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Assay Detail

CHEMBL2343995

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

Binding
Inhibition of PI3K in human BT20 cells assessed as inhibition of AKT Ser473 phosphorylation
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BT-20
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design.
Cheng H, Li C, Bailey S, Baxi SM, Goulet L, Guo L, Hoffman J, Jiang Y, Johnson TO, Johnson TW, Knighton DR, Li J, Liu KK, Liu Z, Marx MA, Walls M, Wells PA, Yin MJ, Zhu J, Zientek M.
ACS Med Chem Lett (2013) 4 : 91 -97
PubMed 24900568 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.66 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2331664 1 8.04
CHEMBL2331659 1 8.02
CHEMBL2331666 1 7.96
CHEMBL2331668 1 7.94
CHEMBL2331658 1 7.81
CHEMBL2331661 1 7.78
CHEMBL2331663 1 7.76
CHEMBL2331665 1 7.65
CHEMBL2331669 1 7.55
CHEMBL2331667 1 7.50
CHEMBL2331662 1 7.50
CHEMBL2331660 1 7.24
CHEMBL2331657 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2331664 IC50 = 9.1 nM 8.04
CHEMBL2331659 IC50 = 9.52 nM 8.02
CHEMBL2331666 IC50 = 11.1 nM 7.96
CHEMBL2331668 IC50 = 11.6 nM 7.94
CHEMBL2331658 IC50 = 15.4 nM 7.81
CHEMBL2331661 IC50 = 16.8 nM 7.78
CHEMBL2331663 IC50 = 17.3 nM 7.76
CHEMBL2331665 IC50 = 22.5 nM 7.65
CHEMBL2331669 IC50 = 28.3 nM 7.55
CHEMBL2331667 IC50 = 31.5 nM 7.50
CHEMBL2331662 IC50 = 31.6 nM 7.50
CHEMBL2331660 IC50 = 57.9 nM 7.24
CHEMBL2331657 IC50 = 144.0 nM 6.84