Assay Detail
Binding
CHEMBL4845570
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Inhibition of PI3Kalpha (unknown origin) by ADP-Glo assay
24
Total Activities
24
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
Macrocyclization as a Source of Desired Polypharmacology. Discovery of Triple PI3K/mTOR/PIM Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.10 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4878958 | — | — | 1 | 9.89 |
| CHEMBL4860369 | — | — | 1 | 9.64 |
| CHEMBL4876895 | — | — | 1 | 9.37 |
| CHEMBL4869487 | — | — | 1 | 9.18 |
| CHEMBL1236962 | OMIPALISIB | 2.0 | 1 | 8.99 |
| CHEMBL4866710 | — | — | 1 | 8.51 |
| CHEMBL4860117 | — | — | 1 | 8.50 |
| CHEMBL4851911 | — | — | 1 | 8.48 |
| CHEMBL4854645 | — | — | 1 | 8.20 |
| CHEMBL4854225 | — | — | 1 | 8.20 |
| CHEMBL4874628 | — | — | 1 | 8.17 |
| CHEMBL4866896 | — | — | 1 | 8.16 |
| CHEMBL4868086 | — | — | 1 | 8.13 |
| CHEMBL4854392 | — | — | 1 | 7.86 |
| CHEMBL4869696 | — | — | 1 | 7.78 |
| CHEMBL4862404 | — | — | 1 | 7.77 |
| CHEMBL4868512 | — | — | 1 | 7.72 |
| CHEMBL4870601 | — | — | 1 | 7.54 |
| CHEMBL4876693 | — | — | 1 | 7.44 |
| CHEMBL4859036 | — | — | 1 | 7.30 |
| CHEMBL4871634 | — | — | 1 | 7.23 |
| CHEMBL4851433 | — | — | 1 | 7.13 |
| CHEMBL4857726 | — | — | 1 | 6.91 |
| CHEMBL4857792 | — | — | 1 | 6.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4878958 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL4860369 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL4876895 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL4869487 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL1236962 | OMIPALISIB | IC50 | = | 1.02 | nM | 8.99 |
| CHEMBL4866710 | — | IC50 | = | 3.08 | nM | 8.51 |
| CHEMBL4860117 | — | IC50 | = | 3.15 | nM | 8.50 |
| CHEMBL4851911 | — | IC50 | = | 3.29 | nM | 8.48 |
| CHEMBL4854645 | — | IC50 | = | 6.34 | nM | 8.20 |
| CHEMBL4854225 | — | IC50 | = | 6.28 | nM | 8.20 |
| CHEMBL4874628 | — | IC50 | = | 6.72 | nM | 8.17 |
| CHEMBL4866896 | — | IC50 | = | 6.91 | nM | 8.16 |
| CHEMBL4868086 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4854392 | — | IC50 | = | 13.71 | nM | 7.86 |
| CHEMBL4869696 | — | IC50 | = | 16.77 | nM | 7.78 |
| CHEMBL4862404 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4868512 | — | IC50 | = | 19.03 | nM | 7.72 |
| CHEMBL4870601 | — | IC50 | = | 28.9 | nM | 7.54 |
| CHEMBL4876693 | — | IC50 | = | 36.23 | nM | 7.44 |
| CHEMBL4859036 | — | IC50 | = | 50.2 | nM | 7.30 |
| CHEMBL4871634 | — | IC50 | = | 58.3 | nM | 7.23 |
| CHEMBL4851433 | — | IC50 | = | 74.6 | nM | 7.13 |
| CHEMBL4857726 | — | IC50 | = | 123.4 | nM | 6.91 |
| CHEMBL4857792 | — | IC50 | = | 389.73 | nM | 6.41 |