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Assay Detail

CHEMBL5730889

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Binding
PI3K Delta Assay: In some embodiments, the PI3Kδ inhibitor is selective. By ¿selective¿ is meant that the compound binds to or inhibits a kinase with greater affinity or potency, respectively, compared to at least one other kinase. In some embodiments, the PI3Kδ inhibitors are selective inhibitors of PI3Kδ (e.g., over PI3Kα, PI3Kβ and PI3Kγ). In some embodiments, selectivity can be at least about 2-fold, 5-fold, 10-fold, at least about 20-fold, at least about 50-fold, at least about 100-fold, at least about 200-fold, at least about 500-fold or at least about 1000-fold. Selectivity can be measured by methods routine in the art. In some embodiments, selectivity can be tested at the Km ATP concentration of each enzyme. In some embodiments, the selectivity of compounds described herein can be determined by cellular assays associated with particular PI3K kinase activity.
24
Total Activities
8
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Pyrrolopyrimidine derivatives as TAM inhibitors
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.12 7.12
kon 8 - -
k_off 8 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4576207 3 7.12
CHEMBL5775827 3 -
CHEMBL2216863 DEZAPELISIB 2.0 3 -
CHEMBL5965697 3 -
CHEMBL5847111 3 -
CHEMBL5773238 3 -
CHEMBL5914931 3 -
CHEMBL2216867 3 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4576207 IC50 = 75.0 nM 7.12
CHEMBL5775827 IC50 < 50.0 nM -
CHEMBL5775827 kon = - -
CHEMBL5775827 k_off = - s-1 -
CHEMBL2216863 DEZAPELISIB IC50 < 50.0 nM -
CHEMBL2216863 DEZAPELISIB kon = - -
CHEMBL2216863 DEZAPELISIB k_off = - s-1 -
CHEMBL5965697 IC50 < 50.0 nM -
CHEMBL5965697 kon = - -
CHEMBL5965697 k_off = - s-1 -
CHEMBL5847111 IC50 < 50.0 nM -
CHEMBL5847111 kon = - -
CHEMBL5847111 k_off = - s-1 -
CHEMBL5773238 kon = - -
CHEMBL5773238 k_off = - s-1 -
CHEMBL5914931 IC50 < 50.0 nM -
CHEMBL5914931 kon = - -
CHEMBL5914931 k_off = - s-1 -
CHEMBL2216867 IC50 < 50.0 nM -
CHEMBL2216867 kon = - -
CHEMBL2216867 k_off = - s-1 -
CHEMBL4576207 kon = - -
CHEMBL4576207 k_off = - s-1 -
CHEMBL5773238 IC50 < 50.0 nM -