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Assay Detail

CHEMBL3591915

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

Binding
Inhibition of His-tagged p110gamma (unknown origin) expressed in Sf9/Baculovirus system using [gamma-33P]ATP by scintillation proximity assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Design, synthesis and biological evaluation of novel condensed pyrrolo[1,2-c]pyrimidines featuring morpholine moiety as PI3Kα inhibitors.
Ibrahim MA, Abou-Seri SM, Hanna MM, Abdalla MM, El Sayed NA.
Eur J Med Chem (2015) 99 : 1 -13
PubMed 26037808 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 4.93 5.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3589372 1 5.87
CHEMBL3589370 1 5.34
CHEMBL3589371 1 5.24
CHEMBL3589324 1 5.12
CHEMBL3589377 1 4.90
CHEMBL3589379 1 4.81
CHEMBL3589376 1 4.73
CHEMBL3589375 1 4.63
CHEMBL3589378 1 4.57
CHEMBL3589320 1 4.04
CHEMBL3589321 1 -
CHEMBL3589322 1 -
CHEMBL3589323 1 -
CHEMBL3589373 1 -
CHEMBL3589374 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3589372 IC50 = 1340.0 nM 5.87
CHEMBL3589370 IC50 = 4560.0 nM 5.34
CHEMBL3589371 IC50 = 5780.0 nM 5.24
CHEMBL3589324 IC50 = 7640.0 nM 5.12
CHEMBL3589377 IC50 = 12570.0 nM 4.90
CHEMBL3589379 IC50 = 15560.0 nM 4.81
CHEMBL3589376 IC50 = 18480.0 nM 4.73
CHEMBL3589375 IC50 = 23640.0 nM 4.63
CHEMBL3589378 IC50 = 26870.0 nM 4.57
CHEMBL3589320 IC50 = 91560.0 nM 4.04
CHEMBL3589321 IC50 = 125800.0 nM -
CHEMBL3589322 IC50 = 465500.0 nM -
CHEMBL3589323 IC50 = 345900.0 nM -
CHEMBL3589373 IC50 = 781500.0 nM -
CHEMBL3589374 IC50 = 967700.0 nM -