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Assay Detail

CHEMBL3376673

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

Binding
Inhibition of human class 3 PI3K by non-radiometric ADP-Glo assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.
Mountford SJ, Zheng Z, Sundaram K, Jennings IG, Hamilton JR, Thompson PE.
ACS Med Chem Lett (2015) 6 : 3 -6
PubMed 25589915 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.84 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1229535 1 6.50
CHEMBL3354566 1 6.35
CHEMBL1241857 1 6.08
CHEMBL573339 PI-103 1 5.64
CHEMBL98350 LY-294002 -1.0 1 5.46
CHEMBL3218571 1 5.00
CHEMBL3354564 1 -
CHEMBL3354565 1 -
CHEMBL586702 ZSTK-474 2.0 1 -
CHEMBL521851 PICTILISIB 2.0 1 -
CHEMBL3218581 1 -
CHEMBL2216870 IDELALISIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1229535 IC50 = 320.0 nM 6.50
CHEMBL3354566 IC50 = 450.0 nM 6.35
CHEMBL1241857 IC50 = 830.0 nM 6.08
CHEMBL573339 PI-103 IC50 = 2300.0 nM 5.64
CHEMBL98350 LY-294002 IC50 = 3500.0 nM 5.46
CHEMBL3218571 IC50 = 10000.0 nM 5.00
CHEMBL3354564 IC50 - -
CHEMBL3354565 IC50 - -
CHEMBL586702 ZSTK-474 IC50 > 100000.0 nM -
CHEMBL521851 PICTILISIB IC50 > 100000.0 nM -
CHEMBL3218581 IC50 > 5000.0 nM -
CHEMBL2216870 IDELALISIB IC50 = 978000.0 nM -