Compound name
SGC-PIKFYVE-1
Protein family
Protein Kinase
Target name
PIKFYVE
Affinity biochemical (nM)
6.9
Affinity on-target cellular (nM)
4
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001550a
SMILES
CN(C)CC#Cc1ccc2[nH]c3c(c2c1)-c1nc(N)ncc1CCC3
InChIKey
DORZPJWJOBMQKC-UHFFFAOYSA-N
NCBI gene ID
200576
UniProt ID
Q9Y2I7
Synonyms
CFD, FAB1, HEL37, PIP5K, PIP5K3, ZFYVE29
Mode of action
Inhibitor
Negative control
SGC-PIKFYVE-1N
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic assay (SignalChem)
Affinity Biochemical Source Knowledge
https://www.thesgc.org/chemical-probes/sgc-pikfyve-1
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (HEK293T cells)
Affinity on-target cellular source knowledge
https://www.thesgc.org/chemical-probes/sgc-pikfyve-1
Affinity on-target cellular relation
=
Selectivity platform
Kinome Scan (DiscoverX)
Selectivity platform number of targets
403
Selectivity remarks
Screened at 1 µM, closest targets as % of contr.: MYLK4 (1.8%), MEK1 (4.5%), RIPK5 (5.2%), IRAK3 (9.2%), MEK2 (9.6%), DYRK1A (9.9%), YSK4 (9.9%), ULK3(11%), MEK4 (12%), HASPIN (13%), STK16 (14%), CLK2 (20%), CDK7 (20%), IRAK4 (21%), AURKB (23%), DYRK1B (26%), CLK1 (30%), RIOK2 (32%), CLK4 (34%), PIP4K2C (53%), MAP4K5 (96%); In-vitro follow-up of closest targets: IC50(MYLK4) = 66 nM, IC50(MEK1) >10000 nM, IC50(RIPK5) >10000 nM, IC50(MEK2) >10000 nM, IC50(DYRK1A) = 2040 nM, IC50(YSK4) = 4020 nM, IC50(ULK3) >10000 nM, IC50(MEK4) >10000 nM, IC50(HASPIN) = 1400 nM, IC50(STK16) = 560 nM, IC50(CLK2) = 290 nM, IC50(CDK7) >10000 nM, IC50(IRAK4) = 4500 nM, IC50(AURKB) = 1400 nM, IC50(DYRK1B) = 380 nM, IC50(CLK1) = 420 nM, IC50(CLK4) = 440 nM, IC50(PIP4K2C) = 1900 nM, IC50(MAP4K5) = 89 nM; In-cellulo follow-up of closest targets (NanoBRET assay in HEK293T cells): IC50(MYLK4) = 270 nM, IC50(PIP4K2C) >10000 nM, IC50(MAP4K5) >10000 nM (https://www.thesgc.org/chemical-probes/sgc-pikfyve-1)
Selectivity Source Knowledge
https://www.thesgc.org/chemical-probes/sgc-pikfyve-1