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Assay Detail

CHEMBL4828199

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

ADMET
Inhibition of VPS34 in human HL-60 cell extract measured after 2 hrs by kinobeads based chemoproteomic competition binding assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type HL-60
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode.
Down K, Amour A, Anderson NA, Barton N, Campos S, Cannons EP, Clissold C, Convery MA, Coward JJ, Doyle K, Duempelfeld B, Edwards CD, Goldsmith MD, Krause J, Mallett DN, McGonagle GA, Patel VK, Rowedder J, Rowland P, Sharpe A, Sriskantharajah S, Thomas DA, Thomson DW, Uddin S, Hamblin JN, Hessel EM.
J Med Chem (2021) 64 : 13780 -13792
PubMed 34510892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.00 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4872328 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4872328 IC50 = 100.0 nM 7.00