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Assay Detail

CHEMBL5720979

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Binding
Inhibition of human PI3Kbeta assessed as reduction in PIP3 product complex formation
8
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Inhibition of Human Class I vs Class III Phosphatidylinositol 3'-Kinases.
Hassett MR, Sternberg AR, Roepe PD.
Biochemistry (2017) 56 : 4326 -4334
PubMed 28719179 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.43 7.20
Ki 1 9.89 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1236962 OMIPALISIB 2.0 1 9.89
CHEMBL3218578 BGT-226 FREE BASE 2.0 1 7.20
CHEMBL1765602 1 6.75
CHEMBL5723005 1 6.70
CHEMBL1229535 1 6.23
CHEMBL3545097 SAPANISERTIB 2.0 1 5.28
CHEMBL3622372 1 -
CHEMBL3781415 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1236962 OMIPALISIB Ki = 0.13 nM 9.89
CHEMBL3218578 BGT-226 FREE BASE EC50 = 63.0 nM 7.20
CHEMBL1765602 EC50 = 180.0 nM 6.75
CHEMBL5723005 EC50 = 200.0 nM 6.70
CHEMBL1229535 EC50 = 590.0 nM 6.23
CHEMBL3545097 SAPANISERTIB EC50 = 5290.0 nM 5.28
CHEMBL3622372 EC50 > 10.0 nM -
CHEMBL3781415 EC50 > 9100.0 nM -