Assay Detail
Binding
CHEMBL934448
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3K expressed in Escherichia coli by microtiter plate-based fluorescence polarization assay
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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
Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 7.09 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273832 | — | — | 1 | 8.57 |
| CHEMBL272898 | — | — | 1 | 8.30 |
| CHEMBL409427 | — | — | 1 | 8.08 |
| CHEMBL272816 | — | — | 1 | 8.02 |
| CHEMBL407214 | — | — | 1 | 8.00 |
| CHEMBL272897 | — | — | 1 | 7.92 |
| CHEMBL405258 | — | — | 1 | 7.82 |
| CHEMBL272595 | — | — | 1 | 7.66 |
| CHEMBL429577 | — | — | 1 | 7.62 |
| CHEMBL407215 | — | — | 1 | 7.62 |
| CHEMBL273038 | — | — | 1 | 7.51 |
| CHEMBL410071 | — | — | 1 | 7.48 |
| CHEMBL411950 | — | — | 1 | 7.43 |
| CHEMBL271780 | — | — | 1 | 7.42 |
| CHEMBL271544 | — | — | 1 | 7.37 |
| CHEMBL408074 | — | — | 1 | 7.35 |
| CHEMBL409671 | — | — | 1 | 7.30 |
| CHEMBL271184 | — | — | 1 | 7.25 |
| CHEMBL260313 | — | — | 1 | 7.22 |
| CHEMBL405230 | — | — | 1 | 7.20 |
| CHEMBL410643 | — | — | 1 | 7.19 |
| CHEMBL271257 | — | — | 1 | 7.18 |
| CHEMBL271982 | — | — | 1 | 7.11 |
| CHEMBL406237 | — | — | 1 | 7.06 |
| CHEMBL411907 | SONOLISIB | 2.0 | 1 | 7.06 |
| CHEMBL410637 | — | — | 1 | 7.05 |
| CHEMBL271430 | — | — | 1 | 7.04 |
| CHEMBL270039 | — | — | 1 | 6.98 |
| CHEMBL271413 | — | — | 1 | 6.90 |
| CHEMBL270553 | — | — | 1 | 6.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273832 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL272898 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL409427 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL272816 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL407214 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL272897 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL405258 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL272595 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL429577 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL407215 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL273038 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL410071 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL411950 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL271780 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL271544 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL408074 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL409671 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL271184 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL260313 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL405230 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL410643 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL271257 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL271982 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL411907 | SONOLISIB | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL406237 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL410637 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL271430 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL270039 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL271413 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL270553 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL272593 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL409620 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL272197 | — | IC50 | = | 382.0 | nM | 6.42 |
| CHEMBL270746 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL405157 | — | IC50 | = | 444.0 | nM | 6.35 |
| CHEMBL428873 | — | IC50 | = | 496.0 | nM | 6.30 |
| CHEMBL410644 | — | IC50 | = | 638.0 | nM | 6.20 |
| CHEMBL409251 | — | IC50 | = | 635.0 | nM | 6.20 |
| CHEMBL412076 | — | IC50 | = | 918.0 | nM | 6.04 |
| CHEMBL271190 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL272281 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL406655 | — | IC50 | = | 7850.0 | nM | 5.11 |
| CHEMBL272190 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL409294 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL271191 | — | IC50 | > | 10000.0 | nM | - |