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Assay Detail

CHEMBL3404165

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

Binding
Inhibition of PI3Kdelta (unknown origin) assessed as inhibition of AKT phosphorylation by cell-based HTRF 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 SAR study of potent and selective PI3Kδ inhibitors.
Bui M, Hao X, Shin Y, Cardozo M, He X, Henne K, Suchomel J, McCarter J, McGee LR, San Miguel T, Medina JC, Mohn D, Tran T, Wannberg S, Wong J, Wong S, Zalameda L, Metz D, Cushing TD.
Bioorg Med Chem Lett (2015) 25 : 1104 -1109
PubMed 25666823 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.65 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3403664 1 10.00
CHEMBL2216892 1 9.30
CHEMBL3403665 1 9.10
CHEMBL3403676 1 8.92
CHEMBL3403675 1 8.85
CHEMBL3403670 1 8.62
CHEMBL2216870 IDELALISIB 4.0 1 8.57
CHEMBL3403666 1 8.55
CHEMBL3403669 1 8.51
CHEMBL3400185 1 8.51
CHEMBL3403674 1 8.44
CHEMBL3403678 1 8.34
CHEMBL3403668 1 8.15
CHEMBL3403673 1 7.96
CHEMBL3403677 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3403664 IC50 = 0.1 nM 10.00
CHEMBL2216892 IC50 = 0.5 nM 9.30
CHEMBL3403665 IC50 = 0.8 nM 9.10
CHEMBL3403676 IC50 = 1.2 nM 8.92
CHEMBL3403675 IC50 = 1.4 nM 8.85
CHEMBL3403670 IC50 = 2.4 nM 8.62
CHEMBL2216870 IDELALISIB IC50 = 2.7 nM 8.57
CHEMBL3403666 IC50 = 2.8 nM 8.55
CHEMBL3403669 IC50 = 3.1 nM 8.51
CHEMBL3400185 IC50 = 3.1 nM 8.51
CHEMBL3403674 IC50 = 3.6 nM 8.44
CHEMBL3403678 IC50 = 4.6 nM 8.34
CHEMBL3403668 IC50 = 7.0 nM 8.15
CHEMBL3403673 IC50 = 11.0 nM 7.96
CHEMBL3403677 IC50 = 12.0 nM 7.92