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Assay Detail

CHEMBL4135740

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

Binding
Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate pretreated for 15 mins followed by substrate addition measured after 1 hr
9
Total Activities
9
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

From PIM1 to PI3Kδ via GSK3β: Target Hopping through the Kinome.
Henley ZA, Bax BD, Inglesby LM, Champigny A, Gaines S, Faulder P, Le J, Thomas DA, Washio Y, Baldwin IR.
ACS Med Chem Lett (2017) 8 : 1093 -1098
PubMed 29057057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.68 5.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4165288 1 5.00
CHEMBL4176717 1 4.70
CHEMBL4172211 1 4.60
CHEMBL4168859 1 4.60
CHEMBL4174177 1 4.60
CHEMBL4175904 1 4.60
CHEMBL260163 1 -
CHEMBL4161596 1 -
CHEMBL4163479 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4165288 IC50 = 10000.0 nM 5.00
CHEMBL4176717 IC50 = 19952.62 nM 4.70
CHEMBL4172211 IC50 = 25118.86 nM 4.60
CHEMBL4168859 IC50 = 25118.86 nM 4.60
CHEMBL4174177 IC50 = 25118.86 nM 4.60
CHEMBL4175904 IC50 = 25118.86 nM 4.60
CHEMBL260163 IC50 > 25118.86 nM -
CHEMBL4161596 IC50 > 25118.86 nM -
CHEMBL4163479 IC50 > 25118.86 nM -