Assay Detail
Binding
CHEMBL5153854
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Inhibition of PI3Kalpha H1047R mutant in human HCC1954 cells assessed as reduction in PRAS40 phosphorylation after 24 hrs by electrochemiluminescent assay
17
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HCC1954 |
| 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 |
|---|---|---|---|
| EC50 | 15 | 7.33 | 7.72 |
| Inhibition | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4650215 | INAVOLISIB | 4.0 | 1 | 7.72 |
| CHEMBL2387080 | TASELISIB | 3.0 | 1 | 7.62 |
| CHEMBL5186155 | — | — | 1 | 7.57 |
| CHEMBL5196718 | — | — | 1 | 7.55 |
| CHEMBL5209048 | — | — | 1 | 7.41 |
| CHEMBL5202305 | — | — | 1 | 7.40 |
| CHEMBL5205438 | — | — | 1 | 7.31 |
| CHEMBL5182371 | — | — | 1 | 7.28 |
| CHEMBL5189517 | — | — | 1 | 7.25 |
| CHEMBL5192172 | — | — | 1 | 7.20 |
| CHEMBL5182339 | — | — | 1 | 7.19 |
| CHEMBL3771364 | — | — | 1 | 7.05 |
| CHEMBL5186223 | — | — | 1 | 6.80 |
| CHEMBL5198796 | — | — | 1 | - |
| CHEMBL5209168 | — | — | 1 | - |
| CHEMBL5208487 | — | — | 1 | - |
| CHEMBL5171276 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4650215 | INAVOLISIB | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2387080 | TASELISIB | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5186155 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5196718 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5209048 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5202305 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5205438 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5182371 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5189517 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5192172 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5182339 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3771364 | — | EC50 | = | 89.0 | nM | 7.05 |
| CHEMBL5186223 | — | EC50 | = | 157.0 | nM | 6.80 |
| CHEMBL5198796 | — | Inhibition | - | % | - | |
| CHEMBL5209168 | — | Inhibition | - | % | - | |
| CHEMBL5208487 | — | EC50 | - | — | - | |
| CHEMBL5171276 | — | EC50 | - | — | - |