Assay Detail
Binding
CHEMBL3611486
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Inhibition of PI3Kalpha (unknown origin)
29
Total Activities
29
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
Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.22 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2396661 | ALPELISIB | 4.0 | 1 | 8.30 |
| CHEMBL2397186 | — | — | 1 | 8.15 |
| CHEMBL3609540 | — | — | 1 | 7.85 |
| CHEMBL3608927 | — | — | 1 | 7.85 |
| CHEMBL3218581 | — | — | 1 | 7.82 |
| CHEMBL3609536 | — | — | 1 | 7.70 |
| CHEMBL3608926 | — | — | 1 | 7.66 |
| CHEMBL3608928 | — | — | 1 | 7.62 |
| CHEMBL3609545 | — | — | 1 | 7.58 |
| CHEMBL3608924 | — | — | 1 | 7.52 |
| CHEMBL3609538 | — | — | 1 | 7.48 |
| CHEMBL3608930 | — | — | 1 | 7.41 |
| CHEMBL3609543 | — | — | 1 | 7.41 |
| CHEMBL3608929 | — | — | 1 | 7.37 |
| CHEMBL3609542 | — | — | 1 | 7.36 |
| CHEMBL3609537 | — | — | 1 | 7.16 |
| CHEMBL3608931 | — | — | 1 | 7.15 |
| CHEMBL3608932 | — | — | 1 | 7.08 |
| CHEMBL3609539 | — | — | 1 | 7.06 |
| CHEMBL3608925 | — | — | 1 | 7.00 |
| CHEMBL3609544 | — | — | 1 | 6.80 |
| CHEMBL3608933 | — | — | 1 | 6.77 |
| CHEMBL2071330 | — | — | 1 | 6.75 |
| CHEMBL3608936 | — | — | 1 | 6.75 |
| CHEMBL3608321 | — | — | 1 | 6.68 |
| CHEMBL2071336 | — | — | 1 | 6.55 |
| CHEMBL3608934 | — | — | 1 | 6.28 |
| CHEMBL3609541 | — | — | 1 | 6.26 |
| CHEMBL3608935 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2396661 | ALPELISIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2397186 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3609540 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3608927 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3218581 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3609536 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3608926 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3608928 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3609545 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3608924 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3609538 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3608930 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3609543 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3608929 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3609542 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3609537 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3608931 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3608932 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL3609539 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3608925 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3609544 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3608933 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2071330 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3608936 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3608321 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL2071336 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3608934 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL3609541 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL3608935 | — | IC50 | = | 1200.0 | nM | 5.92 |