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Assay Detail

CHEMBL3122829

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

Binding
Inhibition of GST-tagged PI4K-alpha (1 to 2044) (unknown origin) using D-myo-phosphatidylinositol as substrate preincubated for 30 mins followed by substrate addition measured after 180 mins by luminescence assay
29
Total Activities
27
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 alpha (CHEMBL3667)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of selective small molecule type III phosphatidylinositol 4-kinase alpha (PI4KIIIα) inhibitors as anti hepatitis C (HCV) agents.
Leivers AL, Tallant M, Shotwell JB, Dickerson S, Leivers MR, McDonald OB, Gobel J, Creech KL, Strum SL, Mathis A, Rogers S, Moore CB, Botyanszki J.
J Med Chem (2014) 57 : 2091 -2106
PubMed 23944386 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.69 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3121323 1 9.50
CHEMBL3121314 1 9.10
CHEMBL3121319 1 9.00
CHEMBL3121322 1 9.00
CHEMBL3121327 1 8.80
CHEMBL3121334 1 8.80
CHEMBL3121318 1 8.60
CHEMBL3121320 1 8.40
CHEMBL3121308 3 8.30
CHEMBL3121333 1 8.30
CHEMBL3121324 1 8.20
CHEMBL3121326 1 8.00
CHEMBL3121311 1 8.00
CHEMBL3121321 1 7.80
CHEMBL3121316 1 7.70
CHEMBL3121312 1 7.50
CHEMBL3121325 1 7.40
CHEMBL3121328 1 7.40
CHEMBL3121310 1 7.30
CHEMBL3121309 1 7.30
CHEMBL3121329 1 7.00
CHEMBL3121317 1 6.90
CHEMBL3121331 1 6.70
CHEMBL3121313 1 6.50
CHEMBL3121330 1 6.20
CHEMBL3121315 1 5.40
CHEMBL3121332 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3121323 IC50 = 0.3162 nM 9.50
CHEMBL3121314 IC50 = 0.7943 nM 9.10
CHEMBL3121319 IC50 = 1.0 nM 9.00
CHEMBL3121322 IC50 = 1.0 nM 9.00
CHEMBL3121327 IC50 = 1.585 nM 8.80
CHEMBL3121334 IC50 = 1.585 nM 8.80
CHEMBL3121318 IC50 = 2.512 nM 8.60
CHEMBL3121320 IC50 = 3.981 nM 8.40
CHEMBL3121333 IC50 = 5.012 nM 8.30
CHEMBL3121308 IC50 = 5.012 nM 8.30
CHEMBL3121324 IC50 = 6.31 nM 8.20
CHEMBL3121326 IC50 = 10.0 nM 8.00
CHEMBL3121311 IC50 = 10.0 nM 8.00
CHEMBL3121321 IC50 = 15.85 nM 7.80
CHEMBL3121308 IC50 = 15.85 nM 7.80
CHEMBL3121316 IC50 = 19.95 nM 7.70
CHEMBL3121312 IC50 = 31.62 nM 7.50
CHEMBL3121325 IC50 = 39.81 nM 7.40
CHEMBL3121328 IC50 = 39.81 nM 7.40
CHEMBL3121310 IC50 = 50.12 nM 7.30
CHEMBL3121309 IC50 = 50.12 nM 7.30
CHEMBL3121329 IC50 = 100.0 nM 7.00
CHEMBL3121317 IC50 = 125.89 nM 6.90
CHEMBL3121308 IC50 = 125.89 nM 6.90
CHEMBL3121331 IC50 = 199.53 nM 6.70
CHEMBL3121313 IC50 = 316.23 nM 6.50
CHEMBL3121330 IC50 = 630.96 nM 6.20
CHEMBL3121315 IC50 = 3981.07 nM 5.40
CHEMBL3121332 IC50 = 7943.28 nM 5.10