Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3706092

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

Binding
Biochemical Assay: Compounds of the present invention were evaluated for potency against PI3-Kα using an in vitro kinase assay. PI3-Kα activity is measured in vitro by determining the level of phosphorylation of the substrate PI(4,5)P2. The formation of product PI(3,4,5)P3 is monitored by binding to the Grip1 PH domain in a ligand displacement fluorescence polarization (FP) assay, in which the TAMRA-labeled PI(3,4,5)P3 complexed with Grip1 PH domain is displaced by PI(3,4,5)P3 formed in the PI3-Kα reaction resulting in a decrease in FP signal.
ChEMBL ↗
174
Total Activities
173
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

Target

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-methylpyridopyrimidinone compounds
(2014)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 174 7.82 9.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3648918 — — 1 9.32
CHEMBL2375957 — — 1 9.16
CHEMBL3648932 — — 1 9.14
CHEMBL3648913 — — 1 9.12
CHEMBL3652248 — — 1 9.10
CHEMBL3648924 — — 1 9.01
CHEMBL3648930 — — 1 9.00
CHEMBL3218401 — — 1 8.99
CHEMBL3648966 — — 1 8.96
CHEMBL3648942 — — 1 8.92
CHEMBL3648944 — — 1 8.92
CHEMBL3648937 — — 1 8.89
CHEMBL3652250 — — 1 8.89
CHEMBL3649018 — — 1 8.85
CHEMBL3652257 — — 1 8.84
CHEMBL3648910 — — 1 8.80
CHEMBL2375963 — — 1 8.80
CHEMBL3652249 — — 1 8.80
CHEMBL3648980 — — 1 8.80
CHEMBL3648957 — — 1 8.80
CHEMBL3648950 — — 1 8.80
CHEMBL3649010 — — 1 8.77
CHEMBL3648922 — — 1 8.75
CHEMBL3652247 — — 1 8.74
CHEMBL3648974 — — 1 8.70
CHEMBL3649011 — — 1 8.70
CHEMBL3652273 — — 1 8.67
CHEMBL3649019 — — 1 8.66
CHEMBL3652256 — — 1 8.66
CHEMBL3648975 — — 1 8.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3648918 — IC50 = 0.48 nM 9.32
CHEMBL2375957 — IC50 = 0.686 nM 9.16
CHEMBL3648932 — IC50 = 0.731 nM 9.14
CHEMBL3648913 — IC50 = 0.75 nM 9.12
CHEMBL3652248 — IC50 = 0.788 nM 9.10
CHEMBL3648924 — IC50 = 0.989 nM 9.01
CHEMBL3648930 — IC50 = 1.01 nM 9.00
CHEMBL3218401 — IC50 = 1.03 nM 8.99
CHEMBL3648966 — IC50 = 1.1 nM 8.96
CHEMBL3648944 — IC50 = 1.2 nM 8.92
CHEMBL3648942 — IC50 = 1.2 nM 8.92
CHEMBL3648937 — IC50 = 1.3 nM 8.89
CHEMBL3652250 — IC50 = 1.3 nM 8.89
CHEMBL3649018 — IC50 = 1.43 nM 8.85
CHEMBL3652257 — IC50 = 1.44 nM 8.84
CHEMBL3648910 — IC50 = 1.57 nM 8.80
CHEMBL3648957 — IC50 = 1.6 nM 8.80
CHEMBL3648980 — IC50 = 1.6 nM 8.80
CHEMBL3648950 — IC50 = 1.6 nM 8.80
CHEMBL2375963 — IC50 = 1.58 nM 8.80
CHEMBL3652249 — IC50 = 1.59 nM 8.80
CHEMBL3649010 — IC50 = 1.7 nM 8.77
CHEMBL3648922 — IC50 = 1.77 nM 8.75
CHEMBL3652247 — IC50 = 1.8 nM 8.74
CHEMBL3649011 — IC50 = 2.0 nM 8.70
CHEMBL3648974 — IC50 = 2.0 nM 8.70
CHEMBL3652273 — IC50 = 2.14 nM 8.67
CHEMBL3652256 — IC50 = 2.2 nM 8.66
CHEMBL3649019 — IC50 = 2.2 nM 8.66
CHEMBL3648975 — IC50 = 2.3 nM 8.64
CHEMBL3652246 — IC50 = 2.3 nM 8.64
CHEMBL3648955 — IC50 = 2.4 nM 8.62
CHEMBL3652263 — IC50 = 2.6 nM 8.59
CHEMBL3648964 — IC50 = 2.7 nM 8.57
CHEMBL3648984 — IC50 = 2.8 nM 8.55
CHEMBL3652251 — IC50 = 2.9 nM 8.54
CHEMBL2057725 — IC50 = 2.96 nM 8.53
CHEMBL3648923 — IC50 = 3.08 nM 8.51
CHEMBL3649012 — IC50 = 3.1 nM 8.51
CHEMBL3652270 — IC50 = 3.11 nM 8.51
CHEMBL2375961 — IC50 = 3.62 nM 8.44
CHEMBL3648971 — IC50 = 3.7 nM 8.43
CHEMBL3652252 — IC50 = 3.9 nM 8.41
CHEMBL2375964 — IC50 = 3.87 nM 8.41
CHEMBL3639478 — IC50 = 3.9 nM 8.41
CHEMBL3649016 — IC50 = 4.0 nM 8.40
CHEMBL2375956 — IC50 = 4.11 nM 8.39
CHEMBL3648953 — IC50 = 4.3 nM 8.37
CHEMBL3652245 — IC50 = 4.4 nM 8.36
CHEMBL2057736 — IC50 = 4.5 nM 8.35