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Assay Detail

CHEMBL4195901

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant human full length GST-tagged PI4K3beta expressed in baculovirus expression system using PI lipid kinase substrate after 60 mins by ADP-Glo assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Phosphatidylinositol 4-kinase beta (CHEMBL3268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Potent, Orally Bioavailable PI4KIIIβ Inhibitor (UCB9608) Able To Significantly Prolong Allogeneic Organ Engraftment in Vivo.
Reuberson J, Horsley H, Franklin RJ, Ford D, Neuss J, Brookings D, Huang Q, Vanderhoydonck B, Gao LJ, Jang MY, Herdewijn P, Ghawalkar A, Fallah-Arani F, Khan AR, Henshall J, Jairaj M, Malcolm S, Ward E, Shuttleworth L, Lin Y, Li S, Louat T, Waer M, Herman J, Payne A, Ceska T, Doyle C, Pitt W, Calmiano M, Augustin M, Steinbacher S, Lammens A, Allen R.
J Med Chem (2018) 61 : 6705 -6723
PubMed 29952567 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 6.93 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4205416 1 8.70
CHEMBL4211696 1 8.40
CHEMBL4215340 1 8.40
CHEMBL4203566 1 8.15
CHEMBL4215244 1 8.15
CHEMBL2397317 1 8.10
CHEMBL4209793 1 8.10
CHEMBL4203041 1 8.10
CHEMBL4207851 1 8.05
CHEMBL1652677 1 8.00
CHEMBL4211181 1 7.96
CHEMBL4210308 1 7.96
CHEMBL4204100 1 7.75
CHEMBL4206816 1 7.72
CHEMBL4207928 1 7.70
CHEMBL4215615 1 7.38
CHEMBL4217096 1 7.29
CHEMBL4209824 1 6.94
CHEMBL4205444 1 6.84
CHEMBL4216301 1 6.76
CHEMBL4210718 1 6.67
CHEMBL4213363 1 6.56
CHEMBL4210332 1 6.51
CHEMBL4203671 1 6.50
CHEMBL4202963 1 6.38
CHEMBL4206897 1 6.29
CHEMBL4214728 1 6.26
CHEMBL4202542 1 6.21
CHEMBL4205943 1 6.02
CHEMBL4212822 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4205416 IC50 = 2.0 nM 8.70
CHEMBL4211696 IC50 = 4.0 nM 8.40
CHEMBL4215340 IC50 = 4.0 nM 8.40
CHEMBL4203566 IC50 = 7.0 nM 8.15
CHEMBL4215244 IC50 = 7.0 nM 8.15
CHEMBL2397317 IC50 = 8.0 nM 8.10
CHEMBL4209793 IC50 = 8.0 nM 8.10
CHEMBL4203041 IC50 = 8.0 nM 8.10
CHEMBL4207851 IC50 = 9.0 nM 8.05
CHEMBL1652677 IC50 = 10.0 nM 8.00
CHEMBL4210308 IC50 = 11.0 nM 7.96
CHEMBL4211181 IC50 = 11.0 nM 7.96
CHEMBL4204100 IC50 = 18.0 nM 7.75
CHEMBL4206816 IC50 = 19.0 nM 7.72
CHEMBL4207928 IC50 = 20.0 nM 7.70
CHEMBL4215615 IC50 = 42.0 nM 7.38
CHEMBL4217096 IC50 = 51.0 nM 7.29
CHEMBL4209824 IC50 = 114.0 nM 6.94
CHEMBL4205444 IC50 = 145.0 nM 6.84
CHEMBL4216301 IC50 = 173.0 nM 6.76
CHEMBL4210718 IC50 = 216.0 nM 6.67
CHEMBL4213363 IC50 = 275.0 nM 6.56
CHEMBL4210332 IC50 = 312.0 nM 6.51
CHEMBL4203671 IC50 = 316.0 nM 6.50
CHEMBL4202963 IC50 = 414.0 nM 6.38
CHEMBL4206897 IC50 = 517.0 nM 6.29
CHEMBL4214728 IC50 = 548.0 nM 6.26
CHEMBL4202542 IC50 = 611.0 nM 6.21
CHEMBL4205943 IC50 = 946.0 nM 6.02
CHEMBL4212822 IC50 = 981.0 nM 6.01
CHEMBL4215775 IC50 = 1000.0 nM 6.00
CHEMBL4208440 IC50 = 1412.0 nM 5.85
CHEMBL4204633 IC50 = 1500.0 nM 5.82
CHEMBL4214225 IC50 = 1946.0 nM 5.71
CHEMBL4217771 IC50 = 2577.0 nM 5.59
CHEMBL4208976 IC50 = 2583.0 nM 5.59
CHEMBL4218639 IC50 = 3387.0 nM 5.47
CHEMBL4215673 IC50 = 5743.0 nM 5.24
CHEMBL4213240 IC50 = 6138.0 nM 5.21
CHEMBL4212121 IC50 > 6000.0 nM -
CHEMBL4218178 IC50 > 10000.0 nM -