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Assay Detail

CHEMBL4231676

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Binding
Inhibition of PI3Kdelta (unknown origin) using Biotin-S11S12 as substrate after 120 mins in presence of ATP by ADPGlo luminescence assay
15
Total Activities
15
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 15 7.42 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2216870 IDELALISIB 4.0 1 8.80
CHEMBL4249477 1 8.08
CHEMBL4245221 1 8.07
CHEMBL4250311 1 7.80
CHEMBL4249850 1 7.58
CHEMBL4241373 1 7.51
CHEMBL4243529 1 7.39
CHEMBL4250842 1 7.09
CHEMBL4238027 1 7.08
CHEMBL4246053 1 7.07
CHEMBL4239740 1 6.97
CHEMBL4251492 1 6.64
CHEMBL4243064 1 6.38
CHEMBL4239308 1 -
CHEMBL4248031 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2216870 IDELALISIB IC50 = 1.6 nM 8.80
CHEMBL4249477 IC50 = 8.4 nM 8.08
CHEMBL4245221 IC50 = 8.6 nM 8.07
CHEMBL4250311 IC50 = 16.0 nM 7.80
CHEMBL4249850 IC50 = 26.0 nM 7.58
CHEMBL4241373 IC50 = 31.0 nM 7.51
CHEMBL4243529 IC50 = 41.0 nM 7.39
CHEMBL4250842 IC50 = 81.0 nM 7.09
CHEMBL4238027 IC50 = 84.0 nM 7.08
CHEMBL4246053 IC50 = 86.0 nM 7.07
CHEMBL4239740 IC50 = 106.0 nM 6.97
CHEMBL4251492 IC50 = 227.0 nM 6.64
CHEMBL4243064 IC50 = 416.0 nM 6.38
CHEMBL4239308 IC50 - -
CHEMBL4248031 IC50 - -