Assay Detail
Binding
CHEMBL3706341
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Alphascreen Assay: The PI3K AlphaScreen assay (PerkinElmer, Waltham, Mass.) measures the activity of a panel of four phosphoinositide 3-kinases: PI3Kalpha, PI3Kbeta, PI3Kgamma, and PI3Kdelta. Each of these enzymes phosphorylates the 3'-hydroxyl group on phosphatidylinositiol (4,5)-bisphosphate (PIP2) to produce phosphatidylinositol (3,4,5)-trisphosphate (PIP3). This phosphorylation activity is measured using a GST-tagged PIP3 binding protein (Echelon Biosciences, Salt Lake City, Utah), an anti-GST-tagged Acceptor bead, and streptavidin-Donor bead. The interaction of biotinylated-PIP3 analog (IP4) and the PIP3 binding protein brings both Acceptor and Donor beads together producing, upon excitation of the Donor beads at 680 nm, a singlet oxygen species leading to the luminescent AlphaScreen signal. When PIP3 is produced via phosphorylation of PIP2 by a PI3K, PIP3 competes with biotinylated-PIP3 analog (IP4) for binding to the PIP3 binding protein.
345
Total Activities
343
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
Inhibitors of PI3 kinase and/or mTOR
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 345 | 7.42 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2170088 | — | — | 1 | 9.00 |
| CHEMBL3646588 | — | — | 1 | 9.00 |
| CHEMBL3646596 | — | — | 1 | 9.00 |
| CHEMBL3646485 | — | — | 1 | 9.00 |
| CHEMBL3646632 | — | — | 1 | 8.70 |
| CHEMBL2206921 | — | — | 1 | 8.70 |
| CHEMBL2206907 | — | — | 1 | 8.70 |
| CHEMBL2170082 | — | — | 1 | 8.70 |
| CHEMBL3646601 | — | — | 3 | 8.70 |
| CHEMBL3646595 | — | — | 1 | 8.70 |
| CHEMBL2170083 | — | — | 1 | 8.70 |
| CHEMBL3646517 | — | — | 1 | 8.70 |
| CHEMBL3646481 | — | — | 1 | 8.70 |
| CHEMBL3646480 | — | — | 1 | 8.70 |
| CHEMBL2165007 | — | — | 1 | 8.70 |
| CHEMBL3646449 | — | — | 1 | 8.70 |
| CHEMBL2170090 | — | — | 1 | 8.70 |
| CHEMBL3646586 | — | — | 1 | 8.52 |
| CHEMBL3646618 | — | — | 1 | 8.52 |
| CHEMBL3646575 | — | — | 1 | 8.52 |
| CHEMBL2170089 | — | — | 1 | 8.52 |
| CHEMBL3646450 | — | — | 1 | 8.52 |
| CHEMBL3643923 | — | — | 1 | 8.40 |
| CHEMBL2170099 | — | — | 1 | 8.40 |
| CHEMBL2170081 | — | — | 1 | 8.40 |
| CHEMBL3646518 | — | — | 1 | 8.40 |
| CHEMBL3646543 | — | — | 1 | 8.40 |
| CHEMBL3646557 | — | — | 1 | 8.40 |
| CHEMBL3357868 | — | — | 1 | 8.40 |
| CHEMBL3646584 | — | — | 1 | 8.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3646485 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3646588 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3646596 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2170088 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3646480 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3646595 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2165007 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3646481 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3646601 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3646632 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2170090 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3646449 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2170083 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2206921 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2206907 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3646517 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2170082 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3646575 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3646586 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3646450 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3646618 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2170089 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3357869 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3646584 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2170099 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2206908 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2170081 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3643923 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3357868 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3646557 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3646518 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3646543 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3646619 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3646634 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3649464 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3646478 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2206912 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3646484 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2165030 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3646623 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3646622 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2206906 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3646617 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3646502 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL3646535 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL3646507 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL3649478 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL3646479 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL3646612 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL3646573 | — | Ki | = | 6.0 | nM | 8.22 |