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Assay Detail

CHEMBL3406098

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

Binding
Inhibition of PI3K (unknown origin) by TR-FRET assay
4
Total Activities
4
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

Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor.
Van Dort ME, Galbán S, Wang H, Sebolt-Leopold J, Whitehead C, Hong H, Rehemtulla A, Ross BD.
Bioorg Med Chem (2015) 23 : 1386 -1394
PubMed 25766633 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.88 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3400288 1 7.00
CHEMBL3400291 1 6.76
CHEMBL3400290 1 -
CHEMBL3400289 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3400288 IC50 = 100.0 nM 7.00
CHEMBL3400291 IC50 = 172.0 nM 6.76
CHEMBL3400290 IC50 < 100.0 nM -
CHEMBL3400289 IC50 > 1000.0 nM -