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Assay Detail

CHEMBL3868302

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Binding
Inhibition of PI3K-delta in rat whole blood assessed as inhibition of anti-IgM/IL4 induced CD86 expression
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Blood
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties.
Hoegenauer K, Soldermann N, Hebach C, Hollingworth GJ, Lewis I, von Matt A, Smith AB, Wolf RM, Wilcken R, Haasen D, Burkhart C, Zécri F.
Bioorg Med Chem Lett (2016) 26 : 5657 -5662
PubMed 27816514 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.88 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3944013 1 7.46
CHEMBL3947814 1 7.18
CHEMBL3977066 1 7.14
CHEMBL3966263 1 6.55
CHEMBL3896413 1 6.53
CHEMBL3905342 1 6.42
CHEMBL3939028 1 -
CHEMBL3930000 1 -
CHEMBL3910692 1 -
CHEMBL3921081 1 -
CHEMBL3948901 1 -
CHEMBL3969716 1 -
CHEMBL3914282 1 -
CHEMBL3960012 1 -
CHEMBL3933360 1 -
CHEMBL3977135 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3944013 IC50 = 35.0 nM 7.46
CHEMBL3947814 IC50 = 66.0 nM 7.18
CHEMBL3977066 IC50 = 72.0 nM 7.14
CHEMBL3966263 IC50 = 282.0 nM 6.55
CHEMBL3896413 IC50 = 297.0 nM 6.53
CHEMBL3905342 IC50 = 377.0 nM 6.42
CHEMBL3939028 IC50 - -
CHEMBL3930000 IC50 - -
CHEMBL3910692 IC50 - -
CHEMBL3921081 IC50 - -
CHEMBL3948901 IC50 - -
CHEMBL3969716 IC50 - -
CHEMBL3914282 IC50 - -
CHEMBL3960012 IC50 - -
CHEMBL3933360 IC50 - -
CHEMBL3977135 IC50 - -