Assay Detail
ADMET
CHEMBL4670193
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant N-terminal GST-tagged full-length human PI3K p110delta/p85alpha co- expressed in Sf9 insect cells using phosphatidylinositol 4,5-bisphosphate as substrate preincubated for 60 mins followed by substrate addition and measured after 1 hr in presence of ATP by ADP-Glo lipid kinase assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of Potent and Selective PI3Kγ Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 5.69 | 6.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4740423 | — | — | 1 | 6.90 |
| CHEMBL4762555 | — | — | 1 | 6.68 |
| CHEMBL4742062 | — | — | 1 | 6.34 |
| CHEMBL4798877 | — | — | 1 | 5.94 |
| CHEMBL4782083 | — | — | 1 | 5.88 |
| CHEMBL4126445 | — | — | 1 | 5.75 |
| CHEMBL4783357 | — | — | 1 | 5.66 |
| CHEMBL4740304 | — | — | 1 | 5.65 |
| CHEMBL4752240 | — | — | 1 | 5.62 |
| CHEMBL4785086 | — | — | 1 | 5.58 |
| CHEMBL4745355 | — | — | 1 | 5.57 |
| CHEMBL4779748 | — | — | 1 | 5.49 |
| CHEMBL4740608 | — | — | 1 | 5.46 |
| CHEMBL4761503 | — | — | 1 | 5.34 |
| CHEMBL4759380 | — | — | 1 | 5.34 |
| CHEMBL4743121 | — | — | 1 | 5.33 |
| CHEMBL4740456 | — | — | 1 | 5.22 |
| CHEMBL4778393 | — | — | 1 | 5.21 |
| CHEMBL4789901 | — | — | 1 | 5.09 |
| CHEMBL4752498 | — | — | 1 | - |
| CHEMBL4744486 | — | — | 1 | - |
| CHEMBL4749404 | — | — | 1 | - |
| CHEMBL4782224 | — | — | 1 | - |
| CHEMBL4762674 | — | — | 1 | - |
| CHEMBL4746190 | — | — | 1 | - |
| CHEMBL4752359 | — | — | 1 | - |
| CHEMBL4793165 | — | — | 1 | - |
| CHEMBL4746682 | — | — | 1 | - |
| CHEMBL4791781 | — | — | 1 | - |
| CHEMBL4764239 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4740423 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4762555 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4742062 | — | IC50 | = | 459.0 | nM | 6.34 |
| CHEMBL4798877 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL4782083 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL4126445 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL4783357 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4740304 | — | IC50 | = | 2240.0 | nM | 5.65 |
| CHEMBL4752240 | — | IC50 | = | 2380.0 | nM | 5.62 |
| CHEMBL4785086 | — | IC50 | = | 2610.0 | nM | 5.58 |
| CHEMBL4745355 | — | IC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL4779748 | — | IC50 | = | 3250.0 | nM | 5.49 |
| CHEMBL4740608 | — | IC50 | = | 3440.0 | nM | 5.46 |
| CHEMBL4759380 | — | IC50 | = | 4550.0 | nM | 5.34 |
| CHEMBL4761503 | — | IC50 | = | 4550.0 | nM | 5.34 |
| CHEMBL4743121 | — | IC50 | = | 4660.0 | nM | 5.33 |
| CHEMBL4740456 | — | IC50 | = | 6050.0 | nM | 5.22 |
| CHEMBL4778393 | — | IC50 | = | 6140.0 | nM | 5.21 |
| CHEMBL4789901 | — | IC50 | = | 8210.0 | nM | 5.09 |
| CHEMBL4742806 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4755285 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4792935 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4743136 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4755842 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4784554 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4797944 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4794833 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4764627 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4764239 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4791781 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4746682 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4793165 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4752359 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4746190 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4762674 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4782224 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4749404 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4744486 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4752498 | — | IC50 | > | 10000.0 | nM | - |