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Assay Detail

CHEMBL5548922

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

Binding
Inhibition of PI3Kalpha (unknown origin) by ADP-glo plus luminescence assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Design, Synthesis, Formulation, and Bioevaluation of Trisubstituted Triazines as Highly Selective mTOR Inhibitors for the Treatment of Human Breast Cancer.
Sun Q, Chu Y, Zhang N, Chen R, Wang L, Wu J, Dong Y, Li H, Wang L, Tang L, Zhan C, Zhang JQ.
J Med Chem (2024) 67 : 7330 -7358
PubMed 38661655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.21 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL592445 GEDATOLISIB 3.0 1 8.22
CHEMBL5566586 1 7.99
CHEMBL5572519 1 7.92
CHEMBL5573179 1 7.82
CHEMBL5573982 1 7.66
CHEMBL5575213 1 7.42
CHEMBL5568655 1 7.36
CHEMBL5568982 1 7.34
CHEMBL5570389 1 7.34
CHEMBL5594441 1 7.19
CHEMBL5566351 1 7.12
CHEMBL5567165 1 6.95
CHEMBL5573450 1 6.79
CHEMBL5574430 1 6.63
CHEMBL5576014 1 6.61
CHEMBL5572006 1 6.59
CHEMBL5568986 1 6.45
CHEMBL5575995 1 6.42
CHEMBL5564044 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL592445 GEDATOLISIB IC50 = 6.0 nM 8.22
CHEMBL5566586 IC50 = 10.3 nM 7.99
CHEMBL5572519 IC50 = 12.1 nM 7.92
CHEMBL5573179 IC50 = 15.2 nM 7.82
CHEMBL5573982 IC50 = 21.8 nM 7.66
CHEMBL5575213 IC50 = 38.4 nM 7.42
CHEMBL5568655 IC50 = 44.0 nM 7.36
CHEMBL5568982 IC50 = 45.4 nM 7.34
CHEMBL5570389 IC50 = 45.4 nM 7.34
CHEMBL5594441 IC50 = 64.0 nM 7.19
CHEMBL5566351 IC50 = 75.4 nM 7.12
CHEMBL5567165 IC50 = 112.3 nM 6.95
CHEMBL5573450 IC50 = 163.0 nM 6.79
CHEMBL5574430 IC50 = 232.3 nM 6.63
CHEMBL5576014 IC50 = 246.0 nM 6.61
CHEMBL5572006 IC50 = 256.1 nM 6.59
CHEMBL5568986 IC50 = 354.0 nM 6.45
CHEMBL5575995 IC50 = 378.6 nM 6.42
CHEMBL5564044 IC50 > 10000.0 nM -