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Assay Detail

CHEMBL4832705

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

Binding
Inhibition of PI3Kalpha (unknown origin) using L-alpha-phosphatidylinositol as substrate incubated for 30 to 60 mins in presence of ATP by Kinase Glo luminescence kinase assay
26
Total Activities
26
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 Toxicological Profiling of Aminopyridines as Orally Bioavailable Selective Inhibitors of PI3-Kinase γ.
Bellenie BR, Hall E, Bruce I, Spendiff M, Culshaw A, McDonald S, Ambarkhane A, Chinn C, Thomas M, Rosner E, Bracher M, Nicklin P, Marshall S, Coote J, Cullen E, Tessier C, Wuersch K, Lal A, Wallis G, Hollingworth GJ, Neef J.
J Med Chem (2021) 64 : 12304 -12321
PubMed 34384024 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.40 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4864109 1 7.47
CHEMBL4855904 1 7.46
CHEMBL4867254 1 7.43
CHEMBL4857826 1 7.26
CHEMBL4863328 1 7.20
CHEMBL4866794 1 7.03
CHEMBL4859017 1 6.96
CHEMBL4850655 1 6.77
CHEMBL4878811 1 6.70
CHEMBL4848126 1 6.54
CHEMBL4878615 1 6.52
CHEMBL4868011 1 6.35
CHEMBL4857001 1 6.34
CHEMBL4849042 1 6.28
CHEMBL4859466 1 6.24
CHEMBL4857607 1 6.21
CHEMBL4854845 1 6.19
CHEMBL4876331 1 6.06
CHEMBL4878721 1 6.06
CHEMBL4861144 1 6.05
CHEMBL4846278 1 6.02
CHEMBL4854857 1 5.80
CHEMBL4873556 1 5.77
CHEMBL2071342 1 5.52
CHEMBL4866311 1 5.12
CHEMBL4855444 1 5.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4864109 IC50 = 34.0 nM 7.47
CHEMBL4855904 IC50 = 35.0 nM 7.46
CHEMBL4867254 IC50 = 37.0 nM 7.43
CHEMBL4857826 IC50 = 55.0 nM 7.26
CHEMBL4863328 IC50 = 63.0 nM 7.20
CHEMBL4866794 IC50 = 94.0 nM 7.03
CHEMBL4859017 IC50 = 110.0 nM 6.96
CHEMBL4850655 IC50 = 169.0 nM 6.77
CHEMBL4878811 IC50 = 200.0 nM 6.70
CHEMBL4848126 IC50 = 290.0 nM 6.54
CHEMBL4878615 IC50 = 300.0 nM 6.52
CHEMBL4868011 IC50 = 450.0 nM 6.35
CHEMBL4857001 IC50 = 460.0 nM 6.34
CHEMBL4849042 IC50 = 520.0 nM 6.28
CHEMBL4859466 IC50 = 570.0 nM 6.24
CHEMBL4857607 IC50 = 620.0 nM 6.21
CHEMBL4854845 IC50 = 640.0 nM 6.19
CHEMBL4876331 IC50 = 880.0 nM 6.06
CHEMBL4878721 IC50 = 880.0 nM 6.06
CHEMBL4861144 IC50 = 900.0 nM 6.05
CHEMBL4846278 IC50 = 950.0 nM 6.02
CHEMBL4854857 IC50 = 1600.0 nM 5.80
CHEMBL4873556 IC50 = 1700.0 nM 5.77
CHEMBL2071342 IC50 = 3030.0 nM 5.52
CHEMBL4866311 IC50 = 7500.0 nM 5.12
CHEMBL4855444 IC50 = 9400.0 nM 5.03