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Assay Detail

CHEMBL5139014

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

Binding
Inhibition of wild type PI3K in human HCC1143 cells assessed as reduction in phosphorylation of AKT at Ser473 residue by Western blot analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HCC1143
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.
Fairhurst RA, Furet P, Imbach-Weese P, Stauffer F, Rueeger H, McCarthy C, Ripoche S, Oswald S, Arnaud B, Jary A, Maira M, Schnell C, Guthy DA, Wartmann M, Kiffe M, Desrayaud S, Blasco F, Widmer T, Seiler F, Gutmann S, Knapp M, Caravatti G.
J Med Chem (2022) 65 : 8345 -8379
PubMed 35500094 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.58 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5203121 1 7.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5203121 IC50 = 26.0 nM 7.58