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Assay Detail

CHEMBL4716067

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

Binding
Inhibition of recombinant full length N-terminal polyHis-tagged PI3K p110beta/p85alpha (unknown origin) expressed in baculovirus infected Sf9 cells using PIP2 as substrate in presence of ATP incubated for 20 mins by Alphascreen assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors.
Shin Y,Suchomel J,Cardozo M,Duquette J,He X,Henne K,Hu YL,Kelly RC,McCarter J,McGee LR,Medina JC,Metz D,San Miguel T,Mohn D,Tran T,Vissinga C,Wong S,Wannberg S,Whittington DA,Whoriskey J,Yu G,Zalameda L,Zhang X,Cushing TD
J Med Chem (2016) 59 : 431 -447
PubMed 26652588 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.51 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4747926 1 7.52
CHEMBL2171931 1 7.11
CHEMBL4780867 1 6.35
CHEMBL4762294 1 6.29
CHEMBL4790186 1 6.27
CHEMBL2216895 1 5.97
CHEMBL4763849 1 5.75
CHEMBL4754382 1 5.63
CHEMBL4784595 1 5.45
CHEMBL4788529 1 5.45
CHEMBL4756034 1 5.26
CHEMBL4747799 1 5.23
CHEMBL4800111 1 5.05
CHEMBL4761860 1 4.98
CHEMBL4745140 1 4.85
CHEMBL4744888 1 4.74
CHEMBL4756545 1 4.73
CHEMBL4798019 1 4.61
CHEMBL4740720 1 4.52
CHEMBL4763925 1 4.50
CHEMBL4759169 1 -
CHEMBL4784596 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4747926 IC50 = 30.0 nM 7.52
CHEMBL2171931 IC50 = 78.6 nM 7.11
CHEMBL4780867 IC50 = 450.0 nM 6.35
CHEMBL4762294 IC50 = 510.0 nM 6.29
CHEMBL4790186 IC50 = 540.0 nM 6.27
CHEMBL2216895 IC50 = 1080.0 nM 5.97
CHEMBL4763849 IC50 = 1780.0 nM 5.75
CHEMBL4754382 IC50 = 2330.0 nM 5.63
CHEMBL4784595 IC50 = 3530.0 nM 5.45
CHEMBL4788529 IC50 = 3580.0 nM 5.45
CHEMBL4756034 IC50 = 5510.0 nM 5.26
CHEMBL4747799 IC50 = 5930.0 nM 5.23
CHEMBL4800111 IC50 = 8960.0 nM 5.05
CHEMBL4761860 IC50 = 10400.0 nM 4.98
CHEMBL4745140 IC50 = 14100.0 nM 4.85
CHEMBL4744888 IC50 = 18100.0 nM 4.74
CHEMBL4756545 IC50 = 18700.0 nM 4.73
CHEMBL4798019 IC50 = 24700.0 nM 4.61
CHEMBL4740720 IC50 = 30200.0 nM 4.52
CHEMBL4763925 IC50 = 31800.0 nM 4.50
CHEMBL4759169 IC50 > 125000.0 nM -
CHEMBL4784596 IC50 > 125000.0 nM -