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Assay Detail

CHEMBL4231678

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Binding
Inhibition of PI3Kalpha (unknown origin) using Biotin-S11S12 as substrate after 60 mins in presence of ATP by Kinase Glo luminescence assay
3
Total Activities
3
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

Publication

Discovery of novel quinazolinone derivatives as high potent and selective PI3Kδ and PI3Kδ/γ inhibitors.
Ma CC, Zhang CM, Tang LQ, Liu ZP.
Eur J Med Chem (2018) 151 : 9 -17
PubMed 29601991 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.19 6.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2216870 IDELALISIB 4.0 1 6.13
CHEMBL4249477 1 4.93
CHEMBL4245221 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2216870 IDELALISIB IC50 = 737.0 nM 6.13
CHEMBL4249477 IC50 = 11814.0 nM 4.93
CHEMBL4245221 IC50 = 31291.0 nM 4.50