Assay Detail
Binding
CHEMBL5657142
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr in presence of ATP by HTRF assay
17
Total Activities
17
Compounds Tested
1
Activity Types
2
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
Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 8.08 | 10.40 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | MONDO:0004992 |
| EFO_TERM | EFO_TERM | - | — | cancer |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1236962 | OMIPALISIB | 2.0 | 1 | 10.40 |
| CHEMBL5661926 | — | — | 1 | 10.00 |
| CHEMBL5661866 | — | — | 1 | 9.00 |
| CHEMBL5661869 | — | — | 1 | 9.00 |
| CHEMBL3544966 | GSK-1059615 | 1.0 | 1 | 8.70 |
| CHEMBL428496 | WORTMANNIN | — | 1 | 8.62 |
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | 8.22 |
| CHEMBL1234114 | — | — | 1 | 8.15 |
| CHEMBL586702 | ZSTK-474 | 2.0 | 1 | 8.13 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 8.05 |
| CHEMBL5571102 | — | — | 1 | 8.00 |
| CHEMBL573339 | PI-103 | — | 1 | 7.92 |
| CHEMBL3349370 | — | — | 1 | 7.41 |
| CHEMBL5661876 | — | — | 1 | 7.14 |
| CHEMBL5661894 | — | — | 1 | 6.58 |
| CHEMBL98350 | LY-294002 | -1.0 | 1 | 6.33 |
| CHEMBL5661923 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1236962 | OMIPALISIB | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL5661926 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5661866 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5661869 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3544966 | GSK-1059615 | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL428496 | WORTMANNIN | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL1879463 | DACTOLISIB | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1234114 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL586702 | ZSTK-474 | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL521851 | PICTILISIB | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5571102 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL573339 | PI-103 | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3349370 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5661876 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL5661894 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL98350 | LY-294002 | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5661923 | — | IC50 | = | 1800.0 | nM | 5.75 |