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Assay Detail

CHEMBL2157253

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Binding
Inhibition of PI3Kdelta-mediated AKT phosphorylation in B cells in presence of human serum
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type B
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.
Sutherlin DP, Baker S, Bisconte A, Blaney PM, Brown A, Chan BK, Chantry D, Castanedo G, DePledge P, Goldsmith P, Goldstein DM, Hancox T, Kaur J, Knowles D, Kondru R, Lesnick J, Lucas MC, Lewis C, Murray J, Nadin AJ, Nonomiya J, Pang J, Pegg N, Price S, Reif K, Safina BS, Salphati L, Staben S, Seward EM, Shuttleworth S, Sohal S, Sweeney ZK, Ultsch M, Waszkowycz B, Wei B.
Bioorg Med Chem Lett (2012) 22 : 4296 -4302
PubMed 22672799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.97 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2152768 1 7.40
CHEMBL2152769 1 7.26
CHEMBL2152772 1 7.17
CHEMBL2152771 1 6.84
CHEMBL2152773 1 6.84
CHEMBL2152770 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2152768 IC50 = 40.0 nM 7.40
CHEMBL2152769 IC50 = 55.0 nM 7.26
CHEMBL2152772 IC50 = 67.0 nM 7.17
CHEMBL2152771 IC50 = 145.0 nM 6.84
CHEMBL2152773 IC50 = 145.0 nM 6.84
CHEMBL2152770 IC50 = 480.0 nM 6.32