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Assay Detail

CHEMBL5116812

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

Binding
Inhibition of PI3Kbeta (unknown origin) incubated for 60 mins in the presence of ATP by Kinase-Glo luminescence assay
20
Total Activities
20
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

Synthesis and biological evaluation of 4H-benzo[e][1,3]oxazin-4-ones analogues of TGX-221 as inhibitors of PI3Kβ.
Mohammed EUR, Porter ZJ, Jennings IG, Al-Rawi JMA, Thompson PE, Angove MJ.
Bioorg Med Chem (2022) 69 : 116832 -116832
PubMed 35752141 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.50 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5173094 1 7.31
CHEMBL5204332 1 7.20
CHEMBL1972466 1 7.19
CHEMBL5176111 1 7.16
CHEMBL5175866 1 7.14
CHEMBL5175395 1 6.87
CHEMBL5191049 1 6.82
CHEMBL5202433 1 6.64
CHEMBL5201399 1 6.62
CHEMBL5203337 1 6.57
CHEMBL5208867 1 6.55
CHEMBL5207448 1 5.91
CHEMBL5183615 1 5.84
CHEMBL5193998 1 5.73
CHEMBL5188598 1 5.61
CHEMBL5174445 1 4.90
CHEMBL5171155 1 -
CHEMBL5172240 1 -
CHEMBL5204523 1 -
CHEMBL5175510 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5173094 IC50 = 49.2 nM 7.31
CHEMBL5204332 IC50 = 62.7 nM 7.20
CHEMBL1972466 IC50 = 65.0 nM 7.19
CHEMBL5176111 IC50 = 70.0 nM 7.16
CHEMBL5175866 IC50 = 72.7 nM 7.14
CHEMBL5175395 IC50 = 136.0 nM 6.87
CHEMBL5191049 IC50 = 152.0 nM 6.82
CHEMBL5202433 IC50 = 227.0 nM 6.64
CHEMBL5201399 IC50 = 240.0 nM 6.62
CHEMBL5203337 IC50 = 272.0 nM 6.57
CHEMBL5208867 IC50 = 281.0 nM 6.55
CHEMBL5207448 IC50 = 1219.0 nM 5.91
CHEMBL5183615 IC50 = 1428.0 nM 5.84
CHEMBL5193998 IC50 = 1880.0 nM 5.73
CHEMBL5188598 IC50 = 2435.0 nM 5.61
CHEMBL5174445 IC50 = 12600.0 nM 4.90
CHEMBL5171155 IC50 > 20000.0 nM -
CHEMBL5172240 IC50 > 20000.0 nM -
CHEMBL5204523 IC50 > 20000.0 nM -
CHEMBL5175510 IC50 > 20000.0 nM -