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Assay Detail

CHEMBL4124222

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

ADMET
Inhibition of recombinant human 6His-tagged PI3K p110beta/p85alpha using DiC8-PIP2 as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins by ADP-Glo assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Intermediate

Target

PI3K p110 beta/p85 alpha (CHEMBL3038510)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-γ Inhibitors.
Pemberton N, Mogemark M, Arlbrandt S, Bold P, Cox RJ, Gardelli C, Holden NS, Karabelas K, Karlsson J, Lever S, Li X, Lindmark H, Norberg M, Perry MWD, Petersen J, Rodrigo Blomqvist S, Thomas M, Tyrchan C, Westin Eriksson A, Zlatoidsky P, Öster L.
J Med Chem (2018) 61 : 5435 -5441
PubMed 29852070 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.89 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4127150 1 5.80
CHEMBL4126601 1 5.00
CHEMBL4127833 1 4.80
CHEMBL4126445 1 4.70
CHEMBL4127396 1 4.70
CHEMBL4129600 1 4.60
CHEMBL4126010 1 4.60
CHEMBL4127414 1 -
CHEMBL4128809 1 -
CHEMBL4128652 1 -
CHEMBL4130021 1 -
CHEMBL4129877 1 -
CHEMBL4128537 1 -
CHEMBL4128230 1 -
CHEMBL4126156 1 -
CHEMBL4129457 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4127150 IC50 = 1584.89 nM 5.80
CHEMBL4126601 IC50 = 10000.0 nM 5.00
CHEMBL4127833 IC50 = 15848.93 nM 4.80
CHEMBL4126445 IC50 = 19952.62 nM 4.70
CHEMBL4127396 IC50 = 19952.62 nM 4.70
CHEMBL4129600 IC50 = 25118.86 nM 4.60
CHEMBL4126010 IC50 = 25118.86 nM 4.60
CHEMBL4127414 IC50 > 31622.78 nM -
CHEMBL4128809 IC50 > 31622.78 nM -
CHEMBL4128652 IC50 > 31622.78 nM -
CHEMBL4130021 IC50 > 31622.78 nM -
CHEMBL4129877 IC50 > 31622.78 nM -
CHEMBL4128537 IC50 > 31622.78 nM -
CHEMBL4128230 IC50 > 31622.78 nM -
CHEMBL4126156 IC50 > 31622.78 nM -
CHEMBL4129457 IC50 > 31622.78 nM -