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Assay Detail

CHEMBL3855737

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

Binding
Binding affinity to human recombinant full length N-terminal His6-tagged PI3K p110beta/p85alpha coexpressed in baculovirus infected Sf9 insect cells by equilibrium fluorescence titration analysis
1
Total Activities
1
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 of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.
Evans CA, Liu T, Lescarbeau A, Nair SJ, Grenier L, Pradeilles JA, Glenadel Q, Tibbitts T, Rowley AM, DiNitto JP, Brophy EE, O'Hearn EL, Ali JA, Winkler DG, Goldstein SI, O'Hearn P, Martin CM, Hoyt JG, Soglia JR, Cheung C, Pink MM, Proctor JL, Palombella VJ, Tremblay MR, Castro AC.
ACS Med Chem Lett (2016) 7 : 862 -867
PubMed 27660692 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 7.09 7.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3984425 EGANELISIB 2.0 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3984425 EGANELISIB Kd = 82.0 nM 7.09