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Assay Detail

CHEMBL2065221

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

Binding
Inhibition of PI3Kbeta by high throughput chemoproteomics binding assay
9
Total Activities
9
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

SAR studies around a series of triazolopyridines as potent and selective PI3Kγ inhibitors.
Bell K, Sunose M, Ellard K, Cansfield A, Taylor J, Miller W, Ramsden N, Bergamini G, Neubauer G.
Bioorg Med Chem Lett (2012) 22 : 5257 -5263
PubMed 22819766 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.92 5.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2064571 1 5.90
CHEMBL2064479 1 4.70
CHEMBL2064514 1 4.70
CHEMBL2064570 1 4.70
CHEMBL2064567 1 4.60
CHEMBL2064478 1 -
CHEMBL2064566 1 -
CHEMBL2064569 1 -
CHEMBL2064572 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2064571 IC50 = 1258.93 nM 5.90
CHEMBL2064479 IC50 = 19952.62 nM 4.70
CHEMBL2064514 IC50 = 19952.62 nM 4.70
CHEMBL2064570 IC50 = 19952.62 nM 4.70
CHEMBL2064567 IC50 = 25118.86 nM 4.60
CHEMBL2064478 IC50 > 100000.0 nM -
CHEMBL2064566 IC50 = 199526.23 nM -
CHEMBL2064569 IC50 > 100000.0 nM -
CHEMBL2064572 IC50 > 100000.0 nM -