Assay Detail
ADMET
CHEMBL4670190
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Inhibition of recombinant N-terminal FLAG-tagged full-length human PI3K p110alpha/human 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 | 5.72 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4740423 | — | — | 1 | 7.08 |
| CHEMBL4762555 | — | — | 1 | 7.02 |
| CHEMBL4742062 | — | — | 1 | 6.71 |
| CHEMBL4798877 | — | — | 1 | 5.94 |
| CHEMBL4740304 | — | — | 1 | 5.82 |
| CHEMBL4782083 | — | — | 1 | 5.71 |
| CHEMBL4745355 | — | — | 1 | 5.70 |
| CHEMBL4779748 | — | — | 1 | 5.65 |
| CHEMBL4789901 | — | — | 1 | 5.61 |
| CHEMBL4783357 | — | — | 1 | 5.56 |
| CHEMBL4126445 | — | — | 1 | 5.41 |
| CHEMBL4740608 | — | — | 1 | 5.38 |
| CHEMBL4743121 | — | — | 1 | 5.26 |
| CHEMBL4740456 | — | — | 1 | 5.20 |
| CHEMBL4785086 | — | — | 1 | 5.08 |
| CHEMBL4778393 | — | — | 1 | 5.05 |
| CHEMBL4759380 | — | — | 1 | 5.01 |
| CHEMBL4752498 | — | — | 1 | - |
| CHEMBL4761503 | — | — | 1 | - |
| CHEMBL4749404 | — | — | 1 | - |
| CHEMBL4744486 | — | — | 1 | - |
| CHEMBL4782224 | — | — | 1 | - |
| CHEMBL4762674 | — | — | 1 | - |
| CHEMBL4746190 | — | — | 1 | - |
| CHEMBL4752359 | — | — | 1 | - |
| CHEMBL4793165 | — | — | 1 | - |
| CHEMBL4746682 | — | — | 1 | - |
| CHEMBL4791781 | — | — | 1 | - |
| CHEMBL4764239 | — | — | 1 | - |
| CHEMBL4764627 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4740423 | — | IC50 | = | 82.4 | nM | 7.08 |
| CHEMBL4762555 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4742062 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL4798877 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL4740304 | — | IC50 | = | 1510.0 | nM | 5.82 |
| CHEMBL4782083 | — | IC50 | = | 1940.0 | nM | 5.71 |
| CHEMBL4745355 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL4779748 | — | IC50 | = | 2260.0 | nM | 5.65 |
| CHEMBL4789901 | — | IC50 | = | 2470.0 | nM | 5.61 |
| CHEMBL4783357 | — | IC50 | = | 2730.0 | nM | 5.56 |
| CHEMBL4126445 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4740608 | — | IC50 | = | 4140.0 | nM | 5.38 |
| CHEMBL4743121 | — | IC50 | = | 5450.0 | nM | 5.26 |
| CHEMBL4740456 | — | IC50 | = | 6290.0 | nM | 5.20 |
| CHEMBL4785086 | — | IC50 | = | 8340.0 | nM | 5.08 |
| CHEMBL4778393 | — | IC50 | = | 8970.0 | nM | 5.05 |
| CHEMBL4759380 | — | IC50 | = | 9850.0 | nM | 5.01 |
| 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 | - |
| CHEMBL4752240 | — | 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 | - |
| CHEMBL4744486 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4749404 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4761503 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4752498 | — | IC50 | > | 10000.0 | nM | - |