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Assay Detail

CHEMBL5504662

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

Binding
Inhibition of recombinant human PI3Kbeta 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
Ki 27 6.91 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5555403 1 8.30
CHEMBL5558448 1 7.70
CHEMBL5542223 1 7.70
CHEMBL5543016 1 7.50
CHEMBL5527852 1 7.30
CHEMBL5558076 1 7.30
CHEMBL5559126 1 7.30
CHEMBL5518064 1 7.20
CHEMBL5557135 1 7.10
CHEMBL5555605 1 7.00
CHEMBL5531964 1 7.00
CHEMBL5517938 1 7.00
CHEMBL5559413 1 7.00
CHEMBL5512440 1 6.60
CHEMBL5505905 1 6.60
CHEMBL5556699 1 6.50
CHEMBL5555181 1 6.50
CHEMBL5542678 1 6.40
CHEMBL5517797 1 6.20
CHEMBL5517641 1 6.00
CHEMBL5505948 1 6.00
CHEMBL5512540 1 5.90
CHEMBL3919512 1 -
CHEMBL5555574 1 -
CHEMBL5559112 1 -
CHEMBL5532174 1 -
CHEMBL5542654 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5555403 Ki = 5.012 nM 8.30
CHEMBL5558448 Ki = 19.95 nM 7.70
CHEMBL5542223 Ki = 19.95 nM 7.70
CHEMBL5543016 Ki = 31.62 nM 7.50
CHEMBL5527852 Ki = 50.12 nM 7.30
CHEMBL5558076 Ki = 50.12 nM 7.30
CHEMBL5559126 Ki = 50.12 nM 7.30
CHEMBL5518064 Ki = 63.1 nM 7.20
CHEMBL5557135 Ki = 79.43 nM 7.10
CHEMBL5555605 Ki = 100.0 nM 7.00
CHEMBL5531964 Ki = 100.0 nM 7.00
CHEMBL5517938 Ki = 100.0 nM 7.00
CHEMBL5559413 Ki = 100.0 nM 7.00
CHEMBL5512440 Ki = 251.19 nM 6.60
CHEMBL5505905 Ki = 251.19 nM 6.60
CHEMBL5556699 Ki = 316.23 nM 6.50
CHEMBL5555181 Ki = 316.23 nM 6.50
CHEMBL5542678 Ki = 398.11 nM 6.40
CHEMBL5517797 Ki = 630.96 nM 6.20
CHEMBL5517641 Ki = 1000.0 nM 6.00
CHEMBL5505948 Ki = 1000.0 nM 6.00
CHEMBL5512540 Ki = 1258.93 nM 5.90
CHEMBL3919512 Ki > 25118.86 nM -
CHEMBL5555574 Ki > 10000.0 nM -
CHEMBL5559112 Ki > 10000.0 nM -
CHEMBL5532174 Ki > 10000.0 nM -
CHEMBL5542654 Ki > 10000.0 nM -