GSK-A1 is a potent inhibitor of PI4KA. In vitro using HEK-AT1 cells, GSK-A1 had an IC50 of about 3 nM.

KDU691 is a PI4K inhibitor.

NVP-BQR695 is a novel PI3K inhibitor.

PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM; shown to inhibit PI3Kα with IC50 of 39 nM.

UCB9608 is a Potent, Orally Bioavailable PI4KIIIβ Inhibitor.

UCT943 (UCT-943) is a potent, selective, next generation Plasmodium falciparum PI4K inhibitor with IC50 of 23 nM.

AZ3 (PI4KB inhibitor 3) is a seletive PI4KB inhibitor with pIC50 of 7.8, shows good lipid kinase selectivity (pIC50 5.1, 4.7 and 4.0 for PI4Kα, PI3Kα and PIP5Kγ respectively).

AZ7 (PI4KA inhibitor 7) is a potent, selective PI4KA inhibitor with pIC50 of 8.2, >100-fold selectivity over PI4Kβ, PI3Kα and PIP5Kγ.AZ7 inhibited the accumulation of IP1 (pIC50 6.3) caused a qualitative reduction in cellular PIP, PIP2 and PIP3 levels.PI4KA inhibitor 7 inhibited cell growth with pGI50 values of >5.0 in 91 of the cell lines in a panel of 183 cancer cell lines.

Pipinib is a small molecule Hedgehog signaling inhibitior by selective inhibition of phosphatidylinositol 4-kinase IIIβ (PI4KB, IC50=2.2 uM), inhibits Purmorphamine-induced osteogenesis with IC50 of 0.6 uM.Pipinib inhibited GLI reporter gene activity in Sonic hedgehog (Shh)-LIGHT2 cells (IC50=1.7 uM) and expression of Hh target genes Ptch1 and Gli1 (IC50=3.1 uM and 4.1 uM, respectively).Pipinib does not modulate Hh signaling via SMO.Pipinib is an ATP-competitive inhibitor of PI4KB activity, does not inhibit isoenzymes PI4KA, PI4K2A or PI4K2B up to 50 uM.Pipinib suppresses GLI-mediated transcription and Hh target gene expression by impairing SMO translocation to the cilium.

CHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selective PfPI4K (Plasmodium falciparum PI4K kinase) inhibitor, with an IC50 of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7 Plasmodium falciparum, with an EC50 of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy.

MI 14 is a selective PI4KIIIβ inhibitor with IC50s of 54 nM, >100 μM, >100 μM for PI4KIIIβ, PI4KIIIα, PI4KIIα, respectively. MI 14 has antiviral activity against HCV 1b, CVB3, HRVM, HVC 2a.

GSK-3923868 (PI4KB inhibitor 30) is a potent, selective, slow-dissociating PI4KB (PI4kIII-beta) inhibitor with pKi of 9.8, >1000-fold selectivity over PI4KA, inhibits HRV viral replication in COPD BECs.

EDI048 (compound 1.16) is an orally active Cryptosporidium PI4K inhibitor for the research of cryptosporidiosis.