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Assay Detail

CHEMBL4370796

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Binding
Inhibition of recombinant human PI3Kbeta using PIP2 as substrate after 35 to 40 mins by HTRF assay
6
Total Activities
6
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

Optimization of 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidines to generate a highly selective PI3Kδ inhibitor.
Hamajima T, Takahashi F, Kato K, Sugano Y, Yamaki S, Suzuki D, Moritomo A, Kubo S, Nakamura K, Yamagami K, Yokoo K, Fukahori H.
Bioorg Med Chem (2019) 27 : 1056 -1064
PubMed 30755348 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.16 5.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4554894 1 5.27
CHEMBL4467692 1 5.05
CHEMBL4530810 1 -
CHEMBL4453747 1 -
CHEMBL4514389 1 -
CHEMBL4528263 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4554894 IC50 = 5400.0 nM 5.27
CHEMBL4467692 IC50 = 8900.0 nM 5.05
CHEMBL4530810 IC50 > 10000.0 nM -
CHEMBL4453747 IC50 > 10000.0 nM -
CHEMBL4514389 IC50 > 10000.0 nM -
CHEMBL4528263 IC50 > 10000.0 nM -