Assay Detail
Binding
CHEMBL3223603
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin)
31
Total Activities
31
Compounds Tested
2
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
Small molecules targeting phosphoinositide 3-kinases
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.10 | 10.40 |
| Ki | 1 | 9.24 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1236962 | OMIPALISIB | 2.0 | 1 | 10.40 |
| CHEMBL592445 | GEDATOLISIB | 3.0 | 1 | 9.40 |
| CHEMBL3218579 | — | — | 1 | 9.24 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 8.52 |
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | 8.40 |
| CHEMBL1922094 | APITOLISIB | 2.0 | 1 | 8.30 |
| CHEMBL1241857 | — | — | 1 | 7.96 |
| CHEMBL1684984 | IZORLISIB | 2.0 | 1 | 7.85 |
| CHEMBL586702 | ZSTK-474 | 2.0 | 1 | 7.80 |
| CHEMBL1233882 | — | — | 1 | 7.77 |
| CHEMBL1233881 | — | — | 1 | 7.77 |
| CHEMBL3218571 | — | — | 1 | 7.64 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 7.52 |
| CHEMBL3218581 | — | — | 1 | 7.50 |
| CHEMBL1229535 | — | — | 1 | 7.41 |
| CHEMBL3349370 | — | — | 1 | 7.41 |
| CHEMBL3218575 | — | — | 1 | 7.41 |
| CHEMBL1081312 | — | — | 1 | 7.28 |
| CHEMBL3218580 | — | — | 1 | 6.45 |
| CHEMBL1230790 | — | — | 1 | 6.32 |
| CHEMBL2216870 | IDELALISIB | 4.0 | 1 | 6.09 |
| CHEMBL1234815 | — | — | 1 | 5.96 |
| CHEMBL3218574 | — | — | 1 | 5.96 |
| CHEMBL2064328 | — | — | 1 | 5.58 |
| CHEMBL3218573 | — | — | 1 | 5.35 |
| CHEMBL2181110 | — | — | 1 | 5.00 |
| CHEMBL478980 | — | — | 1 | 4.50 |
| CHEMBL3218572 | — | — | 1 | 4.21 |
| CHEMBL1213082 | — | — | 1 | - |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1236962 | OMIPALISIB | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL592445 | GEDATOLISIB | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3218579 | — | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL521851 | PICTILISIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1879463 | DACTOLISIB | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1922094 | APITOLISIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1241857 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1684984 | IZORLISIB | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL586702 | ZSTK-474 | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1233882 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1233881 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3218571 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2017974 | BUPARLISIB | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3218581 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1229535 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3349370 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3218575 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL1081312 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3218580 | — | IC50 | = | 356.0 | nM | 6.45 |
| CHEMBL1230790 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL2216870 | IDELALISIB | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL1234815 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3218574 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2064328 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3218573 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL2181110 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL478980 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL3218572 | — | IC50 | = | 61000.0 | nM | 4.21 |
| CHEMBL1213082 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1355736 | THEOPHYLLINE | IC50 | = | 300000.0 | nM | - |
| CHEMBL113 | CAFFEINE | IC50 | = | 400000.0 | nM | - |