Assay Detail
Binding
CHEMBL5738846
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PI3-Kinase HTRF Assay: PI3 Kinase α, β, γ or δ activity was assayed using the PI3 Kinase HTRF® assay kit (catalogue No. 33-016) purchased from Millipore Corporation. Purified recombinant PI3Kα (catalogue No. 14-602-K), PI3Kβ (catalogue No. 14-603-K), PI3Kγ (catalogue No. 14-558-K), and PI3Kδ (catalogue No. 14-604-K) were obtained from Millipore Corporation. Purified recombinant PI3K enzyme was used to catalyze the phosphorylation of phosphatidylinositol 4,5-bisphosphate (PIP2 at 10 μM) to phosphatidylinositol 3,4,5-trisphosphate (PIP3) in the presence of 10 μM ATP. The assay was carried out in 384-well format and detected using a Perkin Elmer EnVision Xcite Multilabel Reader. Emission ratios were converted into percent inhibitions and imported into GraphPad Prism software. The concentration necessary to achieve inhibition of enzyme activity by 50% (IC50) was calculated using concentrations ranging from 20 μM to 0.1 nM (12-point curve).
330
Total Activities
108
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
Heterocyclic compounds and uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 110 | 5.70 | 5.70 |
| kon | 110 | - | - |
| k_off | 110 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5949875 | — | — | 3 | 5.70 |
| CHEMBL3914602 | — | — | 3 | 5.70 |
| CHEMBL5919053 | — | — | 3 | 5.70 |
| CHEMBL6050868 | — | — | 3 | 5.70 |
| CHEMBL5900412 | — | — | 3 | 5.70 |
| CHEMBL3955769 | — | — | 3 | 5.70 |
| CHEMBL6033616 | — | — | 3 | 5.70 |
| CHEMBL5871827 | — | — | 3 | 5.70 |
| CHEMBL5901746 | — | — | 3 | 5.70 |
| CHEMBL5882857 | — | — | 3 | 5.70 |
| CHEMBL5886457 | — | — | 3 | 5.70 |
| CHEMBL5992887 | — | — | 3 | 5.70 |
| CHEMBL5900338 | — | — | 3 | 5.70 |
| CHEMBL5953253 | — | — | 3 | 5.70 |
| CHEMBL3928146 | — | — | 3 | 5.70 |
| CHEMBL5797332 | — | — | 6 | 5.70 |
| CHEMBL5785381 | — | — | 3 | 5.70 |
| CHEMBL5867632 | — | — | 3 | 5.70 |
| CHEMBL5990604 | — | — | 3 | 5.70 |
| CHEMBL5754601 | — | — | 3 | 5.70 |
| CHEMBL5934604 | — | — | 3 | 5.70 |
| CHEMBL6020506 | — | — | 3 | 5.70 |
| CHEMBL5915872 | — | — | 3 | 5.70 |
| CHEMBL5798011 | — | — | 3 | 5.70 |
| CHEMBL5790749 | — | — | 3 | 5.70 |
| CHEMBL5925877 | — | — | 3 | 5.70 |
| CHEMBL3966879 | — | — | 3 | 5.70 |
| CHEMBL6025507 | — | — | 3 | 5.70 |
| CHEMBL5766735 | — | — | 3 | 5.70 |
| CHEMBL6013643 | — | — | 3 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5829946 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL6007856 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3921445 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5791000 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5970890 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5796536 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5895414 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5887753 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5947378 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5806739 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5900898 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5748222 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5762937 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5754944 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5796587 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3895629 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL6048456 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5935134 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5858536 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5838632 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5979518 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5743380 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5933124 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5991752 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL6021741 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3893430 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5754507 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL6033616 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3955769 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5799818 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5900412 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL6052455 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL6050868 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5919053 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5866941 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3914602 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5764062 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5760298 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5980508 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5936480 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5996366 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5977085 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL6011851 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL6011851 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5924108 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5748405 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5971164 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL6053354 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5770638 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5776869 | — | IC50 | = | 2000.0 | nM | 5.70 |