.nih.gov/22827572/;
In-vitro potency (ADP-Glo assay): IC50(RIPK1) = 18.2 nM, https://www.nature.com/articles/cdd201758;
In-vitro follow-up of closest targets in the screen (enzymatic assay, ReactionBiology): IC50(KIT) = 154 nM, IC50(AURKB) = 407 nM, IC50(BRK) = 412 nM, IC50(MAP3K10) = 452 nM, IC50(MER) = 474 nM, IC50(DDR2) = 524 nM, IC50(MYLK2) = 701 nM, IC50(IKBKE) = 1064 nM, IC50(MAP3K11) = 1140 nM, IC500(RET) = 1215 nM, IC50(LCK) = 1250 nM, IC50(NEK4) = 1402 nM, IC50(MAP4K5) = 1569 nM, IC50(MAp3K9) = 1578 nM, IC50(NTRK1) = 1756 nM, IC50(AXL) = 2705 nM, IC50(YES1) = 3195 nM, IC50(WNK2) = 3892 nM, https://pubmed.ncbi.nlm.nih.gov/22827572/;
In-vitro potency (HTRF assay): IC50(EIF2AK1) = 420 nM, https://pubmed.ncbi.nlm.nih.gov/22827572/;
In-vitro potency (HTRF assay): IC50(EIF2AK2) = 696 nM, https://pubmed.ncbi.nlm.nih.gov/22827572/;
In-vitro potency (ADP-Glo assay): IC50(RIPK1) = 18.2 nM, https://www.nature.com/articles/cdd201758;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/22827572/
Selectivity Number of Off-targets
7