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Assay Detail

CHEMBL5029296

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

Binding
Inhibition of PIK3C2B (unknown origin) assessed as reduction in substrate phosphorylation by FRET Adapta assay
3
Total Activities
3
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

Discovery of AZD8154, a Dual PI3Kγδ Inhibitor for the Treatment of Asthma.
Perry MWD, Björhall K, Bold P, Brűlls M, Börjesson U, Carlsson J, Chang HA, Chen Y, Eriksson A, Fihn BM, Fransson R, Fredlund L, Ge H, Huang H, Karabelas K, Lamm Bergström E, Lever S, Lindmark H, Mogemark M, Nikitidis A, Palmgren AP, Pemberton N, Petersen J, Rodrigo Blomqvist M, Smith RW, Thomas MJ, Ullah V, Tyrchan C, Wennberg T, Westin Eriksson A, Yang W, Zhao S, Öster L.
J Med Chem (2021) 64 : 8053 -8075
PubMed 34080862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.87 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5091438 1 9.10
CHEMBL5077865 1 9.00
CHEMBL4558527 AZD-8154 2.0 1 8.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5091438 IC50 = 0.7943 nM 9.10
CHEMBL5077865 IC50 = 1.0 nM 9.00
CHEMBL4558527 AZD-8154 IC50 = 3.162 nM 8.50