Compound name
SGC-PI5P4Ky-1
Protein family
Protein Kinase
Target name
PIP4K2C
Affinity biochemical (nM)
19
Affinity on-target cellular (nM)
67
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001874a
SMILES
Nc1ncc2c(n1)-c1c([nH]c3ccc(C4=CCOCC4)cc13)CCC2
InChIKey
VGFHPNRWHOQLEB-UHFFFAOYSA-N
NCBI gene ID
79837
UniProt ID
Q8TBX8
Synonyms
PIP5K2C
Mode of action
Inhibitor
Negative control
SGC-PI5P4Ky-1n
Affinity biochemical definition
Kd
Affinity biochemical assay type
Binding assay
Affinity Biochemical Source Knowledge
https://www.sciencedirect.com/science/article/pii/S2666246922000180
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (intact HEK293T cells)
Affinity on-target cellular source knowledge
https://www.sciencedirect.com/science/article/pii/S2666246922000180
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
403
Selectivity remarks
Screened at 1 µM, closest targets as % of control: PIKFYVE (0%), PIP5K1C (0%), MYLK4 (0.1%), TYK2 (1.1%), PIP5K2C (1.7%), RIPK5 (6.9%), YSK4 (9.4%), DYRK1A (17%), full screening data are available as supporting information, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (HTRF assay, using ATP = Km): IC50(PIP5K1C) = 840 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (ADP-Glo assay): IC50(PIKFYVE) = 12 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (NanoBRET assay, HEK293T cells): IC50(PIKFYVE) = 450 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(TYK2) >10000 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (HotSpot kinase assays, using ATP = Km, Reaction Biology): IC50(RIPK5) = 6100 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (HotSpot kinase assays, using ATP = Km, Reaction Biology): IC50(YSK4) = 600 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (radiometric assay, using ATP = Km, Eurofins): IC50(DYRK1A) = 520 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (radiometric assay, using ATP = Km, Eurofins): IC50(CLK2) = 370 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (NanoBRET assay, HEK293T cells): IC50(DYRK1A) >10000 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (NanoBRET assay, HEK293T cells): IC50(CLK2) = 3200 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (radiometric assay, using ATP = Km, Eurofins): IC50(STK16) = 1200 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (HTRF assay, using ATP = Km): IC50(PIP5K1C) = 840 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (ADP-Glo assay): IC50(PIKFYVE) = 12 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (NanoBRET assay, HEK293T cells): IC50(PIKFYVE) = 450 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-cellular potency (NanoBRET assay, HEK293T cells): IC50(TYK2) >10000 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (HotSpot kinase assays, using ATP = Km, Reaction Biology): IC50(RIPK5) = 6100 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (HotSpot kinase assays, using ATP = Km, Reaction Biology): IC50(YSK4) = 600 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (radiometric assay, using ATP = Km, Eurofins): IC50(DYRK1A) = 520 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (radiometric assay, using ATP = Km, Eurofins): IC50(CLK2) = 370 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (NanoBRET assay, HEK293T cells): IC50(DYRK1A) >10000 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (NanoBRET assay, HEK293T cells): IC50(CLK2) = 3200 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
In-vitro potency (radiometric assay, using ATP = Km, Eurofins): IC50(STK16) = 1200 nM, https://www.sciencedirect.com/science/article/pii/S2666246922000180;
Selectivity Source Knowledge
https://www.sciencedirect.com/science/article/pii/S2666246922000180
Selectivity Number of Off-targets
7