Assay Detail
Binding
CHEMBL4051855
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length recombinant human N-terminal His-tagged PI3K p110alpha/p85alpha expressed in baculovirus using PIP2 as substrate after 1 hr by kinase-glo luminescence assay
37
Total Activities
37
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 Biological Evaluation of Dimorpholine Substituted Thienopyrimidines as Potential Class I PI3K/mTOR Dual Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 6.29 | 8.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 8.32 |
| CHEMBL4071083 | — | — | 1 | 7.82 |
| CHEMBL4060108 | — | — | 1 | 7.62 |
| CHEMBL4064087 | — | — | 1 | 6.91 |
| CHEMBL4068220 | — | — | 1 | 6.78 |
| CHEMBL4082222 | — | — | 1 | 6.72 |
| CHEMBL4076699 | — | — | 1 | 6.71 |
| CHEMBL4088600 | — | — | 1 | 6.67 |
| CHEMBL4078390 | — | — | 1 | 6.67 |
| CHEMBL4092492 | — | — | 1 | 6.62 |
| CHEMBL4066144 | — | — | 1 | 6.62 |
| CHEMBL4063088 | — | — | 1 | 6.60 |
| CHEMBL4084746 | — | — | 1 | 6.55 |
| CHEMBL4080009 | — | — | 1 | 6.55 |
| CHEMBL4100237 | — | — | 1 | 6.52 |
| CHEMBL4063923 | — | — | 1 | 6.17 |
| CHEMBL4092947 | — | — | 1 | 6.17 |
| CHEMBL4098035 | — | — | 1 | 6.16 |
| CHEMBL4101802 | — | — | 1 | 6.00 |
| CHEMBL4104267 | — | — | 1 | 5.99 |
| CHEMBL4097432 | — | — | 1 | 5.91 |
| CHEMBL4065390 | — | — | 1 | 5.73 |
| CHEMBL4071702 | — | — | 1 | 5.69 |
| CHEMBL4086949 | — | — | 1 | 5.66 |
| CHEMBL4065513 | — | — | 1 | 5.45 |
| CHEMBL4077217 | — | — | 1 | 5.38 |
| CHEMBL4066277 | — | — | 1 | 5.32 |
| CHEMBL4060857 | — | — | 1 | 5.30 |
| CHEMBL4084177 | — | — | 1 | 5.21 |
| CHEMBL4095594 | — | — | 1 | 5.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL521851 | PICTILISIB | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4071083 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4060108 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4064087 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL4068220 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL4082222 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL4076699 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL4088600 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL4078390 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL4066144 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL4092492 | — | IC50 | = | 239.0 | nM | 6.62 |
| CHEMBL4063088 | — | IC50 | = | 249.0 | nM | 6.60 |
| CHEMBL4084746 | — | IC50 | = | 279.0 | nM | 6.55 |
| CHEMBL4080009 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL4100237 | — | IC50 | = | 299.0 | nM | 6.52 |
| CHEMBL4063923 | — | IC50 | = | 681.0 | nM | 6.17 |
| CHEMBL4092947 | — | IC50 | = | 675.0 | nM | 6.17 |
| CHEMBL4098035 | — | IC50 | = | 694.0 | nM | 6.16 |
| CHEMBL4101802 | — | IC50 | = | 995.0 | nM | 6.00 |
| CHEMBL4104267 | — | IC50 | = | 1034.0 | nM | 5.99 |
| CHEMBL4097432 | — | IC50 | = | 1242.0 | nM | 5.91 |
| CHEMBL4065390 | — | IC50 | = | 1875.0 | nM | 5.73 |
| CHEMBL4071702 | — | IC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL4086949 | — | IC50 | = | 2203.0 | nM | 5.66 |
| CHEMBL4065513 | — | IC50 | = | 3562.0 | nM | 5.45 |
| CHEMBL4077217 | — | IC50 | = | 4185.0 | nM | 5.38 |
| CHEMBL4066277 | — | IC50 | = | 4817.0 | nM | 5.32 |
| CHEMBL4060857 | — | IC50 | = | 4955.0 | nM | 5.30 |
| CHEMBL4084177 | — | IC50 | = | 6184.0 | nM | 5.21 |
| CHEMBL4095594 | — | IC50 | = | 9468.0 | nM | 5.02 |
| CHEMBL4100335 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4062102 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4087892 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4069279 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4090324 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4066648 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4100890 | — | IC50 | > | 10000.0 | nM | - |