Assay Detail
Binding
CHEMBL4716068
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Inhibition of recombinant full length N-terminal polyHis-tagged PI3K p110delta/p85alpha (unknown origin) expressed in baculovirus infected Sf9 cells using PIP2 as substrate in presence of ATP incubated for 20 mins by Alphascreen assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.47 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4790186 | — | — | 1 | 9.40 |
| CHEMBL4762294 | — | — | 1 | 9.10 |
| CHEMBL4747926 | — | — | 1 | 8.72 |
| CHEMBL2216895 | — | — | 1 | 8.66 |
| CHEMBL4780867 | — | — | 1 | 8.44 |
| CHEMBL4784595 | — | — | 1 | 7.92 |
| CHEMBL4763849 | — | — | 1 | 7.80 |
| CHEMBL4747799 | — | — | 1 | 7.77 |
| CHEMBL4754382 | — | — | 1 | 7.72 |
| CHEMBL2171931 | — | — | 1 | 7.70 |
| CHEMBL4745140 | — | — | 1 | 7.64 |
| CHEMBL4788529 | — | — | 1 | 7.16 |
| CHEMBL4740720 | — | — | 1 | 7.10 |
| CHEMBL4761860 | — | — | 1 | 6.99 |
| CHEMBL4800111 | — | — | 1 | 6.97 |
| CHEMBL4756545 | — | — | 1 | 6.96 |
| CHEMBL4756034 | — | — | 1 | 6.95 |
| CHEMBL4763925 | — | — | 1 | 6.75 |
| CHEMBL4744888 | — | — | 1 | 6.24 |
| CHEMBL4798019 | — | — | 1 | 6.21 |
| CHEMBL4784596 | — | — | 1 | 4.74 |
| CHEMBL4759169 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4790186 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4762294 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4747926 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL2216895 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4780867 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4784595 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4763849 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4747799 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4754382 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2171931 | — | IC50 | = | 20.2 | nM | 7.70 |
| CHEMBL4745140 | — | IC50 | = | 22.8 | nM | 7.64 |
| CHEMBL4788529 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4740720 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4761860 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL4800111 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4756545 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4756034 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL4763925 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL4744888 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4798019 | — | IC50 | = | 612.0 | nM | 6.21 |
| CHEMBL4784596 | — | IC50 | = | 18300.0 | nM | 4.74 |
| CHEMBL4759169 | — | IC50 | > | 125000.0 | nM | - |