Assay Detail
Binding
CHEMBL5153851
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) using PIP2:3PS as substrate in presence of ATP measured after 120 mins by ADP-Glo assay
36
Total Activities
36
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
Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 9.42 | 10.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5208487 | — | — | 1 | 10.59 |
| CHEMBL4650215 | INAVOLISIB | 4.0 | 1 | 10.47 |
| CHEMBL5199631 | — | — | 1 | 10.38 |
| CHEMBL5198796 | — | — | 1 | 10.37 |
| CHEMBL5186155 | — | — | 1 | 10.29 |
| CHEMBL5209168 | — | — | 1 | 10.28 |
| CHEMBL5196718 | — | — | 1 | 10.22 |
| CHEMBL5209048 | — | — | 1 | 10.21 |
| CHEMBL2387080 | TASELISIB | 3.0 | 1 | 10.05 |
| CHEMBL5205438 | — | — | 1 | 10.02 |
| CHEMBL5181348 | — | — | 1 | 10.01 |
| CHEMBL5182371 | — | — | 1 | 10.00 |
| CHEMBL5182339 | — | — | 1 | 9.97 |
| CHEMBL5202305 | — | — | 1 | 9.82 |
| CHEMBL5189517 | — | — | 1 | 9.80 |
| CHEMBL5171276 | — | — | 1 | 9.73 |
| CHEMBL5209394 | — | — | 1 | 9.54 |
| CHEMBL5209238 | — | — | 1 | 9.49 |
| CHEMBL5181675 | — | — | 1 | 9.49 |
| CHEMBL3771364 | — | — | 1 | 9.46 |
| CHEMBL5192172 | — | — | 1 | 9.45 |
| CHEMBL5204346 | — | — | 1 | 9.36 |
| CHEMBL5194906 | — | — | 1 | 9.25 |
| CHEMBL5184370 | — | — | 1 | 9.17 |
| CHEMBL5186223 | — | — | 1 | 9.16 |
| CHEMBL5185638 | — | — | 1 | 9.10 |
| CHEMBL5202964 | — | — | 1 | 9.07 |
| CHEMBL5192556 | — | — | 1 | 8.60 |
| CHEMBL5206005 | — | — | 1 | 8.53 |
| CHEMBL5202549 | — | — | 1 | 8.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5208487 | — | Ki | = | 0.026 | nM | 10.59 |
| CHEMBL4650215 | INAVOLISIB | Ki | = | 0.034 | nM | 10.47 |
| CHEMBL5199631 | — | Ki | = | 0.042 | nM | 10.38 |
| CHEMBL5198796 | — | Ki | = | 0.043 | nM | 10.37 |
| CHEMBL5186155 | — | Ki | = | 0.051 | nM | 10.29 |
| CHEMBL5209168 | — | Ki | = | 0.053 | nM | 10.28 |
| CHEMBL5196718 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL5209048 | — | Ki | = | 0.062 | nM | 10.21 |
| CHEMBL2387080 | TASELISIB | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL5205438 | — | Ki | = | 0.095 | nM | 10.02 |
| CHEMBL5181348 | — | Ki | = | 0.097 | nM | 10.01 |
| CHEMBL5182371 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL5182339 | — | Ki | = | 0.107 | nM | 9.97 |
| CHEMBL5202305 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL5189517 | — | Ki | = | 0.157 | nM | 9.80 |
| CHEMBL5171276 | — | Ki | = | 0.188 | nM | 9.73 |
| CHEMBL5209394 | — | Ki | = | 0.289 | nM | 9.54 |
| CHEMBL5181675 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL5209238 | — | Ki | = | 0.323 | nM | 9.49 |
| CHEMBL3771364 | — | Ki | = | 0.346 | nM | 9.46 |
| CHEMBL5192172 | — | Ki | = | 0.355 | nM | 9.45 |
| CHEMBL5204346 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL5194906 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL5184370 | — | Ki | = | 0.681 | nM | 9.17 |
| CHEMBL5186223 | — | Ki | = | 0.692 | nM | 9.16 |
| CHEMBL5185638 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL5202964 | — | Ki | = | 0.853 | nM | 9.07 |
| CHEMBL5192556 | — | Ki | = | 2.52 | nM | 8.60 |
| CHEMBL5206005 | — | Ki | = | 2.97 | nM | 8.53 |
| CHEMBL5202549 | — | Ki | = | 3.15 | nM | 8.50 |
| CHEMBL5176372 | — | Ki | = | 3.24 | nM | 8.49 |
| CHEMBL5193496 | — | Ki | = | 3.82 | nM | 8.42 |
| CHEMBL5205873 | — | Ki | = | 5.75 | nM | 8.24 |
| CHEMBL5173962 | — | Ki | = | 6.49 | nM | 8.19 |
| CHEMBL5202681 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL5181023 | — | Ki | = | 30.3 | nM | 7.52 |