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Assay Detail

CHEMBL5731104

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

Binding
p110alpha (alpha) PI3K Binding Assay: PI3K Binding assays are intended for determining the biochemical potency of small molecule PI3K inhibitors. The PI3K lipid kinase reaction is performed in the presence of PIP2:3PS lipid substrate (Promega #V1792) and ATP. Following the termination if the kinase reaction, turnover of ATP to ADP by the phosphorylation of the lipid substrate is detected using the Promega ADP-Glo¿ (Promega #V1792) assay.
ChEMBL ↗
645
Total Activities
210
Compounds Tested
3
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

Tricyclic PI3K inhibitor compounds and methods of use
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 215 8.37 10.68
kon 215 - -
k_off 215 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5953956 — — 3 10.68
CHEMBL5778370 — — 3 10.66
CHEMBL5750027 — — 3 10.62
CHEMBL5867381 — — 3 10.62
CHEMBL5855663 — — 3 10.59
CHEMBL5845982 — — 3 10.57
CHEMBL5925143 — — 3 10.52
CHEMBL5968296 — — 3 10.52
CHEMBL5940691 — — 6 10.51
CHEMBL5957586 — — 3 10.49
CHEMBL5930321 — — 3 10.49
CHEMBL5808916 — — 3 10.46
CHEMBL5860320 — — 6 10.41
CHEMBL5907169 — — 6 10.40
CHEMBL6007757 — — 3 10.35
CHEMBL5824088 — — 3 10.35
CHEMBL5764612 — — 3 10.31
CHEMBL5955267 — — 3 10.28
CHEMBL5776576 — — 3 10.25
CHEMBL5996160 — — 3 10.21
CHEMBL5831232 — — 3 10.21
CHEMBL5954637 — — 3 10.15
CHEMBL5909864 — — 3 10.15
CHEMBL6017610 — — 3 10.14
CHEMBL5795361 — — 6 10.12
CHEMBL6034108 — — 3 10.05
CHEMBL5829901 — — 3 10.02
CHEMBL5750909 — — 3 10.00
CHEMBL5769900 — — 3 9.98
CHEMBL5969740 — — 3 9.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5953956 — Ki = 0.021 nM 10.68
CHEMBL5778370 — Ki = 0.022 nM 10.66
CHEMBL5750027 — Ki = 0.024 nM 10.62
CHEMBL5867381 — Ki = 0.024 nM 10.62
CHEMBL5855663 — Ki = 0.026 nM 10.59
CHEMBL5845982 — Ki = 0.027 nM 10.57
CHEMBL5968296 — Ki = 0.03 nM 10.52
CHEMBL5925143 — Ki = 0.03 nM 10.52
CHEMBL5940691 — Ki = 0.031 nM 10.51
CHEMBL5957586 — Ki = 0.032 nM 10.49
CHEMBL5930321 — Ki = 0.032 nM 10.49
CHEMBL5808916 — Ki = 0.035 nM 10.46
CHEMBL5940691 — Ki = 0.038 nM 10.42
CHEMBL5860320 — Ki = 0.039 nM 10.41
CHEMBL5907169 — Ki = 0.04 nM 10.40
CHEMBL6007757 — Ki = 0.045 nM 10.35
CHEMBL5824088 — Ki = 0.045 nM 10.35
CHEMBL5764612 — Ki = 0.049 nM 10.31
CHEMBL5955267 — Ki = 0.053 nM 10.28
CHEMBL5776576 — Ki = 0.056 nM 10.25
CHEMBL5996160 — Ki = 0.062 nM 10.21
CHEMBL5831232 — Ki = 0.061 nM 10.21
CHEMBL5954637 — Ki = 0.071 nM 10.15
CHEMBL5909864 — Ki = 0.07 nM 10.15
CHEMBL6017610 — Ki = 0.072 nM 10.14
CHEMBL5795361 — Ki = 0.076 nM 10.12
CHEMBL6034108 — Ki = 0.09 nM 10.05
CHEMBL5829901 — Ki = 0.095 nM 10.02
CHEMBL5750909 — Ki = 0.1 nM 10.00
CHEMBL5860320 — Ki = 0.102 nM 9.99
CHEMBL5769900 — Ki = 0.104 nM 9.98
CHEMBL5969740 — Ki = 0.108 nM 9.97
CHEMBL5920405 — Ki = 0.113 nM 9.95
CHEMBL5976976 — Ki = 0.117 nM 9.93
CHEMBL6023867 — Ki = 0.119 nM 9.92
CHEMBL5756911 — Ki = 0.127 nM 9.90
CHEMBL5948863 — Ki = 0.143 nM 9.85
CHEMBL6063447 — Ki = 0.149 nM 9.83
CHEMBL5743605 — Ki = 0.15 nM 9.82
CHEMBL5832151 — Ki = 0.171 nM 9.77
CHEMBL6042068 — Ki = 0.191 nM 9.72
CHEMBL5894557 — Ki = 0.201 nM 9.70
CHEMBL5992179 — Ki = 0.209 nM 9.68
CHEMBL6041840 — Ki = 0.208 nM 9.68
CHEMBL6024283 — Ki = 0.214 nM 9.67
CHEMBL6011590 — Ki = 0.221 nM 9.66
CHEMBL5935411 — Ki = 0.242 nM 9.62
CHEMBL5989537 — Ki = 0.237 nM 9.62
CHEMBL5801484 — Ki = 0.261 nM 9.58
CHEMBL5833717 — Ki = 0.264 nM 9.58