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Assay Detail

CHEMBL4430049

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

Binding
Inhibition of PI3Kdelta in Balb/c mouse B cells assessed as reduction in anti-IgM induced CD86 expression preincubated for 1 hr followed by anti-IgM stimulation for 24 hrs by flow cytometry
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.
Hoegenauer K, Soldermann N, Stauffer F, Furet P, Graveleau N, Smith AB, Hebach C, Hollingworth GJ, Lewis I, Gutmann S, Rummel G, Knapp M, Wolf RM, Blanz J, Feifel R, Burkhart C, Zécri F.
ACS Med Chem Lett (2016) 7 : 762 -767
PubMed 27563400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.07 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4588314 1 7.58
CHEMBL3944013 1 7.47
CHEMBL3947814 1 7.16
CHEMBL3977066 1 7.16
CHEMBL4453497 1 7.13
CHEMBL4454454 1 7.07
CHEMBL4467868 1 7.06
CHEMBL4581278 1 7.06
CHEMBL4521888 1 7.03
CHEMBL4460621 1 6.95
CHEMBL4437791 1 6.72
CHEMBL4469006 1 6.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4588314 IC50 = 26.0 nM 7.58
CHEMBL3944013 IC50 = 34.0 nM 7.47
CHEMBL3947814 IC50 = 70.0 nM 7.16
CHEMBL3977066 IC50 = 70.0 nM 7.16
CHEMBL4453497 IC50 = 74.0 nM 7.13
CHEMBL4454454 IC50 = 86.0 nM 7.07
CHEMBL4467868 IC50 = 87.0 nM 7.06
CHEMBL4581278 IC50 = 87.0 nM 7.06
CHEMBL4521888 IC50 = 93.0 nM 7.03
CHEMBL4460621 IC50 = 112.0 nM 6.95
CHEMBL4437791 IC50 = 190.0 nM 6.72
CHEMBL4469006 IC50 = 393.0 nM 6.41