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Assay Detail

CHEMBL5504663

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

Binding
Inhibition of recombinant human PI3Kalpha using L-alpha-phosphatidylinositol sodium salt and L-alpha-phosphatidyl-L-serine as substrate incubated for 60 mins in presence of ATP by ADP-glo kinase assay
27
Total Activities
27
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

Discovery and Optimization of Pyridazinones as PI3Kδ Selective Inhibitors for Administration by Inhalation.
Bruno P, Micoli A, Corsi M, Pala D, Guariento S, Fiorelli C, Ronchi P, Fioni A, Gallo PM, Marenghi G, Bertolini S, Capacchi S, Mileo V, Biagetti M, Capelli AM.
J Med Chem (2024) 67 : 11103 -11124
PubMed 38907711 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.35 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5558448 1 7.30
CHEMBL5531964 1 6.80
CHEMBL5555605 1 6.70
CHEMBL5555403 1 6.70
CHEMBL5557135 1 6.70
CHEMBL5527852 1 6.60
CHEMBL5512440 1 6.30
CHEMBL5518064 1 6.20
CHEMBL5542678 1 6.20
CHEMBL5542223 1 6.10
CHEMBL5543016 1 6.00
CHEMBL5558076 1 6.00
CHEMBL5517938 1 6.00
CHEMBL5559126 1 5.90
CHEMBL5559413 1 5.80
CHEMBL3919512 1 -
CHEMBL5517641 1 -
CHEMBL5517797 1 -
CHEMBL5555574 1 -
CHEMBL5559112 1 -
CHEMBL5512540 1 -
CHEMBL5505948 1 -
CHEMBL5556699 1 -
CHEMBL5505905 1 -
CHEMBL5555181 1 -
CHEMBL5532174 1 -
CHEMBL5542654 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5558448 IC50 = 50.12 nM 7.30
CHEMBL5531964 IC50 = 158.49 nM 6.80
CHEMBL5555605 IC50 = 199.53 nM 6.70
CHEMBL5555403 IC50 = 199.53 nM 6.70
CHEMBL5557135 IC50 = 199.53 nM 6.70
CHEMBL5527852 IC50 = 251.19 nM 6.60
CHEMBL5512440 IC50 = 501.19 nM 6.30
CHEMBL5518064 IC50 = 630.96 nM 6.20
CHEMBL5542678 IC50 = 630.96 nM 6.20
CHEMBL5542223 IC50 = 794.33 nM 6.10
CHEMBL5543016 IC50 = 1000.0 nM 6.00
CHEMBL5558076 IC50 = 1000.0 nM 6.00
CHEMBL5517938 IC50 = 1000.0 nM 6.00
CHEMBL5559126 IC50 = 1258.93 nM 5.90
CHEMBL5559413 IC50 = 1584.89 nM 5.80
CHEMBL3919512 IC50 > 25118.86 nM -
CHEMBL5517641 IC50 > 10000.0 nM -
CHEMBL5517797 IC50 > 10000.0 nM -
CHEMBL5555574 IC50 > 10000.0 nM -
CHEMBL5559112 IC50 > 10000.0 nM -
CHEMBL5512540 IC50 > 25118.86 nM -
CHEMBL5505948 IC50 > 10000.0 nM -
CHEMBL5556699 IC50 > 10000.0 nM -
CHEMBL5505905 IC50 > 10000.0 nM -
CHEMBL5555181 IC50 > 25118.86 nM -
CHEMBL5532174 IC50 > 10000.0 nM -
CHEMBL5542654 IC50 > 10000.0 nM -