Assay Detail
Binding
CHEMBL4022583
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Competitive inhibition of human PI3K p110alpha/p85alpha using PIP2 as substrate preincubated for 10 mins followed by ATP addition measured after 30 mins by HTRF assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and SAR of new-di-substituted pyridopyrimidines as ATP-competitive dual PI3Kα/mTOR inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 8.18 | 10.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1236962 | OMIPALISIB | 2.0 | 1 | 10.72 |
| CHEMBL4097194 | — | — | 1 | 9.62 |
| CHEMBL4065928 | — | — | 1 | 9.40 |
| CHEMBL4092587 | — | — | 1 | 9.24 |
| CHEMBL4104902 | — | — | 1 | 9.20 |
| CHEMBL4081617 | — | — | 1 | 8.78 |
| CHEMBL4102783 | — | — | 1 | 8.73 |
| CHEMBL573339 | PI-103 | — | 1 | 8.70 |
| CHEMBL4103534 | — | — | 1 | 8.60 |
| CHEMBL4079178 | — | — | 1 | 8.60 |
| CHEMBL4087043 | — | — | 1 | 8.55 |
| CHEMBL4088235 | — | — | 1 | 8.54 |
| CHEMBL4059989 | — | — | 1 | 8.48 |
| CHEMBL4092840 | — | — | 1 | 8.45 |
| CHEMBL4088056 | — | — | 1 | 8.43 |
| CHEMBL4102715 | — | — | 1 | 8.38 |
| CHEMBL4065878 | — | — | 1 | 8.27 |
| CHEMBL4079272 | — | — | 1 | 8.25 |
| CHEMBL4064842 | — | — | 1 | 8.24 |
| CHEMBL4087157 | — | — | 1 | 8.22 |
| CHEMBL4092544 | — | — | 1 | 8.11 |
| CHEMBL4084790 | — | — | 1 | 7.46 |
| CHEMBL3109141 | — | — | 1 | 7.40 |
| CHEMBL4059778 | — | — | 1 | 7.33 |
| CHEMBL4072084 | — | — | 1 | 7.30 |
| CHEMBL3109142 | — | — | 1 | 7.24 |
| CHEMBL4095781 | — | — | 1 | 7.14 |
| CHEMBL4068435 | — | — | 1 | 7.12 |
| CHEMBL4065735 | — | — | 1 | 6.88 |
| CHEMBL4069475 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1236962 | OMIPALISIB | IC50 | = | 0.019 | nM | 10.72 |
| CHEMBL4097194 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL4065928 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4092587 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL4104902 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL4081617 | — | IC50 | = | 1.67 | nM | 8.78 |
| CHEMBL4102783 | — | IC50 | = | 1.88 | nM | 8.73 |
| CHEMBL573339 | PI-103 | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4103534 | — | IC50 | = | 2.54 | nM | 8.60 |
| CHEMBL4079178 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4087043 | — | IC50 | = | 2.79 | nM | 8.55 |
| CHEMBL4088235 | — | IC50 | = | 2.85 | nM | 8.54 |
| CHEMBL4059989 | — | IC50 | = | 3.27 | nM | 8.48 |
| CHEMBL4092840 | — | IC50 | = | 3.57 | nM | 8.45 |
| CHEMBL4088056 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4102715 | — | IC50 | = | 4.14 | nM | 8.38 |
| CHEMBL4065878 | — | IC50 | = | 5.39 | nM | 8.27 |
| CHEMBL4079272 | — | IC50 | = | 5.59 | nM | 8.25 |
| CHEMBL4064842 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4087157 | — | IC50 | = | 6.07 | nM | 8.22 |
| CHEMBL4092544 | — | IC50 | = | 7.83 | nM | 8.11 |
| CHEMBL4084790 | — | IC50 | = | 34.5 | nM | 7.46 |
| CHEMBL3109141 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4059778 | — | IC50 | = | 46.2 | nM | 7.33 |
| CHEMBL4072084 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3109142 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4095781 | — | IC50 | = | 71.6 | nM | 7.14 |
| CHEMBL4068435 | — | IC50 | = | 76.7 | nM | 7.12 |
| CHEMBL4065735 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL4069475 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL2336325 | VISTUSERTIB | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4089494 | — | IC50 | < | 0.5 | nM | - |
| CHEMBL4060651 | — | IC50 | < | 0.5 | nM | - |