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Assay Detail

CHEMBL5029283

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

Binding
Inhibition of recombinant human PI3Kgamma assessed as reduction in ADP production using Dic8-PIP2 as substrate pre-treated for 15 mins followed by substrate addition measured after 60 mins by ADP-glo assay
29
Total Activities
29
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 29 8.86 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5090959 1 9.20
CHEMBL4129600 1 9.10
CHEMBL5089084 1 9.10
CHEMBL5071188 1 9.10
CHEMBL5090799 1 9.10
CHEMBL5088848 1 9.10
CHEMBL4126156 1 9.10
CHEMBL5089229 1 9.10
CHEMBL5081600 1 9.10
CHEMBL5078135 1 9.00
CHEMBL5084355 1 9.00
CHEMBL5077006 1 9.00
CHEMBL5090934 1 9.00
CHEMBL5084078 1 9.00
CHEMBL5080534 1 9.00
CHEMBL5091652 1 9.00
CHEMBL5085312 1 8.90
CHEMBL5091498 1 8.90
CHEMBL5082486 1 8.90
CHEMBL5082066 1 8.90
CHEMBL5081964 1 8.80
CHEMBL5072229 1 8.70
CHEMBL5091438 1 8.60
CHEMBL5085467 1 8.60
CHEMBL5077792 1 8.60
CHEMBL5077239 1 8.50
CHEMBL5076518 1 8.50
CHEMBL5087061 1 8.10
CHEMBL5081634 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5090959 IC50 = 0.631 nM 9.20
CHEMBL4129600 IC50 = 0.7943 nM 9.10
CHEMBL5089084 IC50 = 0.7943 nM 9.10
CHEMBL5071188 IC50 = 0.7943 nM 9.10
CHEMBL5090799 IC50 = 0.7943 nM 9.10
CHEMBL5088848 IC50 = 0.7943 nM 9.10
CHEMBL4126156 IC50 = 0.7943 nM 9.10
CHEMBL5089229 IC50 = 0.7943 nM 9.10
CHEMBL5081600 IC50 = 0.7943 nM 9.10
CHEMBL5078135 IC50 = 1.0 nM 9.00
CHEMBL5084355 IC50 = 1.0 nM 9.00
CHEMBL5077006 IC50 = 1.0 nM 9.00
CHEMBL5090934 IC50 = 1.0 nM 9.00
CHEMBL5084078 IC50 = 1.0 nM 9.00
CHEMBL5080534 IC50 = 1.0 nM 9.00
CHEMBL5091652 IC50 = 1.0 nM 9.00
CHEMBL5085312 IC50 = 1.259 nM 8.90
CHEMBL5091498 IC50 = 1.259 nM 8.90
CHEMBL5082486 IC50 = 1.259 nM 8.90
CHEMBL5082066 IC50 = 1.259 nM 8.90
CHEMBL5081964 IC50 = 1.585 nM 8.80
CHEMBL5072229 IC50 = 1.995 nM 8.70
CHEMBL5091438 IC50 = 2.512 nM 8.60
CHEMBL5085467 IC50 = 2.512 nM 8.60
CHEMBL5077792 IC50 = 2.512 nM 8.60
CHEMBL5077239 IC50 = 3.162 nM 8.50
CHEMBL5076518 IC50 = 3.162 nM 8.50
CHEMBL5087061 IC50 = 7.943 nM 8.10
CHEMBL5081634 IC50 = 10.0 nM 8.00