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Assay Detail

CHEMBL4399809

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

Binding
Inhibition of PI3K delta (unknown origin) using phosphatidyl inositol as substrate measured after 60 mins in presence of ATP by Kinase-Glo Plus reagent-based 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

Synthesis and biological evaluation of 4-(piperid-3-yl)amino substituted 6-pyridylquinazolines as potent PI3Kδ inhibitors.
Feng Y, Duan W, Fan S, Zhang H, Zhang SQ, Xin M.
Bioorg Med Chem (2019) 27 : 115035 -115035
PubMed 31434616 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.37 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4468088 1 9.15
CHEMBL2216870 IDELALISIB 4.0 1 8.92
CHEMBL4476303 1 8.89
CHEMBL4563455 1 8.60
CHEMBL4568130 1 8.49
CHEMBL4515495 1 8.49
CHEMBL4473306 1 8.43
CHEMBL4457318 1 8.41
CHEMBL4459721 1 8.33
CHEMBL4457688 1 8.17
CHEMBL4561357 1 8.11
CHEMBL4562892 1 8.05
CHEMBL4533939 1 8.03
CHEMBL4544144 1 7.84
CHEMBL4530540 1 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4468088 IC50 = 0.7 nM 9.15
CHEMBL2216870 IDELALISIB IC50 = 1.2 nM 8.92
CHEMBL4476303 IC50 = 1.3 nM 8.89
CHEMBL4563455 IC50 = 2.5 nM 8.60
CHEMBL4568130 IC50 = 3.2 nM 8.49
CHEMBL4515495 IC50 = 3.2 nM 8.49
CHEMBL4473306 IC50 = 3.7 nM 8.43
CHEMBL4457318 IC50 = 3.9 nM 8.41
CHEMBL4459721 IC50 = 4.7 nM 8.33
CHEMBL4457688 IC50 = 6.8 nM 8.17
CHEMBL4561357 IC50 = 7.7 nM 8.11
CHEMBL4562892 IC50 = 8.9 nM 8.05
CHEMBL4533939 IC50 = 9.4 nM 8.03
CHEMBL4544144 IC50 = 14.3 nM 7.84
CHEMBL4530540 IC50 = 27.0 nM 7.57